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Overview of Pharmacology Principles

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188 views386 pages

Overview of Pharmacology Principles

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jerishbrijit
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
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UNIT – I –

INTRODUCTION Of PHARMACOLOGY

Pharmacology in the science of that deals ̅ the study of the drug and there instruction ̅ the living system the word
pharmacology is derived from Greek word pharmacon which means drug and logus means study.

Pharmaco kinetics movement

Pharmacology

Pharmacodynamics effect / power

Pharmacology → study of drug

Pharmacon + logos

Drugs to study

Drogs

Dry hub

( first medicine)

Definition –

It include study of pharmacokinetics and pharmacodynamics

It is scientific study of drug movement (ADME) and its effect (Power) on human body is called as pharmacology.
Pharmacokinetics :-

study of drug movement inside the body.

Drug movement involves absorption, distribution, metabolism and exertion.

Pharmacokinetics is also known as what the body does to the drug.

Pharmacodynamics : -

study of drug effect on living system is called as pharmacodynamics.

It is also k/a what the drug does to the body.


Pharmacotherapeutics :-

use of drug for the treatment of disease by the help of pathological states and use of relevant drugs.
Drug :-

drogue (dry hub) → first medicine drug is anything chemical substance that intended to use for prevention, prophylaxis,
treatment, diagnosis and disease of living system.

The definition do not cover oral contraceptives and vitamins as drug.

Acc. to WHO considered both as drugs and revised definition – “ drug is anything that is also use to change, modify,
physiological system for human benefits.”

Definition of drug –

Acc to WHO, drug is anything (chemical substance) that is intended to use for prevention, prophylaxis, treatment,
diagnosis of disease and also use to change modify physiological system for human benfits.

NOMENCLATURE OF DRUGS →
Chemical Name – It is IUPAC name of drug that denotes
chemical of drug.
Eg:- Acetyl salicylic acid.
That are not easy to pronounce and remember so they are not
commonly use.
Generic Name/Non Property/Non Brand
These name are move popular in compare of chemical name.
They are salt name.
They are easy to remember and easy to pronounce.
Eg.:- Aspirin.
They are easy to remember and easy to pronounce Eg. Aspirin.
They are the name of drug by them drug is k/a in market.
Property Name/Brand Name –
They are the marketed or brand name of a drug that are given
by his or her particular company to a particular salt. Eg.- Disprin

Chemical Name Generic Name Brand Name


Acetyl salicylic Aspirin Disprin
Acid
Acetaaminophen Paracetamol Calpol

Therapeutic – Deals the use of drugs in the prevention and


treatment of disease.
Toxicity – Deals the adverse effect of drug and also the study
of poisons, that is detection, prevention and treatment of
poising.
Chemotherapy – It is the use of chemicals you the treatment of
infections. The term how also includes the use of chemical
compounds to treat the malignancies.
Clinical Pharmacology – It is the scientific study of the drug in a
poison. It includes pharmacokinetics and pharmacodynamics,
investigation of healthy voluntary and in patient evaluation of
efficiency and safety of drug and comparative tries other
forms of treatment.
This aim of clinical Pharmacology is generate data for optimum
use of drugs.
*Pharmacy – It is the science of identification, compounding
and dispensing of drugs. It also includes collection, isolation,
synthesis, purification and standardization of medicinal
substances.
*Sources of drug – The sources of drug will be natural and
synthetic.
Natural sources – Drugs can be obtained from
1. Plants – Morphine, Atropine and digoxin.
2. Animals – Insulin, Heparin, Antitoxic – sera, gonadotropins.
3. Minerals – Magnesium sulphate, Aluminum hydroxide,
sulphar, radioactive isotopes such as cobalt 60, and most
commonly iron.
4. Micro-organism – Antibacterial agents are obtained from
some bacteria and fungi, eg:- Tetracycline, cephalosporin’s
penicillin and other antibiotics.
5. Human – some drugs are obtained from man,
immunoglobulin from blood, growth hormone from anterior
Pituitary gland and chorionic gonadotropin from the urine of
pregnant women.
Synthetic sources – Most drugs are now synthesized
Eg:- Quinolones, omeprazole, sulphanamides and Neostigmine.
Many drugs are obtained by cell cultures.
Eg:- Ureokinase
From cultured human kidney cells.
Eg:- Human insulin, tissue Plasminogen activator.

Drug information sources – Drug compendia books that are


sources of information on drugs that is Pharmacopoeias and
formularies are together known as drug compendia. It is of 2
types –
1. Official compendia → It include information sources or books
on drugs which are recognized by the government of that
country as legal standard thus, Indian Pharmacopoeias Natural
formulary, British Pharmacopoeia, British Pharmaceutical codex,
united states pharmacopoeia are official compendia.
(a) Pharmacopoeia – it is the official publication containing a list
of drugs and medicinal preparations.
- In greek, ‘Pharmacon’ means drug and ‘Poeia’ means to make.

Types of drug action – A drug may produce more than one


effect due to ‘its’ chemical makeup and Physiological action
which are classified as follows –
1. Therapeutic effect – It is an intended or Produced
Physiological response that a drug causes each drug has a
derived effect.
2. Side effect – These may be harmless or injurious. They have
predictable response to a drug which cause unintended
secondary effect.
3. Toxic effect – These develop after prolonged intake of high
doses of medications or after prolonged use of a drug intended
you extend application or after a drug accumulates in the blood
because of impaired metabolism or excretion process.
4. Allergic reactions – It is an unpredictable response to a drug
which includes Pruritic, urticaria, eczema and unity.
5. Drug Tolerance – According to usual low metabolism or
response to a drug.
→ An increase in dose may be needed to cause or therapeutic
effect.
6. Drug Interaction – If a drug modified the action of another
drug, the drug interaction occurs.
→ Drug interactions are common in individuals who takes may
medications.
→ When 2 drugs are given simultaneously they can have a
synergistic effect.

#Principles of Drug Administration→


1. Drug administration should be considered in favour of client
health Promotion, early action, least side effects and rarely
complication occurs.
2. Drug should be certified by the Federal organization, state
govt. and local health department.
3. Drug c is to be prescribed should be in the written order by
the physician.
4. Nurse should inform the client about medication, its action
and its side effect.
5. Never administered drug against the clients willingness.
6. Before administer the drug is correct dose should be verified.
7. There should be reverification of the written order if the
nurse is not understand.
8. Unnecessary medicine should not be administered and follow
safety measures of drug administration.

*Factors influencing Drug action –


1. Age – Drug should be prescribed according to the age in
young age the absorption is faster and action is longer but in old
age absorption is slow.
2. Route of Administration:- Action of drug depends on routs of
administration as oral, IM, IV, subcutaneous etc. drugs has its
action on all over body while topical inhaler and rectal drugs
have more effect locally in comparison to all body.
3. Physiological Factor – As liver metabolized the drug, heart
circulate, kidney and skin excrete.
→ Functions of these organs also maintain drug action and
duration.
4. Timing of Administration – Some drugs have therapeutic
effect before the time of having meal like antacids, while some
drugs have maximum effects after meal like antibiotics.

5. Diet – High cholesterol and high fatty diet minimize the drug
action, iron should be taken citrus food. High fiber, High liquid
and High caloric diet se the drug effect.

6. Toxicity – Some drugs have need to evaluate its therapeutic


level in blood because toxicity of these drug may produce side
effect and complicated conditions are occur.
Normal level (0.6 to 1.2 meq/L)
Eg.:- Lithium
Toxic level (1.5-2 meq/L)
7. Other factors – Provide the rest and minimize the activities
produces long term affect while more activity during drugs
which se the effect of drug.
* Steroid have its maximum effects in the morning while
laxatives have its more effect before sleep.

#Essential drugs →
The WHO defined essential medicines are those that certifies
the priority health care need of the population, they are
selected due to regard public health relevance, evidence on
efficacy and safety comparative cost effectiveness.
#Availability of dosage form –
- If no choice like amikacin (injectable form for systemic use)
then we go for available form & route.
- If we have option in dosage form then we choose route acc. to
need.
- Disease condition Severe or mild.
- Patient condition is conscious or unconscious.
 Severe – Injectable
 Mild – Tablet form
 Unconscious – Injectable
 Conscious – Tablet form

Routes of Drug administration

Non Parenteral Parenteral


Oral and enteral Sub-cutaneous or
Sublingual Hypodermal (into
Buccal sub-cutaneous tissue)
Pulmonary route Intramuscular
(Inhalation) Intravenous
Topical Route Intra-arterial
Inunction Intra-cardial
Instillation Intraperitoneal
Irrigation Intraspinal or
Insertion Intrathecal
`In suffocation Intra-osseous
Implantation Route Intra-articular
(into joints)
Routes of drug administration

Local Systematic
- Topical Route - Nasal - Oral
- Deeper tissue route - Parentral - Rectal
- Arterial Route - IM - Sub-lingual
- IV - cutaneous
- ID - Inhalation
1. Local Routes – These routes can only be used for localized
region at the external or excess site or those drugs systemic
absorption is minimum or absent.
Therefore high concentration are desired at the external
application.
1.1 Topical Route –
It is defined as the external application of the drugs to
surface of the body to local action.
Drugs can be appropriately apply or delivered to localized
wound, lesions or trauma on skin, or pharyngeal airway, nasal
mucosa, eye, ear, anal canal or vagina in the form of lotion,
jelly, ointment, cream, powder, drop and spray.

1.2 Deeper tissue –


Some drugs are injected directly into the deeper tissue by
using injection or needle, these are those drugs whom
absorption is slow through systemic route.
Eg:- Intra-articular infection, Hydrocortisone acetate in knee
joints.
Infiltration around the nerve or intrathecal injection ledocan as
anaesthetic.
1.3 Arterial Route – These intra-arterial infection is used in
injection dye or contrast medium in angiography, anticancer
drugs can be infused directly into femoral or brachial artery.

2. Systemic Route – These drugs are administered through


systemic route and these follow absorption, distribution,
metabolism and excretion. These drugs are absorbed into blood
stream distributed all over including from site of action.

2.1 Oral Route –


- Oral Route of drug administration is the oldest & common
method of drug ingestion.
- Oral drug administration is cheaper, less help required, non
invasive, painless and not need to be sterile.
- Both solid such as powder, capsule, tablet or liquid form such
as syrup, emulsion, mixture those form are given by oral route.

2.2 Sub-lingual Route –


- Treatment an agent usually in tablet form placed under the
tongue or breath the tongue.

2.3 Buccal Route –


- Drug placed in the mouth and held b/w the check the gum
until dissolve and absorb through the buccal mucosa.
- The Tablet or Pallate containing drugs are placed under the
tongue or crushed slowly released in the mouth or spread over
the mucosa.
- Only lipid soluble and non-irritating drugs can give sub-
lingually, absorption of these are fast and these follow first pass
effect.
Eg:- NTG (Nitroglycerine)
2.4 Rectal Route –
- Some irritating drugs, unpleasant drugs can put in rectum as
suppositories or retention anemia for systemic effect.
- This route can also use if patient suffering from recurrent
vomiting or unconscious.
Eg:- Diazepam (sedative drugs), Indomethacin (Non-steroidal
anti-inflammatory drugs)
Paracetamol, Erygometrin are sometimes given rectally

Use to contract uterus during labour

2.5 Cutaneous Route→


- High lipid soluble drugs are applied over the skin for slow
prolonged absorption.
- These drugs are bypass from the liver.
- Absorption of these drugs can be increased by rubbing,
massaging the prepared drugs.
Eg:- Trans dermal patches, isosorbid dinitrate and pain killer
containing opoids.

2.6 Inhalation Route →


- Valatile liquid, fumes or gases are given by inhalation for
systematic action.
- Inhalation of budesonide for asthmatic attack hydrocordizon.
- Inhalation of general anaesthetic these drugs act very rapidly.
2.7 Nasal Route –
- The mucus memb. Of the nose can absorb the drugs very fastly
and bypass the liver and digestive juice.
Eg:- Nebulization, desmoprassin.

2.8 Parentral Route –


- Routes of administration other than the central (intestinal
route are k/a parentral routes).
- Here the drugs are directly delivered into tissue fluid or drug.
- A medicine or solution administered via route other than
ingestion by mouth.
- Drug action is more rapidly and predictable than oral
administration.
- These routes can be employed in an emergencies unconscious
or un-cooperative patients.
- Gastric irritants can be given parentrally and therefore to the
gastrointestinal tract can be avoided.
- It can be used in patients vomiting or those unable to
swallow.
- Digestion by the gastric and intestinal juice and the first pass
metabolism are avoided.

*Disadvantages of Parentral Route →


- Asepsis may be maintained
- Injections may be painful.
- More expensive, less safe and inconvenient.
- Injury to nerve and other tissues may occur.
2.8.1 Sub cutaneous Route – Infection beneath the skin into
sub-cutaneous tissue.
Eg:- Insulin
- As this tissue is have rich nerve supply (irritant drugs can’t be
injected) but less vascular supply (Absorption slower than
intramuscular that’s why the drugs have long acting action).
- It is reliable and patients can be trained for self-
administration.
- This route is avoided in stock patient because vasoconstriction
or delayed absorption.
- Max. amount of solution is 1 ml sol. Can be administered by
this route.
2.8.2 Intramuscular Route – The drug is injected in the large
skeletal muscle such as deltoid, triceps, gluteus or rectus
femories.
- Mucus have less nerve supply and much blood supply so, drug
absorbed very fast.
- Aqueous solution, oily solution can be injected by this route.
- Self-injection slightly impossible because required deep
penetration.

* IM infection contraindicated inpatient on anticoagulant


therapy because it produced local hematoma.
→ No more than 4 ml should be injected at one time into an
adult under developed musculature.
→ Angle used in intramuscular infection is 90 .
→ Common size for IM infection –
→ Ventro site – Site mainly used in adult.
- Use gluties medius and minimus muscle in buttocks for
injection.
- Give infection into a triangle area (V-shaped) formed by
placing of index finger on the anterior superior iliac spine and
middle finger on iliac rest of hip.
→ Vastus laterals site – To avoid injury (because poor
development of gluteal muscles) intramuscular infection into
new born, infant and toddlers should be administered in the
middle third of the vastus lateralis muscle.
- Use quadriceps femoris muscle (a large muscle on the anterior
surface of the thigh composed 4 muscles of the rectus femories,
vastus lateralis, vastus medialis and vastus intermedius muscles)
on antrelateral aspect of thigh.
- Divide thigh into 3 parts in horizontal & vertical plan then give
infection into outer middle part.

*Dorso-gluteal site – Divide Buttocks into 4 quadrant by


drawing an imaginary line between posterior – superior iliac
spine and greater trochanter of femur, than use upper quadrant
for injection.

→ Mid-deltoid site:– Injection into large triangular muscle


(deltoid) that covers the shoulder joints.
- Oftenly used for vaccination purpose.
- This route not be used for irrigating drugs.
- Give up to 1ml of solution only.
- Use lateral and upper aspect of upper arm.

2.8.3 Intravenous route –


- The drug administered in a bolus form or infused.
- Infused slowly over a time in the vein.
- The infection into a vein or more commonly into an
intravenous catheter to administration drugs.
- Drugs reach immediately and act fastly.
- It has 100% Bioavailability.

2.8.4 Intradermal Route –


- Injection into the skin just below epidermis used in giving
vaccines (BCG) when a local reaction is desired.
- Longest absorption time among all other parentral routes.
- Also used in ant sensitivity test and tuberculin skin test you TB
because in this route body reaction can easily observed.
- Common sites are inner surface form, below the scapula,
upper aspect of anterior and posterior chest.
- Capacity → 1 ml (for tuberculin syringe)
- Use oat anger of 5 to 15 .
- Use volume less than 0.5 ml.

*Inunction (Topical applic) → An ointment or medicated


substance rubbed onto the skin to produce a local or general
systemic effect like ointment.

*Instillation→ Slowly pouring or dropping a liquid into a cavity


or onto a surface (ear & eye) eg:- Eye drop, Ear drop or Nasal
drop.
*Irrigation→ The cleaning of a conal or cavity by flushing
water or other fluids or the washing of a wound such as colonic
irrigation.
*Skin application – Application of drug through transdermal
patches.
Eg:- Isosobuic dinitrate and pain killer containing opoids.
*Insertion – The Placement or implanting of a drug into body
orifices or cavities like suppositories in rectum & vagina.

*Insufflation – The act of blowing a gas vapour or powder into a


cavity or wound by insufflator. (a device for blowing powder or
a gas into a cavity).

*Implantation – Placing of drug in solid form into body tissues.

#PHARMACOKINETICS→
→ Pharmacokinetic is the study of the absorption distribution,
metabolism & excretion of drugs that is the movement of the
drug into, in and out of the body. For a drug to produce its
specific response.
→ It should be present in adequate concentration at the site of
action.
→ This depends on various factors about from the dose.
→ Once the drug is administered, it is absorbed that’s enters in
the blood and distributed to different parts of the body, reaches
the site of action, is metabolized and excreted outside the body.
→ Intensity of drugs effect depends on concentration of drugs
at the site of action and concentration of drug depends on
pharmacokinetics properties of drug.
→ So, pharmacokinetic Properties determines intensity of drug
action. They are as follows –
1. Dosage.
2. Route of drug administration
3. Onset of Action.
4. Time you Peak action.
5. Duration of Action.
6. Frequency of drug administration.

Absorption Distribution Metabolism Excretion.

Various Pharmacokinetic Process involve transfer of drug across


of biological membrane.
*Biological Membrane – It is a thicker bilayer of phospholipid c
comprises hydrophilic head and hydrophobic tail in
phospholipid bilayer.
→ Because of this cell membrane do not permit nater soluble
substances for transport across biological membrane easily
(limited transport) the transfer only by pores (Particle size less
from pore size).
→ On other hand lipid soluble substances can easily cross to
biological membrane.

*Transportation of substance across Biological Membrane→


1. Passive transport – The kind of transport do not require
energy. This is simple downhill process in c the molecules are
transverse from high concentration to low concern.
(i) Filtration Process – It is a simplest process for transfer of
substance across biological membrane.
In this method substances simply filter through biological
membrane.
Filtration is the passage of drugs through across pores in the
memb.
→ Water soluble drugs cross the biological memb. By filtration if
their molecule size is smaller than diameter of aqueous pores.
Diffusion of the drugs cross the capillaries depend on the blood
flow rather than lipid solubility or PH of medium.
(ii) Passive diffusion – It is downhill process in c substances cross
the biological membrane from high to low concentration is not
equal to both side of biological membrane.
The drugs diffuse across the membrane in its direction of
concentration memb. Playing no active role in this process.
The more lipid soluble drugs attain higher concentration. In
the membrane and diffuse quickly also greater the difference in
the concentration on 2 sides of membrane faster its diffusion.

2. Active Transport→
It requires energy and transport the solute against its
electrochemical gradient. (low concentration to high)
The carrier bind the drug and when transporting the drug
from low concen. To high concn. ATP change into ADP.
(i) Facilitate diffusion – The carrier find drug and diffuse its
concn. Gradient from low ot high concn. (uphill process)
Eg:- AT Pase Pump.

(ii) Carrier Mediated diffusion → This kind of transport require


a carrier for transportation of substance across the biological
membrane.
Eg:- Absorption of Vit-B12 by the help of Pernicious factor.
(iii) Bulk Transport →
The movement of macromolecules such as proteins or
polysaccharides into or out of the all is called bulk transport.
It is further 2 types –
Endocytosis Exocytosis
(Inside) (Outside)

Phagocytosis Pinocytosis
(solid liquid
self eating) (self drinking)

By this process liquid transport take place across the biological


membrane through the formation of vesicles.

#ABSORPTION→
→ Absorption is the movement of drug from site of
administration to systemic circulation.
→ Absorption require transportation of drug from site of
administration into the systemic circulation for a drug to reach
its site of action, it must pass through various membranes
depending on the route of administration.
→ Absorption occurs by one of the process described above.
→ That is passive diffusion or active transport.
→ Thus, except for intravenous route absorption is important
for all other route of administration.
→ This Phenomenon require transportation of drugs across the
biological membrane.
→ It is the first most stage of Pharmacokinetic that determines
how much fraction of drug that reaches into the systemic
circulation.
→ So, it is very important stage to determine drugs effect
because drugs effect are depend on concn. Of drug at the site of
action. And concn. Of drug is depend on fraction of drug that
absorb.
→ Not only the fraction of drug is important but also rate of
absorption of drug is important to determine drugs effect.

*Factors affecting absorption→


1. Particle size – lesser the particle size higher the absorption.
(Because cross the pores).
2. Area of Absorbing surface – Intestine higher surface area
higher the absorption.
Stomach lesser surface area lesser absorption.
3. Water solubility – Higher the solubility, higher the absorption.
4. Lipid solubility – lipid soluble drugs are absorbed faster and
better by dissolving in the phospholipid of the cell membrane.
5. Formulation – Pharmaceutical preparations are formulated to
produce desired absorption. Adding the pharmaceutical
substance then delay the drug absorption.
Eg:- Tetracycline metal ion that delay the absorption of drug.
6. Disintegration – Drugs taken orally should break up into
individual particles (disintegrate) to be absorbed. It then has to
dissolve in the gastrointestinal fluids.
In case of drugs molecules have to dissolve in the tissue fluids.
Delay in disintegration and dissolution result in delayed
absorption.
7. Concentration – Passive diffusion depend on concentration
gradient, drugs given as concentrated solution is absorbed fast.
8. Vascularity of Absorbing surface – Blood circulate remove the
drug from the site of absorption and maintain the concn.
Gradient across the membrane, se the blood flow se the rate
of absorption.
9. Route of administration – Each route have its overspecialty,
these affect the drug absorption.
Rate and extend of drug absorption depend on route of drug
administration.
IV > IM > SC > oral > Topical
10. Presence of food – Food may delay the absorption of some
drugs then they given empty stomach.
Eg:- Rifampicin, levodopa, Roxitromycin, Ampicillin
Food may interact some drugs and delay their absorption.
Eg:- Tetracycline chelate not even milk because present of
calcium se the bioavailability.
11. PH and Ionization – Ionized drugs are overly absorbed while
uninoised drugs are lipid soluble and are well absorbed.
Most drugs are weak electrolytes and ionized acc. to PH.
→ The acidic drugs are unionized in acidic medium of stomach
and rapidly absorbed.
Eg:- Aspirin and Barbiturates.
→ The alkaline drugs are unionized at the alkaline medium and
the rapidly absorbed.
Eg:- Pathidin
12. Metabolism → Some drugs are breakdown in the gut.
Eg:- Nitroglycerine & Insulin are given by alternative routes.
13. Disease → Disease of the gut like malabsorption and
achlorhydria result in reduced absorption of the drugs.
#DISTRIBUTION →
→ After the drug reaches into the systemic circulation it gets
distributed to various compartment to the tissue.
→ The drugs distributed always from high concentration to low
concentration of its concentration gradient.
→ When a drug reaches to in a systemic circulation it have
tendency of distribution.
→ Drug that entered into systemic circulation it get distributed
to those tissues that not having concentration gradient of drug
equal to drug available to in plasma.
→ By the systemic circulation drug is available for distributed
throughout whole body.
→ Distribution also cross the several barrier like filtration,
diffusion and specialized transport.
→ The factor c determine rate and extend of distribution are
lipid solubility, ionization blood flow & binding to plasma
proteins.
* Unionized lipid soluble drugs are widely distributed
throughout the body.
*Factors affecting drug distribution →
1. Nature of drug.
2. Partition coefficient (lipophilibility) – it is a property c
accounts for any drugs lipids solubility. If a drug or chemical
added to a system of 2 immiscible liquid, then that chemical or
drug aril tend to distribute itself. b/w those 2 immiscible liquid
until eqbm, this property is c/a drugs Partition coefficient.
3. Plasma Protein Binding and tissue storage.
4. Barriers – Blood Brain Barrier
- Placental Barrier.
Blood Brain Barrier –
- Penetration into CSP of Brain and spinal cord.
- The capillary endothelial cells in Brain have tight vascular
junction so, lack of large intracellular pores.
* So only high lipid soluble drugs cross the blood brain barrier.
Ex. Thiopental sodium.

* Placental Barrier (Passage across Placenta) –


Lipid soluble unionized drugs rapidly cross the placenta while
lipid insoluble drugs corss to a much lesser extent.
Thus, drugs taken by the mother can cause several
unwanted effects in the fetus.
Eg:- Drug chloramphenicol causes greyish colour of skin in child.
The sedative Thalidomide taken during early pregnancy for
relieve from morning sickness resulted in of babies being born
with Phocomelia.
5. Apparent volume of distribution (V.D) – The volume of
distribution is the volume of fluid into c a drug would need to
be distributed to achieve a concentration equal to the
concentration ultimately measured in plasma.
Volume of fluid in which drug dissolve throughout the
body.
V.D →
For Eg:- Drug administered IV is 500 mg Plasma concentration is
1mg/10ml then what is the V.D
V.D = → 5000
→ Dose administered is 500 ml, Plasma concentration is
1mg/5ml, what is V.D
V.D = → 2500
Hence we understand lesser the concentration higher the
distribution and higher the concentration lesser the
distribution.
Higher VD volume denotes lesser plasma concentration and
higher volume of drug distribution.
Higher V.D volume usually show by lyophilic drugs because of
higher distribution cross blood brain barrier and placental
barrier.

6. Redistribution – Lipid soluble drugs are initially distributed to


organ c have greater blood supply such as heart, kidney and
brain.
- Fat tissue takes time to supply drug.
- Greater the lipid solubility, faster the drug redistribution.
- Drug that are highly lipid soluble if they are given through IV
route.
- They have tendency to distribution first in those tissue or
organs that are highly profused (Brain and liver) due to this
concentration of drug at those tissues initially higher, then later
drug going to redistribution from these tissue to other lesser
profused tissue. This phenomenon is called as redistribution.
→ Due to this, concentration of drug se from site of action
(Redistribution) and that is responsible for shorter duration of
action.
Eg:- Thiopental sodium.
7. Plasma Protein Binding – Binding of the drug Plasma protein
is c/a Plasma Protein Biding.
Protein bound fraction of drug is Pharmacokineticaly and
Pharmacodynamically inert because it retain in vascular
compartment.
Do not distribute, metabolized and excrete and also not
showing any effect not resist to site of drug.
On Reaching the circulation most drugs bind to plasma Protein,
acidic drugs find mainly albumin and basic drugs bind -
acid glycoprotein.
The free or unbound fraction of drug is the only form available
for action, metabolism and excretion.
Acidic Basic
- Bind albumin - Bind - glycoprotein
Eg. Barbiturates Eg. Lignocrine
(Thiopenton sodium) - Prazocin
- NSAIDS (Asprin’s ) - Atenolol
- Banzodiazepines - Quinidine
(Dizepam)
Bind to albumin is quantively more imp. In compare to –
glycoprotein
Tissue storage –
Drugs may also accumulate in specific organ by active transport
(Need of energy) or get bound to specific tissue constituent.
Eg. Tissue/organ Drug
Skeletal Muscle, Heart → Digoxin
Liver → Chlorquine
Kidney → Chloroquine
Thyroid → Iodine
Brain → Chlorpromazin
CP-Z, Isoniozide)
Adipose tissue → Thiopenton sodium & Ether
Bone & teeth → Tetracycline & Heavy metals

#Bioavailability→
- It refers to the rate and extend of absorption of a drug from
dosage form.
- It is the fraction of the drug that reaches the systemic
circulation following administration by any route thus for a drug
given intravenously, the bioavailability is 100%.
- That is determined concentration time curve of plasma urine.
- It is measure of the fraction of administered dose of a drug
that is reaches to the systemic circulation in the unchanged
form.

#METABOLISM OR BIOTRANSFORMATON→
→ It is the process of biochemical alteration of the drug in the
body.
→ Body treats most drugs as foreign substances and tries to
inactive and eliminate them by various biochemical reactions.
→ It is needed to change the non-Polar (lipid soluble) compound
to Polar (water soluble) so, that they are not reabsorbed in the
renal tubules and are excreted throughout the body.
→ The most important organ of biotransformation in the liver,
but drugs are also metabolized by the kidney, gut mucosa,
lungs, blood and skin.
→ Biotransformation basically means for conversion of drugs
into such metabolites that can be easily excreted. (lipid soluble
to water soluble)
→ But Biotransformation of drug may also lead to the following
Inactivation – It is the ability in c the biotransformation play
major role in inactivation of the active drugs, active metabolite
and then make less active of drug metabolite.
→ Many drugs and there active metabolites are random inactive
or less active after metabolism.
Eg:- Ibuprofen, PCM (Paracetamol), ledocacine and propranolol
*Active metabolite from an active drug – Active metabolite
from an active drug by the help of metabolism more than one
active drug metabolites are formed.

Active drug Active metabolite


Digitoxine → Digoxin
Phenecetine → PCM
Morphine → Codine
Imipramine → Desinipramine

*Activation of Inactive drug –


Some drugs are inactive at the time of administration and then
they are active in the body.
- Few drugs are inactive so these drugs require conversion in
the body into one more active metabolites.
- These drugs are also called as Pro-drugs
*Pro–drug – It is an inactive drug c gets converted into an active
form in the body. Inactive form of drugs that is active after
metabolism inside the body is c/a pro-drug.
Inactive drug (Pro-drug) active metabolite
Lerodopa Dopamine
Prednisone Prednisolone
Acydonik A cyclonic Prihasphate
Digitoxine Digoxin

All these changes are being made on the basis of chemical


alteration by the help of various enzymes chemical reactions.
So bio transformation basically depends on chemical reaction.
These chemical reactions are basically divided into 2 categories-
* Phase – I * Phase – II reaction

*Phase – I Reaction/Non synthetic reaction/Functionalization


Reaction→
→ A functional group is generated or exposed may be
metabolites active or inactive.
→ Non-synthetic reaction convert the drugs to more Polar
metabolites by oxidation, reduction, hydrolysis cyclisation and
decyclization.
→ Oxidation is the most important reaction catalyzed by mono-
oxigenase enzyme present in the liver
→ If water soluble not become the metabolite at 1st Phase then
it go to Phase – II reaction after forming active metabolite they
do function and then excreted.
(a) Oxidation – Addition of oxygen molecule this reaction
involve addition of vely charged radical a removal of the
hydrogen, positively charged radical oxidation is the most
important drug metabolizing reactions.
Eg:- Phenytoin, Propranolol and Pnenobarbitones.
(b) Reduction – This reaction is the opposite to oxidation and
involve P450 enzymes.
Work in the opposite direction or in the removal of oxygen
molecule or negatively charged molecules.
Eg: Cortizone is converted to hydrocortisone.
(c) Hydrolysis –
This is the cleavage of drug by taking up of a molecule of O.
Eg:- Acetylcholine + O → choline + Acetic acid
(d) Cyclization –
This is the forming of a ring structure from a straight chain
compound.
Eg:- Progranil (anti-malarial drug)
(e) De-cyclization –
This is the opening of a ring structure from a cyclic drug
molecule.
Eg- Phenytoine
*Note – If the metabolites of Phase – I is not sufficiently polar to
eliminate it goes to Phase-II.

*Phase-II Reaction/Synthetic Reaction/Conjugation Reaction →


In Phase – II reaction water soluble drugs or substances present
in the body like glucouronic acid, sulphoric acid, glutaiotion or
an amino acid combined the drug (or its Phase-I metabolites)
to form a highly Polar compound c is inactive and gets easily
excreted by the body through kidney and large molecule
excreted by bile.
After Phase – II reaction metabolites mostly in active it can be
happened after Phase-I reaction if metabolites are active or it
can be happened directly.
→ Phase – II reaction include following reactions –
(1) Glucohonic conjugation – The compound hydroxine or
carboxylic acid group easily conjugate glucoronic acid c is
derived from glucose.
Eg: PCM, Asprin, Digopam, lorozapm, morphine, onetronidzole
and zidovudine.
(2) Acetylation – Compound having amino are hydrazine group
are conjugated help of acetyl co-enzyme
Eg:- Sulphonamide, isomiazoids, Depsome (It is the combination
of clefazimine i.e., used for treatment of leprosy).
(3) Methylation – The addition of methyl group amines or
phenols can be methylated by methyltransferase enzyme.
Eg:- Adrenitine and Nicotinic acid.
(4) Sulphate conjugation – Addition of the sulfate group. The
Phenolic compound and steroid are sulphated by sulpho-
transferase enzyme.
Eg:- chloramphenol, methyldopa and sex-steroid.
(5) Glycine conjugation – Addition glycine group the drug,
salicylates, nicotinic acid and other drugs having carboxylic acid
group are conjugated glycin.
(6) Glutathione conjugation – This is carried out by GST enzyme
forming mercoptoporine.
Eg: PCM.
(7) Ribo nucleotide or Nucleotide conjugation – This pathway is
important for the pathway of Purine, and anti-metabolite used
in cancer chemotherapy.
→ Many drugs metabolise by these reactions.
→ All the Phase – I and Phase – II reactions required enzymes
for drug metabolism.
→ These drugs metabolizing enzyme, divided into 2 categories.
* Microsomal
* Non-microsomal
(1) Microsomal enzyme – These are located in smooth ER.
Eg:- cytochrome, P450 reductase and these are +nt is liver
microsome.
(2) Non-Microsomal enzyme – These are +nt in the cytoplasm,
Mitochondria, hepatic cell and also in other tissues like Plasma.
Eg: Acetyl transferase.

#First Pass Metabolism →


→ This referred to metabolism of drug during its passes from
site of absorption to site of systemic circulation.
→ This is happen only by intestinal wall and liver.
→ When drug is absorbed through GIT (Stomach and intestine)
it reaches to liver by Portal vein (1st Pass metabolism).
→ Where it got metabolise via liver and intestinal wall.
→ Then distributed via systemic circulation.
(*It means metabolism before distribution).
→ Normally drugs distributed and the same time it reaches to
liver and get start to metabolism.

#Excretion→
→ It is the passes of the drug c is systematically absorbed.
→ Drugs are excreted from the body after being converted to
water soluble metabolites while some drugs are directly
eliminated out metabolism.
→ The drugs their metabolites excreted mainly by kidney,
intestine binary system, lungs, drugs are also excreted in a small
amount of saliva, sweat & milk.
→ The drugs and their metabolites are excreted by the following
route.
(1) Through kidney (urine)/Renal excretion –
It is the most important channel of excretion for majority of
drugs is that renal excretion.
* The unabsorbed interaction or parts of drug are excreted from
the kidney.
* Kidney are the most important organ for the drug excretion.
* The 3 Processes involved in the elimination of drugs through
kidneys are –
*Glomerular filtration
*Active tubular secretion
*Passive tubular re-absorption.

*Passive Tubular Reabsorption – Highly lipid soluble drugs are


largely reabsorbed in the renal tubules and therefore excretion
is slow.
- Acidic drugs get ionized in alkaline urine and are easily
excreted while basis are excreted faster in acidic.
- This property is useful in the treatment poising.

2. Through feces –
A part from the unabsorbed function of drug, most of the drug
present in feces that is derived from the bile (Unabsorbed drug
directly excrete by feces) Billiary excretion is mostly through
feces like steroid drugs.

3. Through lungs/exhaled drugs or air –


→ Gases, volatile liquids, fumes, general anesthetics ana alcohol
are eliminated by lungs.
Eg: O
4. Saliva and sweat – Some drugs are also excreted by saliva and
sweat.
Eg:- Metronidazole Phentoid are excreted by saliva.
Potassium iodied, lithium and metallic ions are excreted by
sweat.
5. Milk – The excretion of the drug in milk is in small amount &
is no significant to the mother But it may lethal or toxic for
sucking infant contraindicated to the mother.
Eg:- B Blockners, Ami darone (VT), Phenobarbito, Theophyline
(Bronchlodialator) and anti cancer drugs.
*Plasma T ½ or Half life → The Plasma ½ life of a drug is the
time, taken by a drug to remain in ½ concentration. In plasma to
its original value.

*Prolongation of drug action – Drug action can be prolonged by


sing duration of action that is done by –
(i) By prolong of absorption eg:- Insulin via S.C route
(ii) By sing plasma Protein Binding.
(iii) By retarding rate of Metabolism.
(iv) By Retarding Renal excretion.

Note:- By all these methods can be increase duration of action


that is helpful to reduce frequency of administration or to show
over effects.

#Pharmacodynamics →
→ It is the study of drug effect (Power).
→ It is the study of action of drugs on the body and their
mechanism of action that is to know what drugs do and how
they do it.
→ What the drug does to the body this include Physiological
and biochemical effects of drugs and their mechanism of action
at organ or system.
→ It is an attempt to clarify the complete effect sequence and
the dose effect relationship and the modification of action of
one drug by another drug is also a part of Pharmacodynamic.
→ Drug produce their effect by interacting the physiological
system of the organism. By such interaction drugs can only
modify the rate of function of the various system.
→ Drugs may se or decrease the secretions but they can’t
change the basic functions of any physiological system.

* HOW THE DRUG ACT ON HUMAN BODY →


→ Drugs act on human body by various principles and
mechanism by drug action.

*Principles of drug action –


1. Stimulation → It refers to selective enhancement of the level
of the activity of specialized calls.
→ Drugs do not impact new function to any system they only
after the pace of going activity.
These basic types of drugs action can be classified as
stimulation.
Eg: Adrenaline stimulate cardiac response.
2. Depression – It is the selective diminution of activity of
specialized cells.
Eg:- Quinidine depress the heart, Barbiturates depress CNS.

3. Irritation – This can occur an all types of cells of the body and
may result in inflammation necrosis of the cell.
Mild Irritation may stimulate associated function.
Eg:- Bitter may se salivary and gastric acid secretions.

4. Replacement – Drugs may be used for replacement when


there is deficiency of Natural substances, metabolites, humans
& nutrients in the body.
Eg:- Insulin in DM Iron in anemia & Vit – C in scurvy.

5. Cytotoxic or Ant infective action – Drugs may act by specially


destroying the infective organism and it kills the invading
parasites or destroy the cancer cell without significantly affect
the host cells.
Eg: Cyclophosphamide (Anti-cancer drug)
Chloroquine (Anti-malarial drug)

6. Modification of Immune system – vaccine and sera act by


improving over immunity while immunosuppressant act by
depressing Immunity.
Eg:- Glucocorticoids.

*Mechanism of Drug action → Barring a handful of drug whose


action can be explained on the basis of their simple physical or
chemical properties but majority of drug action in complex
manner and elements of c are sheldom not known.
1. Physical Property – Physical property of drug responsible for
its activity. The drugs may have physical & chemical Property &
they act acc. To their mechanism of action.
Drugs acting by their Physical Property are –
*Osmotic Property – It is like osmotic diuretics such as
Mannitol, osmotic Purgatives likes magnesium sulphate.
* mass of drug – Bulk laxative (Isaphgalla)
* Radioactivity – is a chemical but property is physical (kill
cancer cells)
* Radio capacity – Barrium sulphate contrast media.

2. Chemical action – Chemical action of drug responsible for its


action drugs react extra cellular on the basis of simple chemical
equation or reaction.
Eg: Antacid neutralized gastric acid.
3. By enzymes – All Biological Reaction are carried by under
catalytic influence of enzyme.
→ Enzymes are very important target of drug action.
→ Drug can either se or se enzymatically mediated reaction.
→ In Physiological system enzyme activities are apparent se in
enzyme activity can also occur enzyme induction.

3.1 Enzyme Induction or Stimulation – The enzyme induction


are the process where by drugs act as sing the activity of
enzyme than drug do own act fastly.
3.2 Enzyme inhibition – Inhibition of enzyme is a common
mode of drug action. It can be specific or non-specific.

3.2.1 Non specific Inhibition – Many chemicals and drugs are


capable of denaturating Protein. This they could after the str.
Any enzyme and inhibit in its activity.
Eg:- Heavy metals such as cl, fe, strong acid, strong Base &
Phenol inhibits enzyme non specifically.

3.2.2 Specific Inhibition – Many drugs inhibit particular


enzymes without affecting others it is of 2 types –
(i) Competitive Inbibition ( types) → The drugs being
structural similar competes the normal substrate (drug) for
catalyting binding sites of the enzymes so that product is not
formed or a non functional product is formed.
→ High concentration of drug are required for its maximum
reaction attained.

Enzyme Endogenous substrate Competitive Inhibitor


Ace Angiotensinogen I Captopril
ALE inhibitor BP
Inhibitor Acetylcholine Neastrigorine

(ii) Non-competitive Inhibitor → Inhibitor reacts an adjacent


site and not catalytic site but after the enzyme in such a way
that it loss its catalytic property.
Non competitive Enzyme
Inhibitor
Aceta Zola mine carbonic anhydrase
Aspirin Cyclo-oxygenase
Lovastatin HMG Co-enzyme

4. Through the Ion channels→


Drugs may interfere the movement of ions across specific
channels.
Eg:-
→ Equilibiline blocks myocardial sodium channel.
→ Aminoderone blocks potassium channel of myocardium.
→ Nifidifine blocks calcium channel.

5. Altering Metabolic Process →


Drugs like antimicrobial alter the metabolism pathway in the
microbes resulting in destruction of the M.O. Eg:- Sulphonamide
intergose bacterial folic aicd synthesis.

6. Through Receptors –
A large amount of drug add through specific macromolecule of
a component of cell, c regulates critical function like enzyme
activity, permeability gene excretion and structural features.
- A receptor is a site on the c an genised bind to bring about a
change.
- Receptors are protech, they may be +nt in the cytoplasm or on
the nucleus.

*Functions of receptors –
The receptor has to identify the compound and when the
compound bind to the receptor. It has to convey the message to
bring about a response.

*Mechanism →
(1) Agonised – An agonist substance that bind to the receptor &
produce a response.
(2) Inverse agonist – An agent c activates a receptor to produce
an effect in the opposite direction to that of the agonist.
(3) Antagonist – An agent c prevent the action of an agonist on
a receptor or the subsequent response but does not have any
effects on its own.
(4) Partial Agonist – An agent c activates the receptor to
produce sub maximum effect but antagonist the action of full
agonist.
Partial agonist binds to the receptor but has slow intrinsic
activity that is to produces partial response.
(5) Ligand – (latin word – liger means to bind)
Any molecule c attach selectively to particular receptor or sites
the term only inhibits ability a affinity to bind out regard to
functional changes.
The sub type of receptors are –
1) G-Protein coupled Receptor – There are large family
receptors c are linked to the effector (enzymes, channels and
barrier) through one or more GTP (Guanosin –tri-phophate)
- GTP activated protein for response stimulation.
- All such receptor have common pattern of structural
organization.
- The sub unit of G protein are , B and R.
- A number of G Protein differentiated by their - sub units.
- The important once their action the effector are –
- GS Adenylyl cycles activation of channel opening.
- GI Adenylyl cycles inhibition of channel opening.
- Go channel inhibition.
- Gq phospholipase activators.

2) Ion channel receptors – These are all surface receptors also


called ligand gated Ion channel endose ion selective channels
( , ) within their molecules.
Agonist binding open the channels and causes depolarization
and hyperpolarization changes in cytosolic ionic composition,
depending on the ion that flow through it.
The Nicotinic, colligernic and glycin (Inhibitory amino acid)
Excitatory amino acids (glutamide) and serotonin receptors are
in this category.

3) Channel Regulation – The activated G Proteins (Gs, GI, GO)


can also open or inhibit ionic channels specific for calcium and
potassium out the intervention on any 2nd messenger like (A
MP-Adenosine Monophosphate) and bring about
hyperpolarization & depolarization change into the intracellular
calcium.
The Gs open channel in myocardial and skeletal muscle
while GI and GO open potassium channel in the heart and
smooth muscles as well as inhibit neuronal calcium channel.

Trans membrane Enzyme linked receptor →


On enzyme linked receptor also k/a catalytic receptor is a
transmemb. receptor , where the binding of an extracellular
ligand causes enzymatic activity on the intracellular site. Hence,
a catalytic receptor is an integrated membrane protein
containing both enzymatic catalytic and receptor function.
They have 2 important domains, an extracellular ligand binding
domain and an extracellular domain c has a catalytic function
and a trans membrane helix.
The signaling molecule bind to the receptor on the outside of
the cell and causes a conformational changes on the catalytic
function located on the receptor inside the cell.
Eg:- Serine specific protein kinase as in bone morphogenetic
protein .
Receptor Regulating gene expression →
Regulation of gene expression includes a wide range of
mechanism that are used by cells to se or se the production
of specific gene products (Protein or RNA) and is informally
turned gene regulation.
→ The step of gene expression can be moderate from
transcriptional inhibition, RNA Processing and post translation
modification of a protein often 1 gene regulator controls
another so, on in a gene regulatory network gene regulation is
essential for virus prokaryotes, Eukaryotes as it versatility and
adaptability of an organism.

Dose Response Relationship →


The response to the sing dose of the drug can be plotted on a
graph, initially the extent of response se sing dose till the
max. response is reached.
After the max. effect has be obtained further se in dose does
not se the response.

Drug Potency and maximal efficacy→


The amount of drug required to produce a response indicates
the potency of drug.
Eg:- 10 mg of morphine is equal in effect o more potent to 100
mg of pathiedine it means morphine 10 times potent from
pathiedine.
→ Lesser the dose for certain responses denotes higher
potency.
→ Higher the dose for certain response denotes lesser potency.

Efficacy→
It indicates the maximum response that can be produced by a
drug.
It refers to the maximum response that can be illicit ate by drug.
Efficacy A B C
Higher the maximum response, higher the efficacy and lesser
the max, response, lesser the efficacy.
Eg:- Morphine produces such degree of Analgesia that can’t be
obtained from any dose of aspirin so, morphine more efficacy
from aspirin.

*Therapeutic Index →
Drugs of low therapeutic index have low safety margin.
Eg:- Digoxine and lithium.
Therapeutic index indicates the safety margin of the drug.
It is the index c denotes therapeutic range (therapeutic window)
of drug.
→ It is the ratio of LD50 and ED50. It denotes safety profile dose
range and therapeutic liability of a drug.
→ Higher the therapeutic index, greater the therapeutic range
so, safety margin in dose range (lesser liability).
→ Lesser the therapeutic index, lesser therapeutic and poor
safety margin and dose range (higher liability)

# 50 (lethal dose) → It is the dose of drug on c 50% subjects


are died.
# 50 (effective dose) → It is the dose of a drug on c 50%
subjects shows their therapeutic effect.
Therapeutic Index =
Eg:- If a drug is having 500 mg and is 100 mg than
that therapeutic index is 5 mg
500/100 = 5mg
This value (therapeutic index) denotes how much differents
(time b/w and )

#Combined effect of drugs/Drugs synergism & Antagonism→


When 2 or more drugs are given concurrently the effect may be
additive may be synergic or Antagonic.
*Synergism – When the action of 1 drug is enhanced or
facilitate by another drug then they are said to be synergistic
and this Phenomenon is called synergistic effect of drug.
→ Synergism can be 2 types –
- Additive sup additive (Potentiation effect)
- Additive effect → Combined effect of 2 drugs equals to
addition of alone effect of these drug.
The effect o 2 or more drugs get added up & the total
effect is equal to the sum of there individual action.
Effect of Drug A + Effect of Drug B → Effect of Drug AB
Eg:- Diclogenac sodium + Paracetamol act as analygesic or
antipyretic effect.

- Super additive effect – Combined effect of drug greater than


total of individual effect of drug.
Effect of Drug A + Effect of Drug B < Effect of Drug A + B
Eg:- Levodopa + Carbidopa having greater effect in combination
due to inhibition of Peripherol metabolism.
Sulphonamide + Trimethoprim having greater effect in
combination due to sequential block, Both alone are
bacteriostatic but in combination they have bactericidal effect.

*Antagonism→ One drug opposing or inhibiting the action of


another drug is antagonism when one drug ses or inhibit the
action of other drug this Phenomenon is called as Antagonism
and drugs are e/a Antagonist.
Effect of Drug A + Effect of Drug B > Effect of Drug A + B
*Based on the mechanism, antagonism can be in further types –
1. Physical antagonism
2. Chemical antagonism
3. Antagonism at the receptor level.
Reversible (competitive)
Irreversible
4. Non-competitive Antagonism

1. Physical antagonism – Based on Physical Property, charcoal


adsorb alkaloids.
2. Chemical Antagonism – Two substance interact chemically to
result in inactivation of the effect.
Eg:- Chelating agent inactivate heavy metals like lead & Mercury
to form inactive complexes.
Antacids like Aluminum Hydroxide Neutralize gastric acid.

*Physiological Antagonism – 2 drugs act at different sites to


produce opposing effects.
Eg:- Histamin acts on receptors to produce bronchospasm
and Hypotension.
Histamin and Adrenaline having opposite effect on Bronchi and
blood vessels.
Drug Bronchi Blood vessels
Histamin Constrict Dilate
Adrenaline Dilate Constrict

*Insulin and glucagon have opposite effects on the blood sugar


level.
4. Antagonism at the receptor level → The antagonize inhibits
the binding of the agonist to the receptor such antagonism may
be reversible or irreversible receptor antagonist interfere the
finding of agonist its receptor due to this antagonist prevent
generation of response through agonist.
4.1 Reversible Competitive Antagonist – The agonist and
antagonist compete for the same receptors by sing the
concentration of agonist & Antagonism can be replaced or
overcome so, it is reversible antagonism.
Eg:- Acetylcholine muscardinic receptor agonist Atropine
muscarinic receptor agonist.
Atropine Prevent or inhibit action of acetylcholine through
muscranine receptor antagonist.

Irreversible Antagonist → The antagonist binds to family by


molecular bond to the receptor that is dissociates very slow or
not at all. Thus, its blocks the action of the agonist and the
blockage cannot be overcome by singgg the dose of the
agonist and hence it is irreversible antagonist.
Eg:- Adrenaline and Phenoxybenzamine at - adrenergic
receptor.

Non-competitive Antagonist →
The antagonist blocks at the level of receptor effector linkage.
Eg:- Verapamil blocks the cardiac calcium channels and inhibits
the entry of ca. during depolarization.

#Drug Dosage →
→ Dose is an appropriate amount of drug that is required to
produce certain degree of response in a patient, these are
mainly of 4 types –
- Standard dose
- Regulated dose
- Target level dose
- Titred dose (calculated dose)
(i) Standard dose – For many drugs, dose is some for most pt. is
k/a standard dose of drug.
Eg:- BCG.
(ii) Regulated dose – The drug modify a finally regulated body
physiological function c can be easily measured, so that dose
can be accurately adjust by repeated measurement of affected
Physiological function.
Eg:- Anti-hypertensive, diver tics and anti-pyretics drugs.
(iii) Target level dose – In many condition, the response is not
easily measured but has been demonstrated to be obtained on
a certain range of drug concentration in plasma.
Eg:- Antiepileptic drug and antidepressant drugs.
(iv) Titrated dose – (calculated dose) – Dose needed to produce
maximal therapeutic effect. These cannot be used or given
because of intolerable adverse effect.
In such conditions optimum dose is calculate acceptable level
of adverse effect.
Eg:- Anticancer drugs
#Factors modifying drug action or factors affecting drug acton
or factors affecting effect of drug
→ A drug may have some pharmacological action in different pt.
but the intensity and duration of action is not same in different
pt. because of drug response may be affected by various factors
and these are as follows –
1. Age – The Pharmacokinetic of many drugs change with age
resulting in altered response in extremes of age.
→ Infant, children and older require different amount of dose in
compare to others. This is because of difference in body size
and metabolic enzyme system so, they require lesser amount of
dose.
Formula to calculate dose in children.
→ Young’s formula
Adult dose
* Note:- Use for below 12 year children.

→ Dillings Formula
Adult dose
* Note:- Use for Above 12 years of age.
Eg:- Adult dose of oflaxicin is 200 mg calculated dose for 8 year
of child is –
200 → → 80 mg

2. Body size and Body weight – It Influence the concentration


drug attained at the site of action, large body size require large
dose of drug.
→ Higher the body size, lesser the concentration.
→ Lesser the body size, higher the concentration.

*So to achieve therapeutic concentration


- Higher body size required higher dose.
- Lesser body size required lesser dose.
→ Higher the body size indicate higher body weight.
→ Lesser the body size indicate lesser body weight.
→ So, higher the body weight, higher the dose.
→ Lesser the body wt., lesser the dose.
Body size Body weight Dose
→ That’s why infants, children and older require lesser dose
(lesser body size) in compare to adults.
→ Patients higher body weight requires higher dose in
compare to lower body weight pt.
→ dark formula – Adult dose.
Adult dose.
3. Gender → male requires large dose as compare to female to
produce similar response it is due to mental makeup and body
size.

4. Races – There may be racial difference for drug response or


for drug action.
It may be due to different genetics and different life style.
5. Genetic factor – In affect the metabolism and excretion of
drug. This is mainly due to difference in enzymes activity.
Eg:- Inability to metabolizing phenytogine leading to toxicity at
usual dosage.
(due to deficiency of metabolitec enzymes).
6. Route of drug administration – Drug c have given through
oral route have delayed effect and require more dose as
compared to drug given through parenteral route.
→ Occasionally route of administration may modify the
Pharmacodynamics response –
Eg:- magnesium sulphate given orally is a purgative, but given IV
it causes CNS depression & has anti-convulsion effect
7. Health and illness – many drugs are metabolite in liver &
excreted through kidney so the disease of these organ or
system may affect the metabolism and excretion of drugs.

8. Effect of other drugs – When 2 or more drugs given


simultaneously they can modify each other response this is k/a
drug interaction.
Eg:- caroidopa + levodopa potentiate action of one another.

9. Psychological Factors – Patient believe, attitude and behavior


also affect the effect of drug.

10. Tolerance – Many drugs as repeated use develops tolerance


in our body, it means for same action dose of the drug should
be sed repetitive dose or use.
It not happens all drug, it occurs mostly drugs acting on CNS or
drugs that induce dependence.
Eg:- Tolerance develops to sedative action of chlorpromazine
but not its anti psychotic action.
* Prolonged administration of drugs like acting on CNS opioids,
Narcotics required sing dose for producing some action or
effect it is because of tolerance effect.

11. Accumulation – Many drugs accumulate inside the body on


repetitive use and can should cumulative toxicity.
Eg:- Digoxin & lithium.

12. Tachyphylaxis – It is the rapid development of tolerance


when some drugs are administered repeatedly at shout
intervals, tolerance develops rapidly and is k/a Tachyphylaxis or
acute tolerance.
Eg:- Ephedrine – In this of tolerance. Tolerance is developed
very fast because of drug is given in quick section of time and
after sometime drug show no response even on higher dose but
if drug is stopped for some time it show again similar response.

13. Placebo – It is a treatment insert substance that is similar


to colour, shape and size from a drug.
It altered Psychological state, change in Psychological effect
may produce effect.
Eg:- Distilled water injection.

Adverse effects of drugs –


→ Adverse effect is any undesirable and unintended
consequences of drug administration.

→ Adverse drug effect is any lethal or noxious change c is


suspected to be due to a drug, requires treatment or decrease
in dose and indicates a caution in future of some drugs.
→ It is very important to know abou them for nurse because the
nurse is the first person who is reported the adverse effect and
a nurse to know about drug adverse reaction and there
possibilities she may be the first person to realize that
something is wrong pt.
→ Adverse effect are of 2 types –
- Types – A Reaction/Predictable Reaction – These are due
more pronounced Pharmacological action of drug.
- These are excessive and extra – pharmacological effect c are
depend upon does that can be easily predictable if they are
excessive. Can be caused by reducing the dose.
- This can be due to excessive absorption of drug or due to sed
excretion and metabolism of drug these reaction are usually
related to the dose drug that can be correct by giving lower
dosage.

-Type-B Reaction/Unpredictable Reaction – These are based on


individual genetic variation and not on drug own action.
These are not depend on the dose and that are not assume so,
drug should be stopped in the unpredictable type of drug
adverse reaction.
Eg:- Hypersensitivity, allergy, idiosyncrasy (any allergy tnt from
birth).
They are less common but more serious and often requires
withdrawal of drug.

*Side effects of drugs →


These are extra pharmacological effect that are because of
drug act more than 1 site.
→ These are unwanted but often unavoidable
pharmacodynamics effect that occur at the therapeutic dose
generally they are not more serious can predict by
pharmacological profile of the drug.
→ It means effects that are not required but comes as extra
pharmacological effect k/a side effect.
Eg:- Atropin used in pre-anaesthetic medicine for its
antisecretory action, the same action produced dryness of
mouth.

*Toxic effect of drug –


→ These are pronounced or excessive pharmacological reaction
effect of the drug that is because of prolonged use and
overdose of drug.
→ Overdose may result to poisoning.
Eg:-Morphine (Analgesic) may be causes respiratory failure in
over dose.
→ Overdose may be absolute (accidental or suicidal) and
relative usual dose of imipramine over dose causes cardiac
arrhythmia.

*Drug poising →
→ Poising is the harmful effect of chemical on a biological
system, it may from large dose of the drug because it is the
dose c distinguish a drug from a poision.
Eg:- Organ phosphorous poision, insecticides or industrial
chemicals.

*Intolerance →
→ When a pt. is more sensitive to the effect of drug then the
drug produce toxic effect even at therapeutic dose.
Eg:- 1gm chlorine may produce nausea, vomiting, abdominal
pain and diarrhea in some facets at the therapeutic dose.
*Idiosyncrasy →
→ It is genetically determined abnormal reactivity to the
chemical or a particular drug.
→ Certain adverse effect of some drugs are largely restricted
individual a particular genotype and these kind of effects are
due to individual genetic variation are k/a Idiosyncrasy.
→ Eg:- Chloramphenicol produce serious Aplastic anemia
(suppresses erythropoiesis)
- Aspirin induces Asthma.

*Drug allergy and hypersensitivity →


→ It is Immunological mediated reaction produces different
symptoms c are unrelated to Pharmacodynamic profile of the
drug.
→ The target organ Primary affecting in the drug allergy are
skin, airway, blood, blood vessels, GIT tract.
→ These reaction are similar to other allergic reaction.
Only difference is that it is the drug that act as an allergen.
→ The types of reaction are –
- Humoral →
Types – I – Anaphylatic Reaction
Types – II – Cytotoxic Reaction
Type – III – Retarded or arths reaction such as vasculitis.

- Cellular or cell mediated →


Type – IV – Delayed Hypersensitivity Rxn.
Eg: Drug causing allergic Rxn are –
- Penicillin
- Sulphonamide
- Tetracyclin
- Multivitamins

Mutagenicity →
→ Many drugs that can cause mutation are k/a as Mutagen the
characteristics of inducing mutagen is c/a mutagenicity.
Eg:- Anti-cancer drugs.

*Carcinogenicity →
→ Many drugs can induce carcinoma & this type of drug are k/a
carcinogen and the characteristics of them carcinoma is k/a
carcinogenicity.
Eg:- Tobacco, Smoking & Metromazole.

*Iatrogenic→ (Drug induced disease or physician induced


disease).
→ Many times a drug can induced a disease if it is not taken
property or for a proper time in a proper amount (dose and
frequency), this might be because of a doctor fault, pharmacist
fault, nurse fault because of them pt. taken.
→ Corticosteroids are used for the treatment of inflammation,
Asthma, Allergy can induce peptic ulcer on long term use, so
here if peptic ulcer arises they are called drug induced disease.
Unit - 03
Antiseptics, Disinfectants and Insecticides
INTRODUCTION
Disinfectant is an agent, which destroys the entire pathogenic
organisms except spores and the process is called disinfection. If
spores are also killed, it is called sterilization. A disinfectant is
used on inanimate objects.
Antiseptic is an agent that destroys microorganisms and
can be used on living tissues. The term germicide can be used
for either disinfectant or antiseptic. Germicides are widely used
in domestic products like soaps, toothpastes and aftershave
lotions.

ANTISEPTICS AND DISINFECTANTS


Mechanism of Action
Germicides may act by the following mechanisms:
• Oxidation of bacterial protoplasm
• Denaturation of bacterial proteins
• Detergent like action
• Competition with essential substrates for the important
enzymes in the bacterial cell.
An ideal germicide should have a wide antibacterial
spectrum, should be chemically stable, should have rapid
action, nonirritating to the tissues, not interfere with wound
healing activity even in presence of pus, exudates and tissue
degradation products; it should not be absorbed into systemic
circulation.

Classification
On the basis of chemical nature germicidal agents are classified
into
• Alcohols
• Aldehydes
• Surfactants
• Phenol derivatives
• Halogens
• Oxidizing agents
• Dyes
• Metals.
On the basis of level of disinfection, disinfectants and
antiseptics are classified into:
• High level disinfectants, e.g. glutaraldehyde.
• Intermediate level disinfectants, e.g. phenols, alcohols.
• Low level disinfectants, e.g. quaternary ammonium
compounds (bacillocid).

Classification Name Uses Action


Alcohols Ethyl alcohol Ethyl alcohol is used to clean It rapidly denature
the Ethyl alcohol skin before The bacterial proteins
injections and surgeries Isopropyl alcohol more
Isopropyl alcohol It is used in 68-72% potent and more
concentration as skin toxic Alcohols
antiseptic

Formaldehyde Used in fumigation of rooms Aldehydes act by


Glutaraldehyde It does not damage lenses alkylation of chemical
and groups in proteins and
Aldehydes cementing material in nucleic acids It is
endoscopes
bactericidal,
Used for sterilizing rubber,
plastic and metal appliances
sporicidal, fungicidal and
Two percent solution is used viricidal
for
local application in idiopathic
hyperhidrosis (increased
sweating) of palms and soles.
Surfactants (surfactants are Anionic surfactants, e.g. Effective for gram-positive Microorganism are enmeshed
chemicals that lower the soaps and acid Microorganisms are in the lather and washed
surface tension of solutions fast organisms away on rinsing
and are termed detergents)
Cationic surfactants, Active against gram-positive Cationic surfactants dis
e.g. benzalkonium and gram-negative organisms sociate into large cations
chloride cetrimide (less active against spores, Anionic surfactants
cetylpyridinium viruses and (soaps) neutralize their
chloride, dequali fungi)
action
nium chloride Most effective in neutral
solution Nonirritating and
safe
Benzalkonium 1:1,000 solution for cleansing It has an aromatic odor and is
chloride (zephiran) skin soluble in water
1:2000 for mucous and alcohol
membranes and
denuded skin 1:20,000 for
bladder
irrigation
It is also used for (1:1,000-
4,000) storing sterilized
surgical instruments
Cetrimide (cetavlon) 1% solution is used like The combination of chlo
Savlon is above. rhexidine with cetrimide
cetrimide It is also used as a is most popular antiseptic
3% + chlorhexidine cream. It is very
effective for cleaning wounds
Dequalinium chloride Is used in gum paints
and lozenges

Cetylpyridinium chloride Is used in mouthwashes and


chloride
lozenges

Classification Name Uses Action


Phenol Phenol is used to disinfect it is bactericidal and fun
urine, feces, gicidal, but poor against
sputum of patients and is spores and viruses
sometimes
used as antipruritic
because of its
local anesthetic action
Phenol derivatives Cresol is methylphenol It is used as a disinfectant It is toxic as phenol, but is
for utensils and excreta more active
Lysol Useful disinfectant for Lysol is cresol with soap
hospital and domestic use solution It has higher
antiseptic activity
Chloroxylenol (dettol) An antiseptic and It is effective against gram-
disinfectant positive and gram negative
organisms
Hexachlorophene It is used in soaps for This chlorinated phenol
surgical scrubbing, for acts by inhibiting bacterial
cleaning the skin in enzymes and causing lysis
obstetrics, carbuncles and
seborrheic dermatitis, used
as a deodorant
Chlorhexidine (hibitane): Effective against gram- It is rapid acting and non-
Savlon chlorhexidine + positive and gram negative irritating
cetrimide organisms and fungi
Iodine To clean skin before Is a powerful bactericidal,
surgery used to sterilize sporicidal, fungicidal and
water for cleaning viricidal agent
vegetables, treatment of
tonsillitis and pharyngitis,
lodine ointment is used as
Halogens fungicide in ringworm
lodophors, e.g. povidone Used for preoperative Are soluble complexes of
iodine (Betadine)-5% scrubbing, skin iodine with surfactants like
solution preparation, disinfection of detergents
instruments, as local
antiseptic in boils,
furunculosis, burns, ulcers,
ringworm and in
oral/vaginal moniliasis
Chlorine It is widely used for is a potent germicide and is
disinfection of water bactericidal. It also
supply destroys protozoa and
viruses

Classification Name Uses Action


Oxidizing agents Hydrogen peroxide is used for cleansing Oxidizes bacteria and
wounds, abscesses and for necrotic tissue
irrigation, to clean septic It is also a deodoran,
dental sockets and root
canals, as a mouthwash
and deodorant gargle and
while removing ear wax
Potassium permanganate Potassium permanganate It is an oxidizing and an
is used for gargling, astringent
irrigating body cavities and
wounds, stomach wash,
athlete's foot, topically to
oxidize venom, to purify
well water, to disinfect
vegetables and fruits

Gentian violet (aniline dye, 0.5-1% solution is used It is effective against gram-
crystal violet or medicinal topically on furunculosis, positive organisms and
gentian violet) burns, boils, chronic ulcers, fungi
infected eczema, thrush,
ringworm and mycotic
infections of the skin and
mucous membranes
Staining is the only
disadvantage
Brilliant green Used as a 0.5-1% solution
in the treatment of burns,
impetigo and infected
wounds like gentian violet
Methylene blue Used systemically in It converts methemoglobin
Dyes cyanide poisoning to hemoglobin
Acriflavine and proflavine 1: 1,000 solution is used in Acridine dyes active
infected against gram-positive
wounds and burns, 2% bacteria and gonococci
pessary in (proflavine is better)
vaginitis and cervicitis
They are nonirritant;
efficacy is
unaffected by organic
matter, but are increased
in alkaline medium
Triple dye lotion contains 0.1%-it is used in burns Active against gram
gentian violet 0.25% + dressing and dressing positive bacteria,
brilliant green 0.25% umbilical stump in gonococci and fungi
+acriflavine or proflavine neonates

Classification Name Uses Action


Silver compounds Silver nitrate is used for the prophylaxis of It has antiseptic,
ophthalmianeonatorum astringent and caustic
properties

Silver sulfadiazine Is used in burn wounds Active against


Pseudomonas

Colloidal silver Used as nasal and eye drops It slowly release silver
compounds They are
Metals noncorrosive,
nonirritant,nonastring
ent and have
better penetrability
Zinc salts It is used as an ointment or lotion in Zinc salts like zinc
eczema, impetigo and psoriasis oxide has astringent
and mild
antiseptic properties
Mercury compounds Not commonly used Act by inhibiting
sulfydryl enzymes of
bacteria They are
bacteriostatic and are
poor antiseptics

Factors that Influence the Activity of Germicidal Agents


Concentration of the Drug
In general, higher the concentration of the antiseptic, greater is
its effect. But alcohol is an exception to this and at 70%
concentration maximum antiseptic effect is seen.

Duration of Contact
Higher the concentration of the antiseptic, greater is its effect.

Susceptibility of the Organism


spores and viruses are resistant to many antiseptics.

Temperature
A rise in temperature will increase antiseptic activity of most
germicides.
COMMONLY USED ANTISEPTICS AND DISINFECTANTS
Povidone-iodine Solution
• Povidone iodine (Betadine)-5% solution
• Povidone iodine-5% ointment.
It is used as an antiseptic for skin that is infected or that is
likely to become infected. Povidone lodine works by slowly
slowly releasing iodine, which kills or prevents the growth of
bacteria, fungi and viruses. It has a rapid and prolonged
germicidal action against a wide spectrum of microbes including
gram-positive and gram-negative bacteria, fungi, protozoa and
viruses and also active against bacterial spores in the presence
of blood, serum, exudates and necrotic tissue. It gives a golden
brown color to the tissues. Its activity persists as long as the
color remains.

It is used for the antiseptic treatment of the skin


preoperatively and postoperatively. It is also applied to
superficial wounds, traumatic injuries, burns, vaginal
preparation prior to a surgical procedure.

Nursing Responsibilities
Povidone-iodine solution should be applied in full strength as
paint. The ointment can be applied with a gauze dressing or
directly over the area. It is better to clean and dry the affected
area of skin before applying povidone iodine.

Isopropyl Alcohol
Isopropyl alcohol is used in 68-72% concentration as skin
antiseptic, e.g. ciprit (70%). It rapidly denatures bacterial
proteins. It more potent and more toxic than ethanol.

Nursing Responsibilities
Isopropyl alcohol is used as an antiseptic for cleaning the
injection site. When it is applied give 1 minute time for the
antiseptic to act before doing the procedure.
It is highly inflammable. So it should be kept away from
heat and flame. It is a poison. So care should taken to avoid
ingestion and protect the eyes during its use.

Dettol
Dettol is available as antiseptic liquid, soap and liquid
handwash.
Antiseptic liquid contains choroxylenol-4.8% with terpineol
and alcohol.
It is effective against gram-positive and gram-negative
organisms. Dettol antiseptic liquid is a germicide for personal
hygiene, first aid and disinfection. It can be used to disinfect
linen, floors, etc.

Nursing Responsibilities
For first aid and personal hygiene uses, dettol antiseptic liquid
must always be used diluted with water. It should be diluted to
1:20 ratio for first aid and medical antiseptic use. For
disinfection dettol is diluted to 1:40 ratio.

Savlon
About 1.5% chlorhexidine gluconate and 3% cetrimide as active
ingredients per 100 ml. It is used for first aid and disinfection of
floor, mattress, etc. Hypochlorite bleaches may cause brown
stains to develop in fabrics, which have previously been in
contact with savlon antiseptic. An oxidizing bleach such as
sodium perborate should be used in laundering. Ototoxicity has
been reported after direct instillation into the middle ear.
Savlon is incompatible with anionic agents and its activity is
reduced in the presence of organic matter and soap.

Nursing Responsibilities
Do not use for disinfecting linen. Dilute the product based on
recommendations.

Cidex Solution
Cidex solution is activated glutaraldehyde solution (2%):
• Glutaraldehyde solution-5L
• Glutaraldehyde activator-33 g.
It is an effective antimicrobial and can work in presence of
organic matter. It is non-corrosive, if used properly. The
prolonged contact of cidex solution can cause skin burn
Inhalation of vapors causes mucous membrane irritation. When
ingested accidently it causes burns of mouth, throat, esophagus
and stomach. It is used to disinfect laproscopes, endoscopes,
anesthesia equipments.

Nursing Responsibilities
Wear gloves, mask, aprons when using solution. Use in
ventilated areas to prevent sensitization by inhalation.
Thoroughly clean instrument before putting into solution. The
solution should be used maximum for 14 days. Use in closed
container with tight fitting lid. pH of activated solution should
be lower than 8.2-9.2.

Chlorine
For example, hypochlorites (sodium hypochlorite solution):
• Sodium hypochlorite-5%
• Water-95.5%.
Chlorinated lime (bleaching powder) is obtained by the
action of chlorine on lime. It is used for disinfection of water in
swimming pools and water for drinking.
Chloramine is an organic chloride. The freshly prepared
solution is used for mouthwash, irrigating bladder and urethra.
Eusol is chlorinated lime with boric acid.
It is used to disinfect syringes after use. Bleaching powder is
used to disinfect water. For large scale disinfection chlorine gas
is used directly. Chlorine is a highly effective germicide
(bactericidal, fungicidal, virucidal).
It is corrosive. It is unstable and ineffective in the presence of
organic matter and the action is exhausted fast. So excess
chlorine should be added to during disinfection of water to
obtain free chlorine concentration (0.2-0.4 ppm).
Nursing Responsibilities
Make proper solution, i.e. add adequate amount of sodium
hypochlorite. Wear gloves while handling.

PHENOL AND OTHERS


Sterillium
Each 100 g contains:
• 2-propanol-45 g
• 1-propanol-30 g
• Ammonium ethyl sulfate-0.2 g.
It is used to disinfect stethoscope domes, intravenous (IV)
site connections, thermon Effective against antibiotic resistant
bacteria, tubercle bacilli, fungi and viruses. It is no disinfectant
in hand rub solution. Coagulates protein. It cannot disinfect
large surface areas.

Nursing Responsibilities
Do not apply this disinfectant on wounds. It is inflammable
therefore keep out of reach of the and electricity. Do not touch
eyes when using.

Phenol
Phenol is used to disinfect urine, feces, sputum of patients and
is sometimes used as antipruritic because of its local anesthetic
action. Phenol is used to disinfect floor and also used in
microbiology laboratory.
Has good activity against mycobacteria. It is toxic if diluted
improperly. Phenol causes tissue irritation. It causes
hyperbilirubinemia in neonates.

Nursing Responsibilities
Phenol cannot be used to disinfectant instruments. Protect eyes
when using. It should be kept out of reach of children.

Bacillocid
Each 100 g contains:
• 1,6-dihydroxy 2-5, dioxyhexane
• Glutaraldehyde-5 g
• Benzalkonium chloride-5g
• Alkyl urea derivative-3 g.
It is used to disinfect walls, beds, trolleys, Boyle's apparatus in
operation the Bacillocid is more active against gram-positive
bacteria than gram-negative bacteria. Has good detergent
properties. Inactivated by organic matter. It may support
growth of bacteria in dilute solution. But it is not sporicidal.

Nursing Responsibilities
For OT and other critical care areas use: 2% solution, intensive
care (ICU): 1% solution consulting rooms: .5% solution and for
wards: 0.5% solution should be used.
Do not mix with any other cleansing agent. Wear double
gloves during use. Switch off air conditioner when using. Keep
area wet for half-an-hour. Close room after use for 1 hour. Do
not ventilate AC rooms immediately. Do not use for
instruments.
Formaldehyde
Aldehydes act by alkylation of chemical groups in proteins and
nucleic acids. It is bactericidal, sporicidal fungicidal and viricidal.
It is used for fumigation of rooms. Formaline is 40% solution of
formaldehyde vapor in water. When it is heated, formaldehyde
vapor is generated.

Fumigation
Fumigation is most effective above a temperature of 20 °C and
relative humidity of 65% and at temperatures below 18 °C,
formaldehyde fumigation is less effective. Formaline and water
are mixed and heated using a heating apparatus, which
generates formaldehyde gas.

Nursing Responsibilities
The rooms to fumigated must be well sealed to prevent the
escape of gas. The room should be ventilated only after a period
of 12 hours. There should be an exhaust system to avoid any
person entering the room to exhaust. It is highly toxic to inhale
the vapors. Fumigation should be carried out by trained
personnel. To assess the effectiveness of fumigation culture can
be done or spore strips can be placed at significant locations.
UNIT – 4
DRUG ACTING ON GIT
#Histamine–
Is a biogenic amine found in both plants and animals. It is
an auto acoid. The term auto acoid was derived from 2 greek
words “flutos” c means “Alcos” c mean healing subs so autocoid
means self-healing or self remedy subs.
→ The world histamine was derived from greek word “Histos” c
means tissue or at may be understood as Tissue Amine.
→ Histamine is a compound c is found in all body cells produce.
- ed after break down/decarboxylation of Histamine (a basic
amino acid), so it is considered as biologic amine.
→ Histamine is found in body cells, body cells, body fluids,
platelets, leucocytes, Basopills, most cells, lungs ul G1 mucos
etc.

*Histamine Release – Histamine is a natural amine found in our


body, a no. of chemical, mechanical, or immunological stimuli
can stumilate the release of histamine, mainly from the most
cells for Eg –
i. Trauma
ii. Stings (Bee sting)
iii. Vinoms
iv. Tissue damage
v. Action of Protelytic enzymes.
vi. Ag-Ab involving Igb.
vii. Drugs like morphine, atropine, vaniomycin.
viii. Exposure to allergic etc.

*Mch of Action:- Histamine release occur in response to many


stimuli after it whose action occur through specific receptors.
1. Action by Receptors – This type of action occur on smooth
muscles of different organs except gastric secretion like on
blood vessels, respiratory system etc.
2. Action by Receptors – receptors are located in
stomach only causes gastric juice secretion.
[ The drugs c block the receptors are called Antii Histamines
or RA, they inhibit allergic response, but the action of
receptors is inhibited by RA ( receptor Antagonists) only ul
not by general anti Histamine drugs]

#Pharmacological Action of Histamine –


1. Action of BP – Histamine cause dilation of vessels so BP fall
down, there is pooling of various blood also.
2. Action on Blood vessels – Histamine causes marked
vasodilation of blood vessels ul capillaries. It lead to flushing of
face ul throbbing headache it is called Histamine headache. It is
realized by the use of anti histamine ul ergot c constrict the
capillirus ul blood vessels especially dilated carotid (A) so
headache relives.
3. Triple Response – ID infection of Histamine produces a series
of events, called triple response. It include –
A. local redress (flash) due to dilatation of capillaries ul unnules.
B. Local arteriolar dilatation (Flare)
C. Local oedema (wheal) due to exudation of fluid from
capillaries & venmules.

4. Action on smooth muscles – Histamine causes contraction of


smooth muscles producing Broncho construction, constriction
of intestinal muscles ul uterus.

5. Action on glands ul secretions – Histamine ses gastric juice


secretions it also ses acid – pepsin release it has mild stimulant
action on salivary glands, pancreas and lacrival glands.
6. Action On CNS – Intro cerebro-ventricular administration of
Histamine causes Hypothermia, vomiting, cardic stimulation, so
BP ses (otherwise BP ses)
7. Action on Sensory Nerves – It stimulates nerve endings
itching occurs.
8. Allergic – Histamine is responsible for allergic in host like
sneezing, pruritus lacrimation etc.
→ Histamine is not used pharmacologically, but when its release
become uncontrolled then antihistamine drugs are used
according.

#Anti-Histamincs ( Antagonists) –
- These drugs competitively anlogonizes action of Histamine at
H receptors.

*Pharmacological actions –
1. Antagonism of Histamine – They effectively block Hista
induced brocho constriction. Constraction of intestinal ul other
smooth muscles they inhibit triple response- What flare and
itch. Precautionary use of blockers protect animals fr. Dt
caused by large, I.V doses of Histamine. They denot have any
action on histamine induced gastric secretion ( RA gastric
accretion.)

2. Ant allergic Action – RA control Type I Hypersensitivity liks


urticaria itching ul angio edema.

3. On CNS – Produces sedation, produces CNS depression as


they can penetrate B.B.B. they can prevent motion sickness
reduces tremor rigidity & siolorrhia of Parkinsonism.

4. Anti-cholinergic action – They antagonizes the muscarinic


action of Ach.
→ If used Atropine, Phenothizine Tricylic anti depressants
anticholinergic action.
5. LA effect – Some RA liks Phenotimine have strong LA
action while others have weak LA action.
6. BP – se BP on IV Infection (causing smooth muscle relaxtion)

*Indication – Allergic Rph

*Doses – classification
- High sedative
1. Diphenhytramine 25-50 mg orally
2. Promethazine – 25-50 mg oral
1 m – 1mg/kg bwt.
- Mild sedative –
1. Pheniramine 20-50 mg orally
2. Mecizine – 25-50 mg orally.

- Mild sedative –
1. Chlorpheniramine – 2-4 mg orally
1mg/kg bwt I.M
Cyclizine 50 mg orally

I generation RA
Cetrizins 10 mg orally
Fexofenadix 120-180 mg oral
Loratiadine 10 mg orally
Leuocitrizine 5-10 mg orally.

*Side effect ul Toxicity –


→ Sedation, diminished alertness ul consciousness Tendency is
fall asleep dryness of mouth altered bowrl movements, pain
epigastric headache, LA effect contact dermatitis.

*2nd generation RA are defined as dose (SGAs II generation


Antihistomins) c law one/more of following properties.

*Higher selectivity, no anticholinergic side effect.

# II generation Anti Histamines –


- Absence of CNS depressant property.
- Extra anti allergic action by acting on leukotriene or by
activating factor.

*Indication of SGAs –
- Allergic rhimtis conjunctivitis the fever.
- Verticaria, Atopic sczima.
- AC allergic to drugs food.

RA – act on R in stomach ul are used for R-of PU.


Ranitidine – 300 mg Hs/150 mg BD.
Famotidins – 40 mg Hs/20mg BD.
Roxatidins – 150 mg Hs/75 mg BD.

#Emetics –
→ Emetics are the drugs/subs c produce vomiting,
vomiting/emesis is a protective mechanism c eliminate harmful
subs from the stomach. It occur because of stimulation of
emetic centre situated in medulla oblongata. CTZ
(chemoreceptor Tringular Zone) ul NTS (Nucleus Tractus
Solitarius) are the most important relay areas for afferent
impulses from GIT throat ul other viscera’s to initiate vomiting.
→ Vomiting is to be produces only when safe or undesirable
subs liks – poision has been ingested by someone accidently or
intentionally.
*Types – Emetics are classified according to their site of action –
1. Centrally acting emetics – Eg – Apomorphine
- Ipecac.
2. Peripherally acting emetics – Thypertonic sodium, Mustard,
Cu Ipeacac.

#Apomorphine –
Apomorphine is a semi-synthetic derivative of worpluce, it is
microcrystalline powder.
* MOA – it is a central emetic c stimulate CIZ centre ul vomiting
is associated sedation.
* It should not be used if respiration is depressed.
- Large doses can produced red lessness, tremors ul occasionally
convulsions.
- Sometime ut way cause hypotension, syncops of coma.

*Ludication – As emetic
- Treatment hypomobility of GIT, associated
parkin son’s disease.
*Dose – 6 mg SC/IM
* C.1 –
- Hyperson to Apomorpline/related drugs
- Pregnancy ul lactation
- IV administration.
- Concomitant use 5Ht antagonist.

*S.E – Hypersensitivity skin rashes, pruritus, urticaria.


- Sedation Convulsion
- Respiratory depression Hypotension
- Restlessness Synocope
- Tremors Coma

#Ipecacuvanha (Ipecac) –
Ipecac is obtained from dried roots of cephaelis ipecac. It
alkaloid emetine, ul dinethyl ometin.
*MOA – Ipeace is both centrally ul peripherally acting emetic. It
irritate gastric mucos as well as also stimulate CTZ to initiate
vomiting.
* Indication – As an emetic for overloaded or few condition of
stomacle.
*Doses –
Ad. 10-30 ml orally
Children 10–15 orally

*C.I
- Hypersensitivity to Ipecac.
- Pregnancy ul lactation.
- Use CNS depressants.

*S.t
- Hypersensitivity skin moslus, pruritus, urticaria.
- Yawning
- Dry skin
- Dyskinesis
- Drowsiness/somnolence
- Edema
- Dizziness
- Postural hypotension
- Hallcination

*General Contraindications for Emetics –


1. Morphine poisoning or phenothiazine poisoning.
→ Because emetics are ineffective in such cases.
2. Unconscious pts. → Because of risk of aspiration pneumonia.
3. Keronin poisoning → Because of risk of chemical aspiration
pneumonia.
4. CNS stimulant drug poisoning.
→ Convulsions may occur.
5. Acid/Alkali poisoning
→ Risk of preformation ul further damage to mucosa of
esophagus Wliule acid/ Alkali return from mouth.

# Anti Emetics –
- Anti emetics are the drugs c are effective against vomiting ul
nausea. They are mainly used to treat motion sickness ul the
side effects of some opioid analgesics ul chemo-therapy used
against cancers.
- These drugs mainly act by inhibiting the heceptors site asocial
ed emesis, ul sometimes necessary to suppress nausea ul
vomiting ul in severe cases where dehydration develop.

*Classification
1. 5 Antagonists – Dndasetron
- Graniestron
2. Centrally acting dopamines receptor antagonists or prokinetic
drugs –
- Metochlopromide
- Domperi done
- Chlorpromazine
- Prochlorperazine

3. RA (Histamine Receptor antagonist) –


- Cyclizine
- Di phenhydramine
- Meclizine
- Promethazine

4. Muscarinic receptor antagonist/Anti cholinergic –


- Dicyclomine
- Hyoscine

5. Adjuvant drugs –
- Dexamethasone
- Benzodia zepine

1. 5 Antagonists –
These are the drugs c antanosits 5 receptors ul control
emesis. This group ul drug is used to control vomiting effectively
caused due to use of anticancer drugs/heliotherapy.

*MOA – They antagonizes the action of 5 receptors ul inhibit


CTZ centre so vomitning is controlled.

*Indication – Vomiting ul nausea associated cytotoxic chemo


therapy ul radiotherapy.
- Prophylaxis ul treatment of Post op. vomiting.
* Dosage –
1. Ondansetron
- To control vomiting
8 mg orally BD
- Prevention of chemotherapy induced vomiting.
- For children 4-11 year.
4 mg 30 min before chemotherapy, rpt 4 ul 8 hxs after initial
dose.
- For >12 yrs ul adults.
0.15 mg/kg 3 times/day beginning 30 min prior to
chemotherapy.
- Treatment of hyperemesis gravidarum – 8 mg IV over of 5 min
every 12 hrly.
2. Granisetron –
10mg/kg IV 30 min before chemotherapy.

2. Centrally acting Anti-emetics –


These drugs action dopamine receptors ul antagonizes their
action so control vomiting.
- Metochlopramide
- Chemotherapy induced vomiting IV – 1.2 mg/Kg 30 min before
chemotherapy, rpt every 2 hr for 2 doses, every 3hr for 3 doses.
- Post op. nausea ul vomiting IM/IV – 10-20 mg near end of the
surgery.
- Dompridone
Upper GI motility disorder 10 mg orally IDS.
→ Prochlorperzine –
For children – 2.5 mg OO/BD orally
For Adults – 5-10 mg TDS/QID, orally, maximum 40mg/day
- 5-10 mg dep IM every 3-4 hr or 2.5 10 mg IV every 3-4 hr.
3. RA (Histamine Receptor antagonists)
(Described earlier)
Cyclizine – 50 mg orally
Di phenydramine – 25-50 mg QID
Meclizine – 25 mg orally
Promethazine – 25 mg orally.

4. Anti chlinergics – Anti cholinergic drugs act by blocking the


conduction of nerve impulse across a cholinergic pathway
leading from the vesti bular apparatus to the vomiting centre so
control vomiting.
- Hyoscine – 1.5 mg as transdermal patch applied behind the
pinna.
- Dicydomine – 10-20 mg orally, used for the prophylaxis of
motion sickness ul morning sickness.

5. Adjuvant drugs – Adjuvant anti-emetics are those group of


drugs c ses efficiency of usual antiemetics. They are mainly
used in case of vomiting induced by chemotherapy.

Unit – 4 Drugs Used in GIT System


# Histamine Type 2 ( ) Antagonist – These drugs inhibit the
gastric acid secretion but do not completely step it. It blocks
histamine (H) at the receptors of acid producing parietal cells
producton of H ions is reduced resulting in sed production of
HCl.
* Classification –
Dass Examples MOA
Histamine Type 2 Cimetidine Competitive
( ) Antagonise Ramitidice inhibition of
Famotidine histamine of
NIzatidine receptors of the
gastric parietal cells
resulting in reduced
gastric acid
secretion, gastric
volume ul hydrogen
ion.

Indications –
- Duodenal ulcers ul benign gastric ulcers
- Gastric hypersecretory states.
- Gastroesphageal reflex.
- Heart burn, acid indigestion, or sour stomach.
- H. pylori eradication to reduce the risk of duodenal ulcer
recurrence.

*Contra indicts –
Hypersensitivity to particular histamine type 2 ( )
antagonists, any component of the formulation, or other
antagonist.

*Adverse effect –
Dizziness, agitation, headache, drowsiness’
- diarrhea, nausea, vomiting
- Miscellanceous: Bradycardia, hypotension, tachycardia,
confusion, fever, rask, gynecomastia, edema of the beasts, sed
sexual ability, neutropenia, ogranulocytosis, thrombocytopnea,
sed AST/ALT, myalgia, elevated reatinine.

I. Cimetidine Dosage – Children: Oral, IM, IV : 20-40mg/kg/day


in divided doses every 6 hrs.
- Children 12 years ul adults – oral heartburn, acid indigation
four stomad 200 mg up to twice daily, way take 30 minutes
prior to eating foodsor beverages expected to cause heart burn
or indigestion.
- Adults: short term treatment of active ulcers.
- Oral : 300 mg 4 times/day or 800 mg at bed time or 400 mg
twice daily for up to 8 weeks.
- IM, IV:300 mg every 6 hours or 37.5 mg/hour by continuous
infusion, IV dosage should be adjusted to maintain an
intragastric Ph5.
- Hs an active bleed : Administer cimetidine as a continuous
infusion.
- Duodenal ulcer prophylaxis: Oral 400-80 ,g at bedtime.
- Gastric hypersecretory conditions : oral, IM, IV 300-600 mg
every 6 hrs, dosage not to exceed 2.4g/day.
- Helicobecter pylori eradication: 400 mg twice daily, requires
coubination antibiotics.

II. Famotidine – dosage – children: Peptic ulcer: 1-16 years: oral:


0.5 mg/Kg/day at bedtime or divided twice daily (maximum
dose: 40 mg/day). IV: 0.25 mg kg every 12 hrs (maxi dose 40
mg): doses of up to 0.5 mg/kg have been used in clinical studies.

- Adult – Duodenal ulcer : Oral: Acute therapy: 40 mg/day at


bedtime for 4-8 weeks, maintenance therapy 20mg/day at bed
times.
-helicobacter pylori eradication – 40 mg once daily; requires
combine therapy antibiotics.
- Gastric ulcer – Oral Acute therapy 40 mg/day at bedtime.
- Hypersecretory conditions: Oral – Initial 20 mg every 6 hrs,
way in increments up to 160 mg every 6 hrs.
- GERD – Oral : 20 mg twice daily for 6 weeks.
- Esophagitis & accompanying symtpoms due to GERD Oral 20
mg or 40 mg twice daily for up to 12 weeks.
- Pts unable to take oral medications:- 10-20 mg every 12 hrs.

III. Ranitidne – Dosage (children 1 month to 16 years)


- Duodenal ul gastric ulcer: Oral treatment 2.4 mg/kg/day
divided twice daily, maxi treatment dose 300 mg/day
maintenance 2.4 mg/kg once daily, maxi maintenance dose:
150mg/day
- IV 2-4 mg/kg/day divided every 6-8 hrs, maximum 150mg/day.
Adults – Duodenal ulcer oral treatment: 150 mg twicedaily or
300 mg once daily after the evening oral or at bedtime
maintenances: 150 mg one daily at bedtime.
- Helicobactor pylori eradication 150 mg twice daily therapy.
- Gastric ulcer, benign: Oral-150 mg twice daily, maintenance
150 mg once daily at bedtime.
- Pts not able to tape oral medication:-
- IM:50 mg every 6-8 hrs.
- IV intermittent bolus or infusion: 50 mg every 6-8 hours.

*Nsg resp – Assess for allergies of impaired renal or liver


function.
- Use caution in client are confused, discriminated or elderly.
- Take 1 hr before or after antacids.
- For intravenous doses, follow administration guidelines.
- Smoking has been shown to se the effectives of blockers.
*Pt educaton – Inform prescriber of all prescriptions, OTC
medications, or herbal products you are taking & any allergies
you have do not take any new medication during therapy out
consulting prescriber.
- Take exactly as disrected, do not se dose way take several
days before you notice relief. Allow ulcer b/w any other anta
acids ul ranitidine.
- Avoid alcohol follow dict as prescriber recommends.
- May cause drowsiness, dizziness or fatigue.
- Report chest pain or irregular heartbeat, skin rash, CNS
changes, unusual persistent weakness or bethargy, yellowing of
skin or eyes, or change in colour of urine stool.

#Proton pump inhibitors – This is the newest category of drugs


to treat acid related disorders. The parietal cells release the
hydrogen ions (protons) during hcl production, this process is
called the “proton pump”. Other agents such as blockers &
anti histamines do not step the action of this pump. These drugs
irreversibly bind to H/K enzyme this bond prevents the
movements of hydrogen ions from the parietal cell into the
stomach. This result in achlorhydria, gastric acid secretion is
totally blocked.

*Classification
Type Name of the drug NOA Side effect
Proton pump Rabeprozole Suppresses gastric Chest pain,
inhibitors Omeprazole acid secretin by migraine, anxiety,
Pantoprozole inhibiting the dizziness,
lansoprazole parietal cell H/K ATP headache, rash,
pump pruritus,
hyperglycemia,
diarrhea,
constipation,
dyspepsia,
gastroentris,
abdominal pain,
UTI, liver function
test abnormality,
sed cough
dyspnea upper
respiratory tract.

* Indications
Short term (4-8 weeks) treatment of active duodenal ulcer
disease or active benign gastric ulcer.
- Treatment of heartburn ul other symptoms associated gastro
phageal reflex disease (GERD)
- Short term (4-8 weeks) treatment of endoscopically diagnosed
erosive esophagitis, maintenance healing of examine
esophagtives.
- Long term treatment of pathological hypersecretory
conditions, as part of a multidrug regiman for H pylori
eradication to reduce the risk of duodenal ulcer recurrence.
- Short term treatment of frequent, uncomplicated heartburn
occurring 2 days/wee.
- Healing NSAID – induced ulcers, prevention of NSAID induced
ulcers.
*Contradiction – Hyperson to omeprazole, rapeprazole,
pantoprazde, lanscophrzole, or any component of the
formulation.

*Dose – 1 Rabeprazole – Oral : Adults > 18 years ul elderly


- GERD 20 mg once daily for 4-8 weeks, maintenance 20 mg
once daily.
- Duodenal ulcer 20 mg/day before breakfast for 4 weeks.
- H. pylori eradication – 20 mg twice daily for 7 days to be
administered amoxicillur 1000 mg ul darithromycin 500 mg,
also given twice daily for 7 days.
- Hypersecretory conditions: 60 mg once daily, dose need to be
adjusted as necessary doses as high as 100 mg once daily & 60
mg twice daily have been used.
II. Omeprasole
- Children 2 years : GERD or other acid related disorder.
<20 kg: 100mg once daily
20 kg: 20 mg once daily.
- Adult – Active duodenal ulcer 20 mg/day for 4-8 weeks.
- Gastric ulcers: 40 mg/ day for 4-8 weeks.
- Symptomatic GERD : 20 mg/day for upto 4 wees.
- Erosive esophagitis: 20 mg/day for 4-8 weeks.
- H. Pylori eradication – 20 mg once daily or 40 mg/day as single
dose or in 2 divided doses, requires combination therapy
antibiotics.
- Pathlogical hypersecretory conditions: Initial: 60 mg once
daily.
Doses upto 120 mg 3 tissues/ day have been administered.
- Frequent heart burn: 20 mg/day for 12 days: treatment way be
repeated after 4 months if needed.

III. Pantoprzole Adults (oral) Erosive esophagitis associated


GERD:-
- Treatment 40 mg once daily for up to 8 weeks: an additional 8
weeks may be used is pts who have not healed after an 8 week
course.
- Maintenance of healing 40 nsg once daily.
- Note: (over doses 120 mg once daily) have been used
successfully in wild GERD treatment ul maintenance of healing.
- Hypersecretory disorders (including zollinger-ellison): Initial:40
mg twice daily: adjust dose based on pt needs, doses up to 240
nsg/day have been administered.
- H. Pylori eradication: Doses up to 40 mg twice daily have been
used as part of combination therapy.
- IV: Erosive esoplagitus associated GERD: 40 mg once daily for
7-10 days.
- Hypersecretory disorders: 80 mg twice daily, adjust dose
based on acid output measurments: 160-240 mg/day divided
doses has been used for a limited period (up to 7 days)

*Nsg resp. – Assess for allergies ul of liver disease.


- Pantoprozole is the only proton pump inhibitor available for
parenteral administration & can be used for clients who unable
to take oral medications
- May se serum levels of diazepam, phenytoin ul cause sed
chance for bleeding warfarin.
- It should be taken before meals.
- The capsule be taken before meals.
- The capsule/tab. Should be swallowed whole, not cru slued,
opened, or chewed.
- It was be given anta acids.
- Emphasize that we treatment will be short term.
#Antacids –
Antacids are weak bases given orally to neutralize to gastric
acid ul raise the gastric pH of gastric contents. They also inhibit
the pepsin formation.

*Classification –
1. Systemic – Eg – Sodium bicarbonate
2. Non systemic – Eg. Ng hydroxide
carbonate
Al Hydroxide
*MOA –
Neutralize acidity, sing the pH, or reversibly reduce or
black the secretion of acid by gastric cells to reduce acidity in
the stomach.
* Indications – Gastroesplageal Reflux disease
- Acid ingestion
- Peptic ulcer disease
* Contains – Chronic heart disase
- Inspected stools
- Stomach or Intestine blockage
- Complete or infrequent bowel moments
- Kidney disease, serious kidney problems
- Aluminum poisoning
- Chronic diarrhea
- Hypophospheteris, Hypernatremia

1. Hg Hydroxide – It is used for short term treatment of


occasional constipation ul symptoms of hyperacidity, Mg
replacement therapy, promotes bowel evacuation by causing
osmotic retention of fluid, c distends the colon sed peristetic
activity. Reacts hydrochloric acid in stomach to form mg
chloride.

*Dose liquid preparation –


- Children – 2.5 – 5 ul/4 times/day
- Adult – 5-15 ul 4 times/day

*Tablet – Children – 1 tab 4 times/day


Adult – 2–4 4 times/day

2. Co caronate – As an antacid ul treatment ul prevention of Ca


deficiency or hyperphophatemia/osteoporosis, ostomalace wild
woderate renal insufficiency, hypoparathyroidisue, post
menopausal osteoporosis, rickets) has been used to bind
phosphate.
→ Co salts as antacids neutralize gastric acidity resulting in sed
gastric & drodenal bulb pH they additionally inhibit proteolytic
activity of pepsin if the pH is sed > 4 ul se lower essphageal
sphincter tone.

*Dose – 1-2 tablet or 5-10 ul every 2 hours (oral) maximum


7000mg/24 hours.

3. Al hydroxide – It is used for the treatment of Hyperacidity,


hyperphophateria, temporary protection of member cuts,
scraps of burns.
- It should not be used in case of hypersensitivity to at salts or
any component of the formulation. It neutralizes hydrochloride
in stomach to form Al salt + O

* Dose – oral – 600 – 1200 mg b/w meals ul at bed time.


* Drug interactions – Antacids affect the obsorption of other
medicins such as digxin, INH, tetracycline & antibiotics, if given
orally at the sometime, therefore these drugs should be given
two hrs a part from antacids.

*Adverse effects –
* Carbonate ul Bicarbonate – Regular high dose of carbonate ul
bicarbonate can cause alkalosis c way lead to the altered
excretion of other drug ul also the kidney stones.
* Al hydroxide – It can form the insoluble albuminium
phosphate complexes, c is term way cause hypophosphatemia
ul osteomalacia. Al containing drugs are neurotoxic ul can also
cause constipation. Drugs containing al hydroxids are
contraindicated is pregnancy.
* Mg Hydroxide – Has laxative effect ul there may be the
accumulation of mg in pts renal failure boding to
hypermagnecimia causing cardiovascular ul neurological
complication.
* Sodium – Excessive or sed intake of sodium may be unsafe
for arterial hypertension, heart failure ul renal disease

*Nsg Responsibilities –
- Assess for allergies ul preexisting conditions that may restrict
the use of antacids, such as fluid imbalances, renal disease,
heart failure, pregnancy ul GI obstruction.

- Clients heart failure or hypertension should use low sodium


antacids.
- Use caution other medications due to many drug
interactions.
- Most medications should be given 1-2 hrs after giving an
antacid.
- Antacids may cause premature dissolving of enteric coated
medications, resulting or stomach upset, be sure that chewable
tablets are chewed thoroughly ul liquid forms are shaken well
before giving.
- Administer at least 240 ml of water to enhance absorption.
- Caffeine alcohol, harsh spices ul black pepper way aggravate
the underlying GI condition.
* Pt education – Take as directed, preferably 1-3 hours after
meals (when used as an antacid) or any other medications.
- When used to se phophrous, take in 20 minutes of 0 meal.
- Do not se sodium intake ul maintain adequate hydration
onless instructed to restrict fluid intake.
- You many experience constipation/ sed exercise fluids, fruits
or fiber may help if unresolved contact prescriber.
- Report unresolved nausea, malaise, muscle weakness blood
stool or black stool or abdominal pair.

#Anti-muscarinic/Anti Cholinergics drugs.


- It is not commonly used now, because it is the new drugs are
on board, it relives pair by sing GI motility ul secretion.
- Blockage of muscarinic receptors has dramatic effect on
motility ul secretory functions.

I. Pirenzepine –
*MOA – Pirenzepine is a muscarinic receptor antagonist ul binds
to the muscarinic acetyl.
- Choline receptor. The muscarinic Ach receptor mediates
various cellular responses, including inhibition of adenylate
cyclase, breakdown of phosphoinositides & modilatio of K
channels through the action G proteins.
- Relive cramps or spasms of the stomach, cintetives ul bladder.
- Duodenal or stomach ulcer or intestine problems.
- It can be used together antacids or other medicines or the
treatment of peptic ulcer.
- It may also be used to prevent nausea, vomiting ul motion
sickness.
*Side effect – Dry mouth, blurred vision, droziness, dizziness,
nausea or loss of appetite may occur the first few days as your
body adjust to the medication.
- Hearburn, diarrhea, constipation, bitter taste, sed sexual
ability or desire, bad breath ul bloating.
- Tachycardia chest pain skin rash, difficulty urinating,
confession, curating, vision changes.

* Nsg Resp – Monitor heart rate for above 100/min.


- Assess for urinary retention.
- For dry mouth, candy can be offered
- Monitor bowel movements.
* Pt. Education (Prizenepine) Check your dr before you take
Pirenzpine.
- It may cause blurry vision ul dizziness, c way affect driving,
operating machinery ul other activities.
- It may also cause dryness of the mouth, nose ul throat.
- Do not change the dose or step pirenzepines out consulting
four dr.
- The dose of pirenzepine needs to be reduced gradually to
prevent the drawl side effects.
# Anti-Microbial Agents (Anti H. Pylori Drugs) –
→ H. Pylori lives in the stomach ul infection H. Pylori is
associated gastroduodenal disease including gatritic peptic
ulcer. It is also thought to be responsible for recurrence of
peptic ulcer disease ul is considered as a major risk factor for
stomach cancer.
→ Eradication of H. Pylori along drugs that reduce acid
secretion has shown to reduce the relapse rate. Various
combination regimens are tried clarithromycin, amoxicillin or
tetracycline, metronidazole of omeprazole or a receptor
blocker for 1–2 weeks.
Type Name of the Drug MOA
Anti- Amuxicillin Inhibits bacterial cell wall synthesis by
microbial binding to one or more of the
agents penicillin binding proteins (PBPs),
inhibiting cell wall, biosynthesis.
Clarithromycin Exerts its antibacterial action by
binding to 50 S ribosemoal subunit
result in inhibition of protein
synthesis.
Tetracycline Inhibits the protein synthesis.
Metromidazole Inhibits nucleic acid synthesis by
disrupting the DNA of microbial cells.

- The best triple therapy regnum is:-


Medication Dose/Frequency Course of treatment
- Omeprozole/lansoprazole 20/30 mg bd Given for 14 days followed
- Clarithronycin 500 mg bd by P.P.I. for 4-6 weeks.
- Amoxycillin/Metronidozole 1 gul/500 mg bd Short regimens for 7-10
days not very effective.

- Some other triple therapy Regimens are:-


Medication Dose/Frequency
- Bismuth 2 tab qid
subsalicylate
- Metronidazole 250 mg qid
- Tetracycline 500 mg qid

Medication Dose/Frequency
- Ranitidine Bismuth citrate 400 mg bd
- Tetracycline 500 mg bd
Clarithromycin/Metromidazole 500 mg bd

Therapy
- When the tirple pails, quadriple therapy is given
Medication Dose/Frequency
- Omeprazole Cansophrazole 20/30 mg bd
- Bismuth subsalycilate 2 tabs qid
- Metronidozole 200 mg qid
- Tetracycline 500 mg qid

- All the regimens c are used to H. Pylori eradication are


expensive ul complex. Side effect are common ul compliance is
also poor. Failure rate of regimens ul recurrence rate are life bul
anti H. Pylori therapy helps in lowering the prevalence of ulcer
disease ul also prevents the gastric caricenoma ul lymp homa.
# Emetics (Dr sir wala)

#Anti-Emetics
An anti emetics is a drug that is effective against vomiting
ul nausea.
- These drugs are typically used to treat motion sickness ul the
side effects of some opioid analgesics & chemotherapy
disrected against caner.
- Anti emetics act by inhibiting the receptor sites associated
enesis ul sometimes necessary to suppress nausea ul vomiting
ul is severe cases where dehydration develops, intravenous fluid
way need to be administered to replace volume.

* Classfication – 1.5 H Antagonists – Ondonsteron


- Granisteron
- Antagonize 5 H receptors
*Uses – Cytotoxic drug induced vomiting

2. Centrally acting dopamine receptor antagonist


- Metoclopramide/some peripheral activity of 5 H receptor)
- Domeperidone
- Chlorpromazine
- Prochlorperozine

*Mechanism – antagonist ul 5 H Antagonist.


* Uses – cytotoxic drug induced vomiting.

3. NKI Receptor antagonist – Aprepitant


- Neurokinin A antagonist

* Use – cytotoxic drug induced vomiting

4. Histamine receptor antagonist – Cyclizine,


diphenhydramine, meclizine, promethazine.

→ Antagonize receptors
Use – Motion sickness.

5. Muscarinic receptor antagonist –Thyoscine (Scopolamine)


→ Antagonize Muscarinic receptors
Use – Motion sickness

6. Cannabinoid receptor antagonists – Dronabenol


→ Antagonize cannabinoid receptors
Use – Cytotoxic drug induced vomiting

7. Benzodiazepines – Midazolan, lorazepam

*Use – Cytotix drug induced vomiting adjunct Rxn of nausea


vomiting first live drugs.

8. Steroids – Dexamethasone
Use – Nausea/vomiting
*Indications ul side effects –
1. Ondansteron – Indications
- Radio therapy induced vomiting
- Chemotherapy induced vomiting
- Post op. vomiting

*Side effects – Constipation, Headache


2. Metoclopramide – Indications
- Chemotherapy induced vomiting
- Post op. vomiting
- Dyspepsia
- GERD

*Side effect – Rest lessens, dry mouth, Headache, Parkinson’s


symptoms.

3. Domepridone – Indications – Nausea, vomiting, gastro


poxesis, Pediatric GERD.

4. Prochlorprazine – Indication – Nausea/vomiting


Side effect – Drowsiness, Headache

5. Promethazine – Indication – Drug induced, Post anecdotic


nausea/vomiting.
- Disease induced vomiting
- Elevolluraphy induced vomiting

*Side effect – sedation, muscles dystonia


6. Cyclizine – Indication – Motion sickness
- post op. vomiting
Side effect – sedation, dry mouth.
7. Hyoscine (scropolamine) – Indication – Motion sickness, short
brisk journeys.
* Side effect – Dry mouth, dizziness

*Contraindios – Hypersens to any component of formulations.


- Pomperidone should not be used whenever gastro intestinal
stimulation might be dangerous.
Eg:- Cannobinoids should be avoided pts a history of
schicophrenia.
- GI obstruction, peforation or hemorrhage.

*Commonly used anti-emetic drugs –


1. Meto clopramide – Dose
- Chemotherapy induced emesis – IV. 1-2 mg/kg 30 minute
before chemotherapy ul repeated every 2 hrs for 2 doses, every
3 hrs for 3 doses.
- Post. Op. nausea ul vomiting IM/IV – 10-20 mg near and of
surgery.

* Nsg Resps – Assess potential for interaction other


pharmacological agents pt may be taking (any anti psychotirc
agents, opioids)
- Vital sign should be monitored during IV administration.
- In pts should use safety measures/side rails up, call light in
reach/ ul caution pt to call for assistance ambulation.
- Assess results of laboratory test (RFT), therapeutic
effectiveness (relief of symptoms) & adverse Rxn/seizures, fluid
retention, CNS changes etc.)
- Teach pt proper use, possible side effects appropriate
intervention ul adverse symptoms report.

2. Ondansetron – Prevention of chemotherapy – induced


emesis
- 0.15 mg/kg 3 times/day beginning 30 minutes prior to
chemotherapy.
- 0.45 mg/kg once daily.
- 8-10 mg 1-2 times/day
- 24 mg or 32 mg once daily.

- Treatment of hyperemesis gravidum – 8mg administered over


15 minutes every 12 hours or 1mg/hour infused continuously
for up to 24 hrs In/IV.

*Nsg Reps – Post operative nausea ul vomiting as a single dose


approximately 30 minutes before the end of anesthesia.
- Assess allergy history (selective 5 - receptor antagonists)
prior to administering.
- Use caution in presence of or potential for cardiac
conduction abnormalities (QT prolongation, electrolyte
abnormalities.)
- Follow specific administration specifics acc. To formulation.
- Assess therapeutic effectiveness & adverse Rxn on a regular
basis.
- Teach pt possible side effects ul adverse symptoms to report.
3. Domeperidone – Upper gastrointestinal motility disorders.
The usual dosage in adults in 10 mg orally 3 to 4 times a day 15-
30 minutes before meals ul at bed time if required.
- In severe or resistant cases the dose way be sed to a maxi of
20 mg 3 to 4 times a day.
- Nausea ul vomiting associated dopamine agonist of
antiparkinsonian agents. The usual is adult is 20mg orally 3-4
times a day higher dosage way be required to achieve symptom
control while of the anti parkinsonian medication is occurring.

* Pt education – Take as directed, 15-30 minutes prior to meals,


do not se dosage out consulting prescriber.
→ May cause dizziness, headache, insomnia & irritability
contact prescriber if experience abnormal, uncontrolled
movements or confusion occur.
→ Report breast pain or enlargement, milk production
irregularities or importance.
- Pregnancy/breast feeding precautions inform prescriber if you
are or intend to become pregnant breast feeding is not
recommended.

ANTI DIARRHEAL DRUGS


→ Anti diarrheal are the group of drugs, which are used to
relieve symptoms of disorders and the effects of it but do not
care the problem.
Classification:-
(1) Absorbents:-
(A) Ispaghula
(B) Psyliun
(C) Methyl cellulose

Uses:- Irocitative Bowel Syndrome


Ilecotomy colostomy diarrhea
(2) Antisecretory:-
(A) Mesalazine
(B) Bismuth Subslicylate
(C) Racecadrotil
(D) Sulfasalazine

Uses:-
Ulcerative colitis
Travellor’s diarrhea
Acute Secretory Diarrhea

(3) Antimotility:-
(A) Codene
(B) Loperamide
(C) Diphenoxylate astropine

Uses:- Non injective and mild travellor’s Diarrhea


After onal surgery, colostomy

(1) Absorbants:-
- These are the colloidal bulk forming substances which absorb
water and swells up. They modify the consistency and
frequency of stools and give an in ression of improvement but
does not reduce the water and electrolyte loss.
Eg – Ispeghula (Psyllium husk)
(A) Ispaghula (Psyllium Husk):-
→ Psyllium husk is white fibrous material derived from psyllium
seeds.
→ It is an effective product with varieties of uses in
pharmaceuticals, cosmetics and food products industries.
→ It consists of the epidermis and collapsed adjacent layers
removed from the dried ripe seeds of plantago ovate.
→ It acts as a demulcent, cooling loxative, mild purgative and
natural lubricant.

Mechanism of Action:-
→ Psyllium contains up to 70% of soluble and 30% of insoluble
fibers.
→ When psyllium husk is mixed with water or other liquids like
juice, it forms a gel like relations mass. It moves down the
digestive urgen soaking up toxins and harmful residuces, it
flushes out the toxins of the body through stools.
→ Soluble fibres content of psyllium husk has the obility to bind
with bile acids an important player in digestion of fats found in
over body from chlestrcoli this process lowers circulating blood.
Chloestrol level, by excretion of those fats.

Indication –
Constipation, diarrhea
→ Diabetes/reduces the release of dictory surgen from the
digestive tract into the blood stream.
→ Cholestrol control
→ Colon cancer
Contraindications:-
Intestinal blockage, Megacolon, difficulty swallowing,
hypersensitivity to ispaghula.

Dosage:-
Regular dosage of 5-7 of pure psyllium is preferred ample intake
of liquid should be. Accompanied the dose (125-150 ml/5g)

Side effect:-
Such as allergic skin and respiratory reactions to psyllium dust,
have largely been limited to people working in plants
manufacturing psyllium products.

II Anti secretory (Sulfasalazine):-


Mechanism of Action:-
Acts locally in the colon to decrease the inflammatory
response and systemically interferes with secretion by inhibiting
prostaglandin synthesis.

Indication:-
- In ulcerative colitis
- Enteric coated tablets are also used for rheumatoid. Arthritic
(including junile rheumatoid arthritis) in patient who
inadequately respond to analgesics and NSAID’s
→ Ankylosing spondylitis, collagenous colitis, crohn’s disease,
proriasis,
*Contraindications:-
→ Hypersensitivity to sulfasalazine, sulfa drug, salieylates
→ GI obstruction
→ Pregnancy (at term)

* Adverse Effect:- Headache, Photosensitivity, nausea, vomiting,


diarrhea, gastric distress, urticarial, pruritus, aplastic anemia,
drowsiness, leukopenia, hematuria, alopecia, anaphylaxis,
hepatitis etc.

*Dosage → Children > 2 years, ulcerative colitis initial 40-


60mg/kg/day in 9-6 divided doses.
Maintenance dose 20-30 mg/kg/day in 4 divided dose.
→ Children > 6 yrs Rheumatoid arthritis Enteric coated tablet
50-50mg/kg/day in 2 divided doses.

- Adult – ularative colitis – 1g 3-4 times/day, 2g/day


maintenance in dived dodes.

- Rheumatoid arthritis – 0.5-1g/day, se weekly to maintenance


dose of 2jg/day in 2 divided doses, maximum 3g/day.

*Pt education – Inform presciber of any allergies


- Do not take any new medication during therapy out
consulting presciber.
→ Take a missed dose as soon as possible, if almost time for
next dose, skip the missed dose & return to your regular
schedule.
- if you have diabetes monitor blood glucose level closely (way
cause sed effect of oral hypoglycemic agents)
→ Laxatives causes the production of soft, formed stool over
one or more days ul purgatives are responsible for rapid,
intense fluid evacuation of bowel.

*Classification –
1. Bulk laxatives – Bran, plantago seeds, Agar, methyl cellulose,
Ispahul a husk.
* MOA – se the stool bulk ul stimulates peristalsis.
* Side effect – Flatulence ul abdominal distention.

2. Fecal softners – Decusate sodium


- Liquid paraffin (Emollients)

*MOA – Reduce surface tension of the oil water interface of the


stool resulting in exhanced incorporation of water ul fat
allowing for stool softening.

*Side effects –
A. Decusate sodium (dactyl sodium sulphosuccivate) softens
feces by covering the surface tension of the intestinal contexts c
allows more water to be retained in the feces.

*H Education – Should be taken a full glass of water, milk fruit


juice.
- Do not use if abdominal pain, nausea, vomiting are present.
- should be used for a short period of time prolonged use may
result in abuse, dependence, as well fluid ul electrolyte loss.
→ Reporting bleeding or if constipation occurs

B. Liquid paraffin – is a chemically inert mineral oil that is not


digested. It lubricates ul softens feces.
- It is uhpalatable, aspiration may cause lipid pneumonia. It may
lack out of the anus causing discomfort. Not preference.

3. Osmotic purgatives – are solrtes that are not observed in the


intestine osmotically retain water ul se the bulk of intestinal
contents.
→ They se peristatis to evacuate a fluid stool. They are used to
prepare the bowel before surgery ul in food poisoning.

4. Stimulant purgatives – Stimulant purgatives se intestinal


vomiting ul se the secretion of water electrolytes by the
mucosa. They may cause abdominal cramps.

A. Phenolphthalin – An indicator used in laboratories acts on the


colon after 6-8 hours to produce soft, semiliquid stools some
girpping.
→ It undergoes entero hepatic circulation c prolongs its actions,
allergic including pink coloured eruptions, others severe forms
of allergy of colic limit its use.

B. Bisa codyl – R/t phemolphthalin is converted to active


metabolite in the intestine. It can be given orally (Dulocolax
5mg) but usually is used as retal suppositories (10mg) c results
indefication in 15-30 minutes. It is safe except that prolonged
used may cause local infection/inflammation.
C. Castor oil – Is hydrolyzed in the upper small intestine to
ricinoletic acid, a local irritant that ses intestinal motality.

→ It is a powerful purative ul one of the oldest purgation


known.
→ Stool is semiliquid ul is accompanied by gripping.
* Nsg alert – A pt receiving laxative must se fluid intake to
prevent dehydration.

*Nsg responsibilities –
→ Determine cause of constipation before treating,
→ Evaluate therapeutic effectiness (improved bowel function)
ul adverse response (cardiac event, diarrhea, hypovolemia,
hypotension, syncope) ischemic colitis, rectal bleeding,
abdominal pain.
→ Teach pt proper use, side effects, intervention, ul symptoms
to report.
→ Docusate liquid should be given milk, fruit, juice or infant
formula to mask the bitter taste.

*Fluids ul electrolytes –
There are mainly three different types of IV fluids
depending on their osmolality.
- Isotonic
- Hypotonic
- Hypertonic
- Fluids c are having an osmolality nearly equal to that of that of
extra cellular fluid (ECF) of our body or if the electrolyte content
(cations ul anions) is nearly equal to 310 meq/L, they are
considered istonic fluids.

- Isotonic electrolyte content – 310 m eq/L


- Hypotonic electrolyte content -<250m eq/L
- Hypertonic electrolyte content > 375 m eq/L (Plasma
osmolality is nearly)
Equal to 300 m mol/L osmolality of 10% dextrose is 505 m mol)

1. Isotonic fluids – The isotonic fluids are isotonic to human cells


or have some osmolality as that of body fluids. So there is very
little osmosis c dose not affect the size of RbS (neittm slrink not
swell) however pts hypertension ul cordiac failure need
careful vomiting to avoid fluid overload.

* Egs – Normal saline solution (0.9% sodium chloride) remains


in the ECF because the electrolyte make up its osmolality it is
used in hyponatremia. It should be avoided in heart failure,
pulmonary edema ul renal impairement.

- Lactated Ringer’s solution contains , Ca ul sodium chloride


the lactate provides bicarbonate ul helps to correct acidosis, it is
used to correct dehydration, hyponatremia ul replace
gastrointestinal fluids, many other similar solution including
diarrhea treatment solution (DTS) are available which changes
in the electrolyte content.
II. Hypotonic fluids:- Replace cellular fluid because they are
hypotonic as compared to plasma. When a solution has a lower
concentration of solute than another solution then it is known
as hypotonic solution. These solutions have lower osmolality
than the body fluid. Half normal saline (0.45% sodium chloride)
is the commonly used hypotonic solution but other electrolyte
solutions are also available 2.5% dextrose solution ul 0.25%
sodium chloride solutions are other hypotonic solutions,
hypotonic sodium solution is used in hypernatremia ul other
hyperosmolar conditions, over dosage can result in intra
vascular fluid depletion, hypotension, ullular edema ul later
damage.
III Hypertonic fluids – A solution c has higher concentration of
than another solution is known as hypertonic solution. Five
percent dextrose in NS or lactated ringer’s solution or in
hypotonic solution has osmolality more than ECF, 45% to 50%
dextrose solution may be administered in hypoglycemia or to
supplement calories, since these solutions are strongly
hypertonic, they should be injected into central veins for rapid
dilution.
→ Hypertnic saline solutions draw water from the cells ul the
cells slvink. They should be infected slowly ul carefully to aoid
ECF volumes overload.

Unit - 05
Drugs used in Respiratory System
Drugs used in respiratory system –
These are chemical substances used in the respiratory tract
infection, obstruction which improve bronchial secretions &
provide relief from bronchial congestion irritant & inflammatory
mediators.

#Antiasthmatics Drugs –
Bronchial Asthma is characterized by dyspnea & wheeze
due to sed resistance to the flow of air through the bronchi,
Bronchospasm, Mucosal congestion & edema result in sed
resistance.
Individual suffering from asthma have bronchial smooth
muscles which are hypersensitivity to constricting agent
normally present in the body.
Eg:- Acetylcholine, histamine, slow reacting substance A &
prostaglandins.
Reversible constriction of smooth muscles of the bronchi result
in constriction of air passages which produces a wheeze along
with inflammation of the bronchial mucosa when patient
exhales.
The tracheobronchial smooth muscles is hyper sensitive to
various stimuli like – dust, allergens, cold, air, infection & drugs.

These trigger factors, trigger an acute attack Antigen antibody


interaction on the surface of most cells leads to release of
mediators of inflammation. Inflammation is the primary
pathology.

*Classification –
(1) Bronchodilators:-
(A) Sympathomimetic – Salbutamol, salmeteral Adrenaline,
Terbutaline, Ephedrine.
(B) Methylaxanthines – Theophylline, Aminophylline,
Hydroxyethyl theophylline.
(C) Anticholinergies – Ipratropium bromide Tiotropium Bromide.

(2) Leukotriene Antagonists – Mentelukast zafirlukast.


(3) Anti-inflammatory Agents –
(A) Systemic corticosteroids – Hydrocortisone prednisolone.
(B) Inhalation corticosteroids – Beclomethasone, Dpropionate,
Budesonide, Fluticasone, Propionate.
(4) Most cell stabilizers – Sodium cromoglycate, Ketotifen,
Nedocromil.
(5) Anti-Ige Antibody – Omalizemab.

Bronchodilators Drugs –
These are the drugs used in bronchial asthma & relax the
spasm of bronchi by sympathetic nerve system stimulation.

(A) Sympathomimetic
The sympathomimetic drugs whose action mimic that of
sympathetic stimulation.

- The sympathomimetic agents or B-Adrenergic receptor


agonists are more widely used for treatment of asthma.
- There are two types of B-adrenergic receptor & .
- The - adrenergic receptors present in heart & adrenergic
receptors present in lungs.
- By stimulation of adrenergic receptors. These agents, relax
bronchial muscles inhibit the release of mediators from most
cells enhance mucociliary activity activity effect composition of
mucus.
- SO when B-adrenergic receptor agonists are administered,
adverse effects are cause by stimulation of -receptor in heart,
cause cardiac stimulation. This, now drugs having greater
affinity to adrenergic receptor has been develops.

#Selectively receptor Agonist –


(1) Salbutamol [Albuterol] – It is acting adrenergic receptor
agonist for the relief of bronchospasm in conditions such as
asthma & chronic obstructive pulmonary disease.

MOA –
Airway smooth muscles hs little sympathetic nervous supply
but contain lots of adreno receptor that respond to
circulating adrenaline. The stimulation of receptors lead ot in
(C-AMP) intracellular cyclic adenine monophosphate [C-AMP]
levels & subsequent bronchial smooth muscle relaxation.

#Pharmacodynamics/Kinetics –
- On set of action – Nebulization/oral inhalation 0.5-2
hours/oral 2-3 hours.
- Duration – Nebulization/oral inhalation – 3-4 hour oral – 4-6
hours
- Metabolism – Hepatic to on inactive sulfate.
- Half-life Elimination – Inhalation – 3-8 hours oral – 3.7-5 hours
-Ex creation – Urine

#Indication –
- Bronchodilator in reversible airway obstruction due to asthma
or COPD.
- Prevention of Exercise induced bronchospasm.
- Can be aerosolized with a nebulizer for patient with cystic
fibrosis along with ipratropium bromide.
- Nocturnal Asthma, Bronchial Asthma.
- Allergic states.

*Contraindications –
i) Hypertension
ii) Dysrhythmia
iii) Those using Theophylline drug
iv) Hypersensitivity

*Side effects – Tachycardia, Angina, Atria, fibrillation,


palpitation, Supraventricular tachycardia.

→ Anxiety
→ Insomnia
→ Restlessness & fatigue
→ Headache
→ Tremor
→ Muscle Cramps
→ Rashes, urticarial
→ Dry mouth, Diarrhea, Dyspepsia, Nausea & vomiting.

*Dosage → Oral [children] →


- 2-6 years → 0.1-0.2 mg/kg/dose 3 times/day.
- 6-12 yrs → 2mg/dose 3 to 4 times/days.
*2-4mg/dose 3 to 4 times/day
*Stented release – 3mg every 12 hours.
* Elderly → 2mg 3 to 4 times/day.
Maximum 8mg 4 times/day.
*Nebulization –
Children → 2-12 years → 0.63-1.25 mg every 4-6 hours as
needed.
Quick relief – 0.63 – 2.5 mg every 4-6 hours as needed.

→ Exacerbation of asthma 2.5-5mg every 20 min. for 3 doses


then 2.5 – 10mg every 1-4 hours as needed.

*Drug interaction –
→ When used with corticosteroids their action ses.
→ They ses the action of B-blockers or B-blockers ses their
action.

#Role of Nurse →
→ Teach how to use inhaler apparatus. Emphasize to take the
correct dose of medication at the right time.
→ Inhalers can be used at 20 min intervals.
→ If administered three time in one attack, they should seek
medical attention.
→ Instruct to take these medicines early in the evening to avoid
insomnia.
→ In children advice to use inhaler before brushing teeth to
prevent mouth irritation.

(2) Terbutaline –
Dose –
- For adult – 2.5 mg to 5 mg orally 6-8 hourly.
- For children –
*up to 5 years → 1.5mg orally 8 hourly.
*6-8 years → 2.5 mg orally 8 hourly.

(3) Salmeterol – 2 inhalation of 50 mg 12 hourly.


(4) Ephedrine –
For adult – 20 – 30mg orally TDS
For children –
2-3 mg/kg body weight orally in 3 divided doses.
It is a sympathomimetic amine commonly used as a
stimulant, appetite suppressant. Conn. aid, decongestant & to
treat hypotension associated with anesthesia it is chemically
employed for treating allergy & asthma for its decongestant &
bronchodilator properties.
Administered through the mouth or Nose or by injection.

MOA →
Ephedrine release tissue stores of Non-epinephrine &
therapy produces an & B adrenergic stimulation.
Longer actin & less patent than epinephrine.

*Pharmacodynamics/Kinetics:-
- Onset of Action – Oral – bronchodilation – 0.25 – 1hour.
- Duration – Oral – 3 – 6 hours.
- Distribution – Crosses placenta – enters breast milk.
- Metabolism – Minimally hepatic.
- Half-life elimination – 2.5-3.6 hours.
- Excretion – Urine

*Indication –
→ Treatment of bronchial asthma, acute bronchospasm.
→ Idiopathic orthostatic hypotension.
→ Anesthesia induced hypotension.
→ Post operative Nausea & vomiting.
Contraindication → Hypersensitivity to ephedrine or any
component of the formulation. Cardiac arrhythmia glaucoma,
concurrent use of other sympathomimetic agents.

*Adverse Reactions:-
→ Arrhythmias, chest pain, elevation or depression of blood
pressure, tachycardia, Dyspnea.
→ Agitation, anxiety, excitation, fear, headache, hyperactivity,
Insomnia, Diaphoresis.
→ Anorexia, GI tract, Nausea, vomiting xerostomia.
→ Painful urination.
→ Tremor, trembling, weakness.

*Dosage –
* Children – Oral – 3mg/kg/day every 4-6 hours IM.
* Adult – oral – 25 to 50 mg every 3-4 hour as needed.
Parentral adult dose should not exceed 150 mg in 24 hours, IV
5-25 mg/dose slow IV push.

*pt. Education –
Use this medication exactly as directed do not take more
than recommended dosage.
- Avoid other stimulant prescriptive or 09 C medications to
avoid serious overdose reactions.
- Report excessive Nervousness or excitation, inability to sleep,
facial flushing, charges in heartbeat. Muscle tremors, chest-
pain, palpitation, bronchial irritation or coughing, sed
sweating.
- Inform prescriber if you are or intend to become pregnant.
- Breastfeeding is not recommended.

Methylanthines –
Theophylline (Theophylline) –
Theophylline also known as dimethyl xanthine drug used in
therapy for respiratory disease such as COPD or asthma.
- It acts as a member of the xanthine family, it bears structural
& pharmacological similarity to caffeine.
- It is available as a no. of different salts the most common of
which are aminophylline [Ethylene demine] & choline the
ophyllinate.

MOA →
It causes breno hotilation, diures CNS & cardiae stimulation
& gastric secretion by blocking phosphodiesterase which se
tissue cens of CAMP which turn promotes catecholamine
stimulation of lipolysis, glycogenesis & glyconeoger & induce
release of ephinephrine from adrenal medulla cells.

#Pharmacodynamics/Kinetics –
- Absorption –
After oral consumption, drug absorbed in stomach &
intestine.
- Distribution –
0.45 L/kg [0.3-0.7 L/kg] based on ideal based on ideal body
hit. Distributer pearly into the body fat.
- Metabolism – Children > year & adults Hepatic forms active
metabolites.
- Protein binding – 40% primarily to albumin.
- Half-life elimination – Depend upon age, function, cardiae
femotion, lung disease & smoking history.

Children – 3.7 hours [1.5-5.9 hours]


Adult – 8.7 hours [6.1-12.8 hours]

- Excretion – Urine

*Indication –
Airway obstruction due to chronic asthma or other chronic
lung disease.
- Apnea of prematurity.

*Contradictions –
- Hypersensitivity
- Premixed infection may certain corn-derived dextrose & its
use is contraindicated in pts with allergy to its products.

# Adverse effects –
- Flutter, Tachycardia.
- Headache, Hyperactivity, insomnia, seizure.
- Hypercalcemia, Nausea, vomiting, ulcer.
- Difficulty urinating, Diuresis, Tremor.

*Dose –
- Adult Mini/Max dose – 6.0 mg/kg. 24.0mg/kg.
- Pediatric – 2.0 mg/kg, 24.0 mg/kg.

# pt. education –
Take exactly as directed, do not exceed dosage.
- Avoid smoking [May interfere with absorption].
- Preferable to take an empty stomach before or 2 hours after
meals with a glass of water.
- Avoid dietary stimulant eg:- Tea caffeine etc.
- Maintain adequate hydration.
- Inform prescriber if any side effects, adverse effect appear.

3. Anticholinergic Muscarinic Antagonistic Ipratropium


Bromide:-
It is r/t atropine & acts as a broncho dilater by uritue of its
antichalinergic action.
- It is a cholinergic blocking agents.
MOA –
It has a powerful local action on the bronchi but avoids the
unwanted side effects of atropine. It should be used for those
pt. who have not responded to Agonists.
- It blocks muscarinic cholinergic receptors resulting in a se in
the formation of C-GMP.
- Most likely due to actions of C-GMP on intracellular calcium,
this results in sed contractility of smooth anuscle.
* Its bronchodilators effects begin after about 45 minutes &
casts for 3-4 hours, therefor. It is best taken regularly to prevent
an asthmatic effect.

*Pharmacokinetics –
- For the treatment of abstractive lung disease.
- Ipratropium is also combined with albuterol [salbutamol],
trade Name [Combiuent & Duneb] for the management of
COPD & Asthma.
- I can reduce rhinorrhea, but will not help nasal congestion.

#Contraindications –
1. Hypersensitivity.
2. Bronchospasm.
3. Glucoma.
4. Prostatic Hyperplasia.
5. Bladder Neck Obstruction.
6. Pregnancy & lactation.

*Side effect –
i) Dry mouth.
ii) Dry throat.
iii) sed heart rate.
iv) Blurted vision.
v) Urinary difficulty/retention
vi) Constipation.

*Adverse effects –
- Palpitations, Hypertension, Tachycardia, Hypotension, SVT,
fibrillation.
- Cough, Exacerbation of symptoms Bronchitis dyspnea, upper
respiratory tract infection.
- Nervousness, Headache, Dizziness.
- Constipation, Dyspepsia.
- Allergic rexn.

*Dosage –
Aerosal/Inhalation – Two inhalation – 4 times do not exceed
inhalation in 24 times.
Solution – 500mg (1 unit dose vial) administered 3 to 4 times a
day by oral or nebulization.

The solution can be mixed in the nebulizer with albuterol if used


within the hour.
Spray 0.03 formulation – 2 spray per nostril two or three times
daily.
*Pts education –
- Instruct pt. on proper use of inhaler & proper sequencing &
timing if using more than one inhaled agent.
- For relief of dry mouth, suggest use of saliva substitute,
practice of good oral hygiene rising of mouth, after inhalation.
- Instruct pt. to take sips of water frequently.
- Aduise pts. Using aerosol to seek immediate medical attention
if recommendation dosage dose not provide relief or if
symptoms warson.
- Inform the doctor or care given if any adverse or side effect
occur & warson the condition.
Leukatriene Antagonists:-
Montelukast –
A leukotriene antagonists is a drug that inhibits leukotriene.
Leukotriene inhibitors [Modifiers] such as montelukast,
zafirlukast & ziteuten, are used to treat those diseases.
Leukatriene inhibitors are less effective than corticosteroids,
bed have virtually no side effects, so they are often used treat
children.
Leukotriene are a group of Naturally occurring chemicals in the
body that promote inflammation of asthma & seasonal allergic
rhinitis & in other diseases in which inflammation is important
[such as allergy].
MOA –
Selective leukotriene receptor occupation have been
correlated with the pathophysiology of asthma, including airway
edema, smooth muscle contract & altered. Cellular activity
associated with the inflammatory process, which contribute to
the signs & symptoms of asthma. Cysteingl leukotricines are
also released from the nasal mucosa following allergies
exposure leading to symptoms associated with allergic rhinitis.
#Pharmacodynamics/Kinetics –
- Duration – >24hours
- Absorption – Rapid
- Protein binding plasma > 99%.
- Metabolism – Extensively Hepatic.
- Bio assail ability – Tablet – 10 mg – 64%
5mg – 0.3 – 73%
- Half-life – 2.7 – 2.5 hours
- Excretion – feces [86%]
Urine [20.2%]

Indications –
- Prophylaxis & chronic treatment of asthma.
- Relief of symptoms of seasonal allergic rhinitis.
- Prevention of exercise bronchospasm.
- Acute asthma.

#Contraindication –
- Hypersensitivity to Montelukast.

*Adverse Reactions –
- Dizziness, Fatigue, fever, headache.
- Rashes.
- Dyspepsia, Dental pain, Gastroenteritis.
- Aspirate Aminotransferase [AST] sed, adlanine transaminase
sed.
- Weakness.
- Cough, Nasal congestion, epistaxis, Sinusitis, upper respiratory
tract infection.

*Dosage – Oral (children) –


- 6-11 month – Asthma – 4mg – once daily taken in evening.
- 6-23 months – Rhinitis – 4mg – once daily.
- 12-23 months – Asthma – 4mg – once daily in evening.
- 2-5 years – Asthma, Rhinitis – 4mg [Oral chewable tablet] once
daily, evening.
- 6-14 years – Asthma, Rhinitis – Smg [chewable tablet once
daily, in evening]

*Children above 15 years & adult –


- Asthma Rhinitis – 10 mg/day, in evening.
- Asthma, acute – 10 mg as a single dose.
- Bronchoconstriction, Exercise induced prevention 10 mg at
least 2 hours prior to exercise.

Pt. education –
- Do not stop other asthma medication unless advised by
prescriber. Chewable tablet contains phenylalanine take every
evening on a continuous basis.
- Client may experience mild headache (mild analgesic may
help) or fatigue dizziness [use caution when driving]
- Report skin rash or itching or any other effects like cough,
congestion, behavior & mood change [suicidal thoughts]
worsening of asthmatic condition.
- Inform prescriber if you are a intend to become pregnant.
- Consult prescriber if breast feeding.

*Anti-inflammatory Drugs –
Inflammation is the primary pathology in bronchial asthma,
anti-inflammation agents [steroids] give significant benefits in
the treatment of asthma.
*Action –
Steroids se the inflammatory cell activity in the respiratory
tract there by inhibit bronchoconstriction.
These reduce bronchial edema & reactive beta receptors in pts.
Who become resistant to beta agonists.
These drugs are therefor, used only in cases where the pt. has
ceased to respond to common drugs.

#Corticosteroids Systemic:-
(A) Hydrocortisone –
It is a natural cortices steroid produced by the adrenal
glands located adjacent to the kidneys.
- It is used as in immunosuppressive drug, given by infection in
the treatment of the severe allergic reaction such as
anaphylaxis & angioedema.

*Pharmacodynamics/kinetic –
- Onset of action – Hydrocortisone acetate slow, hydrocortisone
sodium surinate [water soluble] – Rapid.
- Duration – Hydrocortisone acetate – long
- Absorption – Rapid by all routes
- Metabolism – Hepatic
- Half life elimination – 8-12 hours
- Secretion – Urine

*Dosage –
Oral – 2.5 – 10mg/kg/day or 75-300mg/ /day every 6-8 hours.
IM, IV – Succinate – 1-5 mg/kg/day or 30-150mg/ /day every
12-24 hrs

*Status Asthmatic – (Child & adult) –


IV – Succinate – 1-2 mg/kg/dose every 6 hrs for 24 hours.
(B) Inhalation Corticosteroids –
#Betamethasone –
Inhaled corticosteroids are the preferred treatment for long
term central of mild persistent, moderate or severe asthma
symptoms in children, terms & adults.
They help central Narrowing & inflammation in the bronchial
tubes. They are generally part of the daily asthma treatment
plan & are used everyday.

*MOA –
Central the rate of protein synthesis & depresses the
migration of polymorphonuclear leukocytes fibroblacts.

It also reverse capillary permeability & lysosome stabilization at


the cellular level to prevent or central inflammation.

Dosage – Inhalation, Nasal –


Rhinitis, Nasal polyps – Children – 6 years adults 1-2 inhalation
each nostril twice daily.

Total dose – 168-336 mg/day

*Inhalation oral – Asthma –


- Children 5-11 year, initial – 40 mg twice daily maximum – 80ug
twice daily.
- Children more than 12 years & adults – pts previously on
bronchodilators only.
- Initially 40-60 ug twice daily. Maximum 320 ug twice daily.
- Patients previously on inhaled corticosteroids initial – 40-160
ug twice daily.
Maximum – 302 ug twice daily.

Indication –
- Prevention of episodes of acute asthma.
- Bronchial hyperactivity.
- Acute Exacerbation.
- Chronic Asthma.
- Status Asthmaticus.

*Contraindications–
- Renal failure, diabetes mellitus.
- Psychosis, Hypertension.
- Liver dysfunction
- Pregnancy & lactation

*Side effects –
- Adrenal insufficiency
- Fungal infection
- Oral & Nasal irritation
- Hoarseness of voice
- Sore throat, Hyperglycemia, muscular weakness.

*Adverse effect –
- Cataract, peptic ulceration.
- Obesity of trunk with relatively thin limbs.
- Psychosis
- Or pharyngeal candidiasis.
- Glycosuria
- Fluid & electrolyte Imbalance.
*Drug Interaction –
Interact with carbamazepine, phenytoin & barbiturates &
its efficacy reduces if used concurrently.
- Rifampicin reduces its activity.
- Dose of anti diabetes & antihypertensive needs to be sed.

Role of Nurse – Advise the client to use inhaler before brushing


the teeth to reduce incidence by of mouth infection.
- Monitor for sign of adrenal insufficiency depression, muscle
pain & weakness.
- Before starting therapy assess for prior complications with
steroids.

(4) Mast cell stabilizers –


These are stabilizers are common medications used to
prevent or central certain allergic disorders.
They block a calcium channel essential for most cell
degramilation, stabilizing the cell & so prevent the release of
histamine & related mediators.
One suspected pharmacodynamics mechanism is the blocking
of IgE – regulated calcium channels. Without intracellular
calcium the histamine, vesicles cannot fuse to the cell memb. &
degramulate.
Most cells are found throughout the body including in the
airway in the lungs. Most cell stabilizers prevent the most cells
from releasing the substance that cause inflammation.
*Action – These drugs inhibit the mediators of inflammation. It
thus prevents bronchospasm & inflammation following
exposure to allergies.

(A) Sodium Cromoglycate –


Cromolyn works because it prevents the release of
mediators that would normally attract inflammatory cells &
because it stabilizers the inflammatory cells.
It is more likely that there work by inhibiting the response of
sensory c-fibers to the irritant capsaicin, inhibiting local axon
refers involved in asthma & may inhibit the release of
preformed T-cell cytokines & mediators involved in asthma.

*Dosage –
* Sodium Cromoglycate – 20 mg capsule for aerosol.
* Ketotifen – 1-2 mg BD with.

*Route – Orally & Inhalation.

Indications –
- As a nasal spray to treat allergic rhinitis.
- As an inhaler for preventive management of asthma.
- As eye drops for allergic conjunctivitis.
- In an oral form to treat Mastocytosis, dermatographic
Urticarial & ulcerative colitis.
- Another oral product is used for food allergies.

*Contraindications –
- Diabetes, Hypersensitivity, pregnancy Lactation.
- Prostatic Hypertrophy.
- Motion sickness.
- Meniere’s disease.
- Glaucoma
- Epilepsy.

*Side effects –
- Drowsiness, Dry mouth, dizziness.
- G.I. Disturbance, Headache, Blurred vision.
- Throat irritation with Cough.
- Bronchospasm.

*Adverse effects –
Sedation through CNS stimulate accompanied by
Hallusination, conclusions.

*Drug Interaction –
- Potentiate effects of sedative, hypotics, antihistamines &
alcohol.
- Reversible fall in platelet count with concomitant use of oral
ant diabetics.
- Reverse chloroquine resistance & potentiate action of
sulphadaxine in acute malaria.

*Role of Nurse –
- pt. of asthma must be advised on prevention of the attack.
- Emergency care kit must keep ready for the pts. During change
of season.
- pt. is kept in reclined posture with raised head end or in
fowler’s position.
- pt. is encouraged to cough out secretions as far as possible &
bring out the mucus plug.
- Aminophylline Adrenaline is given.
- Vitals should be taken at short intervals.
- Avoid morphine administer diazepam or chloral hydrate as
these two can be safety used in pts. Suffering from asthma.

Respiratory function can be Improved by Following –


- Establish pt. airway.
- Provide therapy.
- Supply humidified .
- se airway resistance by –
* Removing secretions
* Reducing viscosity of secretions by mucolytic Agents.
* Reducing bronchial secretions by expectorants use.

→ se anxiety of the pts. By:-


* Reassuring them.
* Providing comfortable surrounding.
- Train your pts. To perform breathing exercises.
- Prevent infections.

(5) Anti-IgE Antibody –


Omalizumab –
It is a Monoclonal antibody targeting the high-affixity
receptors binding side on human immunoglobulin E [IgE].
It reduces the severity of exacerbations & reserve
medication use & improve rhinitis – related quality of life.

MOA –
It is an IgE monoclonal antibody [DNA derived] which
inhibit IgE binding to the high affinity IgE receptor on most cells
& basophils.
By sing bound IgE. The activation & release of mediators in the
allergic response (early & late phase is limited).

- Serum free IgE levels & the no. of high affinity IgE receptors
are sed. Long term treatment in pts with allergic asthma
showed a se in asthma exacerbations & corticosteroids usage.

#Pharmacodynamics/kinetics –
- Absorption – Slow following c infection.
- Metabolism – Hepatic, IgG degradation by reticuloendothelial
system & endothelial cells.
- Bioavailability – 62%
- Half life elimination – 26 days.
- Time to peak – 7-8 days.
- Excretion – Primarily via hepatic degradation intact IgG may be
secreted in bite.

*Indications –
Treatment of moderate to severe, persistent allergic asthma
not adequately controlled with inhaled corticosteroid.

*Contraindications –
Hypersensitivity to malizanal or any component of the
formulation & in acute bronchospasm, status asthmatics.

*Adverse effect –
- Headache, fatigue, Diziness.
- Injection site reaction/occurred within 1 hour tested 28 days &
sed in frequency with additional dosing.
- Upper respiratory tract infecton, sinusitis.
- Dermatitis, pruritus.
- Arthralgia, fracture, leg & arm pain.
- Earache.
- Alopecia, anaphylaxis [Angioedema of the throat or tongue,
bronchospasm chest tightness, cough, dyspnea, hypotension,
generalized pruritus, syncope, thrombocytopenia]
- Viral infection.

*pt. education –
- Medication is administered by infection & gov will be closely
monitored for some time at infection site.
- Report immediately any sign of allergic response, breathing
difficulty, swelling of mouth/tongue.
- If allergic response occurs after you have follow prescribers
directions for contacting emergency treatment immediately.
- Inform prescriber if you are or intend to become pregnant
consult prescriber if you are breast feeding.

*Mucolytics –
Mucus is a slippery liquid that is made by glands in the mucous
memb. That line the mouth, nose, throat, lungs breathing
passage way, disgestive urgans & reproductive organs.

Its purpose is to lubricate & protect the organs that is lines.


Normally it is thin, clear & watery. But in certain diseased
condition, mucus is not thin & watery, it becomes thick & sticky.

During normal respiration, air travels through the nose, down


the trachea & into smaller & smaller airway called bronchi. The
living of the respiratory tract is covered with mucous memb.
Which secrete sticky fluid called mucus. Mucus cleans &
protects the air passage by trapping bacteria & debris, mucus
also keeps the air passage moist & lubricated.

Mucolytic drugs help loosen & thin the mucus. Certain


mucolytis agents contain chemical that enhances the bodies
own production an enzyme called Glutathione.

Glutathione helps breakdown thick stic mucus. Once the mucus


is thinned. It is then easier to cough up or suction from airway,
improving the pt’s breathing. Mucolytics drugs can be taken
with a nebulizer or face mask.

Classification –
I Mucolytic –
MOA – Reducing agents destroy disulfide bonds & photolytic
enzymes Hydrolytic peptide bonds & destroys deoxyribonucleic
acid fibers.
Eg:- N. Acetylcysteine
Trypsine
Deoxyribonuclease
II Expect –
MOA – Stimulate gastro pulmonary refer.
Eg:- Gua

III Muco regulator –


After secretory activity of the bronchial mucosa & activate
sialo nucin synthesis.
Eg:- Bromhexine

IV. Hydrizing agents –


MOA – Correct water & electrolyte disorders in secretions.
Eg:- Ammonium chloride water.

MOA – Make secretions less adhesive.


Eg:- Tyloxapol

V. Other Compounds –
Modify fibrillate structures.
Eg:- Eprazinone

#Bromhexine –
It is a mucolytic agent used in the treatment of respiratory
disorder associated with excessive mucus. In addition
bromhexine hase antioxidant properties.
Bromhexine is a synthetic derivative of the herbal active
ingredient vaccine, it has been shown to se the proportion of
serous bronchial secretions, making it more easily to be
exterminated.

Bromhexine ehhances mucus transport by reducing mucus


viscosity & activating the ciliated epithelium.

It is secretolytic & se the production of serous mucus in the


respiratory tract makes the phlegm thinner & less sticky this
contributes to a secretomotoric effect – it helps the cilia [tiny
hairs that lines the respiratory tract] to transport the
phegmtout of the lungs.

*Indications –
- To tract cough with phlegm.
- To acute & chronic disease bronchus & long violation.

*Contraindications –
- Hypersensitivity.
- Sever liver dysfunction.
- Cardiac dysfunction & DM.
Children <6 years, pregnancy & lactation.

*Side effects –
- Hypersensitivity reaction.
- Dryness of mouth.
- Anxiety & dizziness.
- Difficulty in breathing.
- Nervousness & drowsiness.
- Hallucinations, confusion & slow breathing.
- Headache &restlessness.
- Vomiting & Anorexia.

Dosage –
Adults 8mg TDS.
Children 1-5 year – 4 mg BD
5–10 year = 4 mg TDS

*Nursing responsibilities –
- Determine current medication & allergies.
- Usually given with – bronchodilators [bronchospasm]
- Prepared for suction if cough is ineffective.
- Rinse mouth after every therapy to avoid or pharyngeal
irritation.
- Discard unused medications after 4 days.
- sed fluid intake to thin secretions.
- Teach client to avoid smoking as this ses secretions & ses
ciliary action.

*Ambroxol –
It is a metabolite of bromhexine. Tit is more potent than
bromhexine & commonly used as mucolytic drugs to desolve
the mucus from respiratory passage.
- It works to se mucus viscosity by altering it’s structure.
- Ambroxol is a clinically proven systematically. Onset of action
occur after about 30 minutes.

MOA – It is a mucoactive drug with several properties including


secretion & secretomotoric sections. It restore the physiological
clearance mechanism of the respiratory tract, which play
important role in the body’s natural defense mechanism.

It stimulates synthesis & release of surface and by type 2


pneumocystis surfactant is reducing the adhesion of mucus to
the bronchial wall, in improving it’s transport & in providing
protection against bacterial aggression & irritating agents.

Secretolytic therapy in broncho pulmonary disease associated


with abnormal mucus secretion & impaired mucus transport. It
premotes mucus clearance facilitates expectorant & case
productive cough. Allowing pts to breathe freely & deeply it
concert into bromhexine in the body & act on the respiratory
tract to develop mucus cumulated in it.

Indications –
i) Bronchial asthma
ii) Chronic Bronchitis

Dosage –
For adult – 15-30mg orally 8 hourly. For children – 5-10 orally
8 hourly.
*Contraindication –
In pts. With gastric ulceration & caution should be observed.

→ Adverse effects –
- Allergic reaction – Skin rash, edema, dermatitis & anaphylactic
shock.
- Headache, diarrhea, dry mouth, dysuria, exanthema.
- Nausea, vomiting gastralgia.
- shortness of breath.

*NSG responsibilities –
- Check for the condition such as pregnancy & allergy.
- Check vital signs frequently.
- Check for vomiting, drowsiness, nausea & manage them.
- Maintain potency airway if it faces bronches constrictions & be
prepared with articles of administration.
- Prepared with suction articles in case of ineffective cough.

*Nasal Decongestants –
Most of these drugs stimulate alpha adrenergic receptors of
respiratory mucus to produce vasoconstriction that leads to
chrinkage of swollen nasal mucous & reduction of tissue
hyperemia, & nasal congestion leads to in airway potency &
opening of obstructed Eustachitis.
Decongestants relieve nasal stuffiness by shrinkage swollen
nasal mucosa memb.

Adrenergic agents [Sympathomimetic] do this by


vasoconstriction, sing block flow to the nasal mucosa &
thereby reducing swelling.

Nasal steroids act as anti-inflammatory agent by suppressing


the inflammatory response.
Indications –
i) Nasal & Eustachian tube congestion.
ii) Nasal stuffiness.
iii) Acute or chronic rhinitis.
iv) Sinusitis hay fever & other allergic conditions.
v) To se local blood flow before nasal surgery.
vi) Before nasal diagnostic examination to improve visualization.

Name of Drug Dose Side effects


- Phenylephrine 2-3 spray or drops - Irritation of
in each month 3-4 mucosa
hour - Dryness of nasal
mucosa
- Nervousness
- Pseudoephedrine 60 mg 4-6 hour - Insomnia
- Tremors
- Palpitations
- Ephedrine One spray in each - Nervousness
month a 3-4 month - Dizziness,
BD confusion
- Oxymetazoline 2 to 3 spray or - Insomnia, muscle
drops in each tremor
month BD - Nausea, vomiting
- Tetrahydrozoline 2-4 drops in each - Appetite less
nostrils a 3-4 hour - Urinary retention
3 to 3 sprays or
drops in each nose a
6-10 hr.

*Contraindications –
1) Severe hypertension.
2) Coronary artery disease
3) Narrow angle glaucoma
4) Nasal steroids are contraindicated in nasal mucosal infection.
5) Pregnancy & lactation.
6) Person taking tricyclic anti-depressant or MOA inhibitors.
7) Use caution only in client with cardiad Dysrhythmias,
hyperthyroidism, DM, prostatic hypertrophy & insomnia.

*NSG responsibilities –
- Assess client for other medical history to determine potential
for possible side effects.
- Older adults with significant cardiac disease should avoid nasal
decongestant because they are at high risk for hypertension,
Dysrhythmias, nervousness & insomnia.
- For administration of nasal drops, have client lie down or sit
with neck hypertension to install the medication. Medication
dropper should be washed after each use to prevent
contamination.
- Observe client for ses in nasal congestion.
- Observe for tachycardia hypertension & cardiac Dysrhythmias
also observe for rebound congestion, rhinitis & ulceration of
nasal mucosa.
- Note characteristics of nasal discharge, amount color &
consistency.
- Anti-hypertensive medications can have sed effectivenss
when administered with decongestants.
- Observe pt. for complications of headache or dizziness
monitor blood pressure.
- With parenteral dosing, monitor vital signs closely during
infusion, tachycardia is very common.

*Pt. education –
- Blow the nose before installation of nasal decongestants
drugs.
- Do not use nasal decongestant more frequently then
recommended.
- Smoking should be avoided as this ses ciliary action & se
secretion.
- Eating & drinking should be avoided after the administration
of topical medications.
- Do not use alcohol or other CNS depressant.
- Avoid use of caffeine.
- Practice good hand washing.
- Rinse dropper & spray battle after each use to avoid
contamination.

#Expectorants –
These are the drug which ses fluid flow in the respiratory
tract & reduce viscosity of secretion to aid in removal of
secretion by cough reflex & ciliary action.

The purpose of using expectorants is to make cough more


productive so that mucosa will be cleared from the airway.

*Types of Expectorants –
1. Direct Expectorant:-
Direct expectorants are those which ses the respiratory
secretions by directly acting on it’s mucosa.
Eg: Eucalyptus oil, lemon oil, sodium citrate, potassium citrate
etc.
Reflex Expectorants:-
They are usually emetic substances which are used in sub
emetics closes.
They produces little irritation of the gastric mucosa &
stimulate the gastric secretions & pharyngeal secretions. They
also stimulate other respiratory secretions & at used as
expectorant.
Eg:- Ammonium chloride, Ammonium Bicarbonate potassium
iodide, Tincture of ipecac.

#Indications –
- Non productive cough associated with common cold,
bronchitis laryngitis influenza.
- Dry irritating cough.
- Productive cough.

#Contraindications –
i) Hypersensitivity.
ii) High fever.
iii) Rashes
iv) Prolonged headache
v) Dizziness
vi) Nausea vomiting

Common Drugs –
Drug Dose Side effects
200-400 mg q 4 h - Dizziness,
oral half fir children headache,
- Nausea, vomiting
300-650 mg BD/IDS - Diarrhea
after meal - Stomach pain.
- Terpin Hydrate 85-170 mg tid/qid - Rash
- Urticarial

*NSG responsibilities –
- Assess lung sound note the frequency & type of cough &
documents the characteristics of expectorated secretions.
- To help the thin secretions, encourage fluid intake of 1500-
2000 ml/day unless contraindicated.
- Do not use guaifenesin for more than 1 week if cough is
persistent & do not administer to pt. with high fever rashes &
headache.
- Drugs should be taken with a glass of water to help loosen the
mucus in lungs.
- Instruct the pt. to call if cough persist for more than 1 week.
- Advise pt. to use a humidifier to filler out dust, smoke & air
pollution.
- Advise pt. to use sugarless throat lozeges to ses throat
irritation & associated cough that persist longer than 1 week.
- Encourage client to perform deep breathing exercises.

*Pt. education –
- Take medications exactly as prescribed.
- Be aware of potential side effects.
- Follow each dose of guaifenesin with full glass of water.
- Do not use alcohol or other CNS depressant while taking this
medications.
- Report a fever or cough to physician if it last longer than a
week.
- Avoid smoking as these se secretions & ses ciliary action.
- Take potassium iodide preparations with fruits or milk to
decrease the bitter taste.

*Antitussives –
Antitussive ate drugs used to relieve cough by suppressing
the cough center in the medulla. Coughing usually caused by
irritation of bronchial mucosa.

Coughing is a protective mechanism in that it helps to remove


foreign matter & excessive secretions from the airway.

Antitussive are drugs used to control or bring relief from cough.


They are used to treat dry non productive cough, which is
painful, these agetns used in antitussive effect the cough reflex.
Both narcotics & non-narcotics preparations are used. Some of
the drugs contain antihistamine & Sympathomimetic agents in
addition to the antitussive.

These drugs mainly act in CNS to raise the threshold of cough


cater or act peripherally in the respiratory tract to reduce torsol
impulse is both these actions.
MOA – opioid & non-opioid antitussive suppress the cough
reflex by direct affecting the cough center, non-opioid
antitussive do this without the CNS suppress of the opioid
antitussive.

Peripherally acting agents [Glycerin, ammonium chloride] have


local anesthetic effect to se irritation of the pharyngeal
mucosa they are available in gargles, lozenges & group,
lozenges se saliva flow & therefore suppress the cough.
*Indications –
- Used to stop a non-productive cough or a dry hacking.
- Non-productive cough after interfere with rest & sleep.

*Classification of Antitussives –
1. Opioids – Codeine, Pholcodine, Ethylmorphine, Morphine.
2. Non-opioids – Dextromethorphan, Nosacapine,
chlophedianol.

I. Opioids –
Drugs derived from the juice of the opium poppy [papaver
somniferum] are termed opiates. The term opioids have been
coined to designated both opiates & their synthetic substitute.

(A) Codeine:- Codeine is more selective for cough center & is


treated as the standard antitussive, suppresses cough for about
6 hours.

MOM –
Codeine acts on U-receptor in medulla oblongate.
Inhibits release of excitatory neuropepticks

Suppress cough
#Indications –
* Non-productive cough.
* Complications of ribs.

#Contraindications –
* Pre-existing respiratory depression
* Asthma
* High intracranial pressure.
# Adverse effects –
- Dry mouth, Aorexia, constipation.
- Biliary spasm, Delirium , Disorientation.
- Weakness, Insomnia, Anxiety, Headache.
- Syncope, Mood changes, Hallucination Fantness.
- Respiratory & CV depression.

Dosage –
Available in lozenges syrup/tablet.
- Adult: 10-20 mg every 4-6 hr. maximum 120mg/day.
- Children 6-12 years – 5-10 mg every 4-6 hourly maximum
60mg/day.
- children 2-6 years – 2.5-5mg every 4-6h maximum 30mg.

Codeine 15mg tablets, 15mg/5ml linctus

*NSG Responsibilities –
- Inform pt. that he/she may feel restlessness anxiety or
nervousness, specially on large dose.
- Suggest the pt. drink large amount of studio 2/day may help to
loose the tenacity of bronchial secretions & to use a humidifier
or vaporizer during the night.
- Advise pt’s to use hard candy, gum or throat lozenges to sooth
pharyngeal mucosa irritated by constant coughing.
- Note that codeine alone in tablet form is a schedule, when
used in syrup/form. Administer medications undirected & do
not immediately follow with water.

II Non-opioids – Non-opioids are the drugs that interact with


opioid receptor in the CNS produce antagonistic effect a these
sites. As they displace the effect of opioid molecules from the
acceptor site. So they are termed as opioid antagonist.

Indications –
1) Opioid toxicity.
2) In new term whole mothers received opioids.
3) Opioid dependence.

A) Dextromethorpha –
A widely used non-narcotic antitussive, dextromethorphan
has minimal CNS depressant action & no analgesic effect. It is
administer is unlikely to produce constipation or result
intolerance. It is commonly found in OTC cough histaminic
decongestant & expectorants 30mg dose is approximately
equivalent to 15mg of codeine.
MOA –
It is synthetic compound which raises the threshold of cough
center & is equipotent to codeine.
Indication – Temporary relief of nonproductive coughing.

*Contraindications –
Pt. taking MAO

*Side effects – Dizziness Nausea, drowsiness, ataxia.

*Dosage – lozenges & syrup


* Adult 10 – 30 mg every 4 – 8 hours [120mg/24hr]
*Children 6 – 12 years – 2.5 – 5mg every
4 hours (60mg 124 hours)
* 2–6 years – 1.25 – 2.5 mg every hourly [30 mg 124 hourly]
Nursing alert –
Use caution in pt’s with COPD, high fever, persistent
headache, vomiting & where coughing is accompanied by
excessive secretions.

*Nsg responsibilities –
- Administer syrup undiluted to enhance it’s local effect.
- Do not administer to children under 2 years of age except
under the medical supervision.
- Adjust pt. to consult physician if coughing persistent longer
than 7 days dextromethorphan o any other antitussive therapy.
- Note that dextro is available is lonzenrs from alone & or
combined benzocaine for central of spasmodic coughing.
*Bronchoconstrictors –
The two major classes of receptor proteins are designed
alpha & beta-adrenergic receptors. Each adrenergic receptor
have two major subtype these are alpha 1 & alpha 2, & beta 1 &
beta 2. Compounds have been developed that selectively bind
to one or other type of ordinary receptor & by this means either
promot or inhibit the normal action produced when
epinephrine & nor epinephrine binds to the receptor. As a result
of its binding to an adrenergic receptor, a drug may either
promotes or inhibit the adrenergic effect.
Non-selectively B-adrenergic antagonists such as propranolol
block beta – 2 adrenergic receptors in bronchial smooth
muscles. This usually has little effect on pulmonary function in
normal individuals however, in pt’s with asthma or COPD such
blockage can lead of life threatening bronchoconstriction.

These block beta 2 receptors, which are located in the


bronchials of the lungs, this reducing bronchodilator & produces
broncho constriction & asthma in susceptible people.

Drugs –
1) Propranolol
2) Nadolol
3) Pinctolol
4) Sotadolo
5) Timelol

1) Propranolol –
It is a non-selective beta-blocker which block the action of
epimephrine on both beta 1 & beta 2 adrenergic receptors.

MOA –
It is rapidly & completely absorbed with peak plasma levels
achieved approximately 1-3 hours after ingestion.
It diminishes cardia output, having both negative inotropic &
chronographic effects.

Blocking B-receptors in the lungs of susceptible pt. cause


constriction of the bronchiolar smooth muscles this can
precipitate a respiratory crisis pt. with COPD or asthma.

*Indication –
- Hypertension, Angina pectoris, Myocardia infection,
Tachyrrhythmias, Migrain prophylaxis, Teralogy of Fallot, post
traumatic stress disorder.

*Contraindications –
1) Reversible airway diseases, particularly asthma or COPD.
2) Bradycardia.
3) Sick sinus syndrome.
4) Atrioventricular block.
5) Shock
6) Severe hypotension.
7) Uncontrolled congestion heart failure.
8) cocaine toxicity.

*Side effects –
i) Bronchoconstriction
ii) Arrhythmias
iii) Sexual impairment
iv) Disturbance in metabolism
v) Drug interactions.

Dose –
- Orally 10-19mg
- IV – At a conn in sustained release capsule 80, 120, 160 mg.

#Anti Histamines –
Histamine is an import chemical mediator that is stored in
most cell located in almost all body tissue.
Histamine is released in response to antigen for which a person
has developed antibodies.
- The effect of histamine includes:-
* Contraction of smooth muscle in the bronchi GI tract & uterus.
* Vasodilation & increased capillary permeability [edema]
* Increase secretion of gastric juice also increased bronchial,
intestinal & salivary secretion.
* Pain & itching caused by sensory nerve stimulation.
→ Anti-histamine prevents the effect of histamine by occupying
the histamine receptors. There are types of histamines
receptors.
1. Receptors – Are those associated with the smooth muscle
of the blood vessels bronchioles, GI tract.
2. Receptors – are those found on gastric parietal cells, the
myocardium & certain blood vessels.
MOA –
- Smooth muscles – Antagonist effective inhibits the
response of smooth muscles to histamine. In the vascular
smooth muscles, the antagonist inhibits the vasoconstrictor
effect of histamine includes the large blood vessels.

- Capillary permeability – antagonist blocks the action of


histamine, which leads to increase leakage of plasma.
- Nerve endings – antagonist effectively blocks the action of
histamine on nerve endings which cause itching and flare.
- Anaphylaxis & allergy –
Many manifestations of types – 1 [Immediate]
hypersensitivity rex. like urticaria, pruritis & angioedema are
well controlled.

Name of Drug Dose Route Uses


- Azatadine 1-2 mg Oral Allergic disorder
- Carbocamine Adults 4-8 mg Oral Allergic disorder
children 2-6 mg
4 mg Oral IV Allergic disorders
Adults 2 mg Oral Allergic disorders
Anaphylastic
reaction
Allergic dis.
Adults 25-100 mg Oral Pediatric sedation
Child-25-50 mg IV deep Im Insomnia cough &
cold allergic dis.
Adults 25-50 mg Oral Allergic dis.
Child – 5mg/kg/day IV
25 mg Oral Allergic dis.
12.5-50mg Oral Nause, vomiting &
cough
10mg Oral Allergic, Rhinitis
urticaria
10-20 mg Oral Seasonal allergies
150-250 mg Oral Allergic rhinitis

*Indications –
Allergic disorders, Allergic rhinitis, common cold, Insect
bites, drug reaction, anaphylactic reaction. Insomnia, allergic
cough, urticaria, pruritis, nausea & vomiting.

*Also use to prevent –


- Motion sickness –
- Allergic reaction to transfusion of blood or blood products.

#Contradictions –
Narrow angle glaucoma prostatic hypertrophy, bladder
neck obstruction, peptic ulcers, asthma, pregnant woman,
jaundice, bone marrow depression.

#Side effects –
Sedation, Dizziness, Epigastria distress, dryness of mouth,
thickened bronchial secretions.

*Adverse effects –
*Cardiovascular – Hypotension, palpitation, Tachycardia,
Arrhythmia.
*Respiratory – Wheezing, chest tightness, nasal congestion.
*Gastrointestinal – Anorexia, Diarrhoea, Constipation.
*Urinary – Urinary frequency, Dysuria.
* CNS – Confusion, restlessness, vertigo, Impaired co-
ordination, Heaviness, weakness of hands Tremors, Insomnia,
Excetection.

Hypersensitivity – Drug rash, Anaphylactic shock.


- Other – Headache, sweating, pailer, burning at sited injection.
Overdose may cause fever, hallucinations & convulsion &
respiratory collapse.

*Precautions –
- First generation anthihistemines taken with other CNS
depressants can cause excessive sedation.
- Some antibiotics enhances the effect of laratodine.
- Anti-histamine not recommended in bronchitis or pneumonia
because they dry secretions making them more difficult to
remove.

*NSG responsibilities –
- Monitor for therapeutic & adverse affects.
- Administer IV slowly to prevent severe hypotension.
- Give oral antihistamine with food to se GI distress.
- Caution the client about drowsiness & institate safety
precautions.
- Assess for urinary retention.
- Document stools & encourage extra fluids & fiber to prevent
constipation.
- Administer medications at bedtime to with the side effects of
drowsiness.
- Administer IM anthihistamine deeply into large muscles.
- IV inj. Should be over a few minutes.

*pt. educations –
- Take medications exact as prescribed.
- Teach client potential side effects.
- Teach client action of the medication & potential drug
interaction.
- Do not take more than one medication at a time.
- Do not operate heavy machinery or participate in other
hazardous activities while taking this type of medication.
- Do not use alcohol or other CNS depressants while taking this
type of medication.
- Use hard sugarless candy to relive dry mouth.
Unit – 06

Drugs used in urinary system

Diuretics :-

These are drugs which cause a net loss of Na + & water in urine. There are several categories of diuretics. All diuretics
se the excretion of water from body.

The diuretics act by inhibiting tubular reabsorption just 1 % se in tubular reabsorption would more than double urine
output.
Classification :-

1. High efficacy diretics :-

Full semide, bumetanide, piretanide, ethaerynic acid, tarsemide, azosemide,

2. Moderate efficacy diuretics :-


a. Thiazides :-
. benzothiadiazines chlorothiozide
. hydrochlorothiazide
. polythiazide
. benaroflumethiazide
. cyelopnthiazide
b. Thiazide related agents :-
. chlorthalidone
. clopamide
. indapamide
. metolazone
. xipamide
3. Low efficacy diuretics :-
a. Potassium sparing diuretics –
. triamterene
. aniloride
. spironolactene
b. Carkonic anhydrase inhibitors
. acetazolamide
. methazolamide
. darzolamide.
c. Osmotic diuretics :-
. mannital
. urea
. glyeerol
d. Methylxanthines –
. theophylline
1. High efficacy diuretics :-

Drug names – frusemide, bumetanide, piretanide, ethalrynic acid, torsemide, azosemide.


MOA :-

Frusemide acts by inhibiting NaCl reabsorption in the thick ascending limb of the henle’s loop. It blocks the Na +, K+,
Cl- symporter in the thick ascending limb of the henel’s loop because of which it is called is a loopdiuretics. It greatly
se the excretion of Na+ & Cl- in the urine. As a large amount of NaCl is absorbed in this segment, loop diuretics are
highly efficacious. Diuretics response ses the with dose ← overenthusiastic treatment can cause dehydration.
Other action :-

Loop diuretics also enhance the excretion of K+ , Ca+2 & Mg+2 [but Ca+2 is reabsorbed in the distal tubule – hence no
hypocalemia].
They se reabsorption of uric acid in the proximal tubule

On long – term use, they also after renal homodyamics to reduce fluidselectrelgte, reabsorption in the proximal tubule;
loop diuretics enhance rennin relesae.

Frusemide is also a weak carbonic anhydrase inhibitor hence it ses the excretion of HCO- 3 & phosphate

IV frusemide causes vesodilation 4 reduces left ventricular filling presute. It thus relieves pulmonary congestion in
congestive heart failure (CH) & in pulmonary edema even before the onset of diuresis.
Dosage :-

1. Fcrosemide [lasix] :- 20 – 80mg / day, 20 – 40 mg upto 600 mg / day [oral/ IM]


2. Torsemide :- 2.5 – 5 mg / day sed to 10 mg / day 4 – 6 weeks [oral]
3. Bumetanide :- 1 mg IV loading dose then o.5 – 2 mg / day po divided q / 2h [IV, oral]
Indications :-

Acute CHF, acute pulmonary edema, edema associated with CHF, edema renal & liver disease, hypertemion acute,
renal failure, cerebral edema, acute hypoglycemia & hyperkolmia.
Contraindications :-

. anuria

. severe renal failure

. hepatic

. pregnancy & lactation

Side effects :-

. hypersensitivity reaction

. Hypotension

. ECH changes

. hypokalenia

. cardiae disturbance.

. metabolic alkalosis

. hyponatremia

. blurred vision
NSh responsibilities :-

- Administer drug during day time to avoid sleep disturbance.


- Do not anix parentral solution with highly acidic solutions with PH below 3.5.
- Menitor serum electrolytes, hydration liver & renal function periodicall.
- Administer potascium rich diet to pt.
Pt. education :-

Instruct pt. to weight regularly.

Instruct pt. eat potassium rich diet.

Aduise pt. avoid taking drug at bedtime.


2. Moderated efficacy diuretics :-

Drug :-

Thozides; Benzothiadiazines – chlorothiazide, hydrochlorathiazide, bendrofluemethiazide, polythiazide,


cyclopenthiazide.

Thiazide related agents : chlorthalidone, clopamide, metalazone, xiponicide.


MOA:-

Thiazides act on the early distal tubule, thiazides have a moderate efficacy because 90 % of the filtered sodium is
already reabsorbed before reaching the distal tubule. This group of drugs black Na + / Cl- contrasport system in the early
distal tubule. They also inhibit carbonic anhydrance activity & se bicarbonate loss.

Thiazides also enhance excretion of mg+2 & K+ but they inhibit urinary excretion of Ca +2& hyperuricemia.

[Link]. Name of drug Dose Route


1. Hydrochlorethiazide Adult – 25 – 100 mg / day Oral
2. Chlorothiazide Adult – 0.5- 1 mg [10 – 20 mg / day] Oral / I V
3. Metolazone 5 – 10 mg / day Oral / I V
4. Xipomide 20 – 40 mg / day max. 80 mg / day Oral / I V
5. Indopamide 2.5 -5 mg / day Oral / I V
6. Clopamide 10 – 60 mg / day Oral / I V

Indications

- Edema
- Hypertension
- Diabetes insipidus
- Hypercaleiurea
- Liver ciruhosis
Contraindications :-

- Allergy to thiazides
- Sulfonamides; fluid or electrolyte imbalavie
- Renal disease & liver disease & anuria.
Adverse effect :-

CNS :- dizziness, vertigo, paroestheisa, weakness, headache, drowsiness & fatigue.

CV :- arthostatic gypotension, venous thronkosis, volume depeletion cardiae arrhymias, chestpain,

Dermatilogic :- photosensitivity, rash, purpurl exfoliative dermatitis, hives & alopeila.

GI :- nausea, vomiting, anoreria, druynous hepatitis & panereatitis.

Genitourinary :- polyuria, nocturia, loss aflibide & impotence.

Hematologic :- zeukopenia, thrombocytopenia, agronulocytosis, aplastic anemia, neutropenia.

Other :- muscle cramps, muscle spasms, fever gouty attacks, fluching, wt. loss, rhinorrhea, electrolye imbalances,
hyperglycemia.
NSG responsibilities :-

 Give with food or milk if GI upset occurs.


 Mark calendars or provide other reminders of drug for alternate day or 3 – 5 days / weak therapy
 Reduce dosage of other antihypertensives by at least 50 % if given with thiazides; readjust dosages gradually s BP
responds.
 Administer early in the day so se vrination will not distuble sleep.
 Measure & record weights to monitor fluid changes.
Low efficacy diuretics :

A. Potassium sparing diuretics :-

Triameterene, aniloride & spironolaetone.


MOA :-

Potassium sparing diuretics act as oldesterne antagonist by reduce Na + reabsorption & reduce. K+ secretion in the distal
part of the nephron [ collecting tubules ]
These are not potent diuretics when used alone, they are primarily used in combination with other diuretics. It inhances
the exoretion of calcium by a direct action on the renal tubules.
Does :-

1. Spironolactione :- adult – 25 – 100 mg / qdn [oral] single / divided dose.


2. Trianterenc :- child – 5 – mg qd, may be se to 10 – 20 mg qD [oral]
Adult – 100 mg [ no exceed 300 mg / day ] [oral]
3. Amitoride :- adult – 5 - 10 mg / day oq day or divided q / ah. [oral]
Indications :-

Diagnosis & maintenance of primary hyperaldosternism.

Adjunctive therapy in edema associclted with CHF nephritic syndrome, hepatic cirrhosis when other therapies are
inadequate or inappropriate.

Treatment of hypokalemia orprevention of hypakalemia in pts who would be at high risk if hypokalemia occurred –
digitalized pt. pts with cardiae arrhythmias.

Essential hypertension , usually in combination with other days.


Contraindications :-

- Allergy
- Alyperkolemia
- Renal disease
- Anuria
- Use cautinaly with pregnancy & lactation.
Adverse effect :-

- Dizziness, headache, drowsiness fatigue, atoxia confusion.


- Rushs, urticaria,
- Cramping, diarrhea, dry mouth, thrist comiting impotence irregular menses, cumenorrhea, postmenapaused
bleeding
- Hyperkalemia, hyponatremia, agranulocytsis
- Hirsutism, gynecomasits,
NSG responsibilities :-

Give daily doses early so that se urination does not interpare with sleep.

Make suspension in as follows, tablets may be pulverized & given in cherry syrup for young children.

This suspension in stable for 1 month if refrigerated.


Measure & record regular wt. monitor mobilization of edema fluid.

Avoid giving food rich in potassium.

Mark calendars of edema outpatiens as reminders of alteroute day or 3 – 5 day / week therapy.
Pt. education :-

Advise pt. to take the drug early became of se urination.

Advise pt. to wt. yourself on a regular basis, at the some time in the some colotting & record the wt. on your calendar.

Instruct pt. to avoid foods that are rich n potassium.

Advise pt. that if she / he experience any type of side effect & adverse effect should contact with given & physicion

Advice pt. to repost wt. change of more than 3 pounds in 1 day.


B. Carbonic anhydroze inhibitors :-

Drug :- acetazalamide, methzolamide, dorzolamide.

MOA :-

Carbonic anhydraze is an enzyme theory catalyzes the formation of corbenic acid which spontaneously ionizes to H + &
CO3- this HCO3- combines with Na & is reabsior.

Carbonic anhydrose inhibitors block Na bicarbonate rebsorption & cause HNO3- diversion.

Carbonic anhydrase is present in the nephron eyes, gastric mueosa, pancreas & other sifes.
Dose :-

Acetazolamide - 250 mg – oral

It is sulfonamide derivate which is a carbonic anhyrase inhibitors & enhances those cretion of Na+ , K+ , HCO3- &
WATER . the loss of bicarbonate leads to metabolic acidosis.

Acetazolamide is well absorbed orally & excreted unchanged in urine, action of single dose. 8 -12 hours.
Indication –

Glaueoma, tolkaline urine, epilepsy, acute mountain sikneus, periodic paralysis, hyperphosphatemia.
Adverse effect :-

Acidosis, hypokalmia, drousiness, paresthesia, fatigue, abdominal diseomfort

Hypersenlitivity Hex4
NSG responsibilities :-

Check electrolytes level periodically.

Check vital sings regularly.

Check wt. of pt. daily.

Check for the siqns of inetabolic acidosis.


C. Osmotic diuretics :-

Monintol :-

it is a pharmacologically inert substances. When given IV [ orally] net absorbed. Mannitol get filtered by the
glomerulus, but not reabsorbed.

It causes water to be retained in the proximal tubule & descending limbol hemle’s loop by osmatic effect resulting in
water diveresis. There is also some loss of sodium.

Dose :-

I V as – 10 % , 20 % in 100, 350 and 500 ml vaccum. ]


Indication :-

se intracranial or interaocular tension [ acute congestive glaucoma, need injury, stroke]

Acute renal failure to maintain flomerula filtration rate.

To countered low asmolarity of plamal ECF due to hemodialysis or peritoneal dialysis.


Adverse effects :-

Dehydration, ECF volume expansion headache & allergic rex4.


NSG responsibilities :-

Assus electrolytes level periodically.

Check vital sings regularly

Check wt. of pt. daily

Administer the drug at faster speed until & unless it is contraindicated.

Drug → isosorbide & glycerol :-


These are orally active osmolytic diuretics, which may be used to reduce intra – ocular orintra cronial tesion. IV
glycerol cam cause hemolysis.
D. Methyloxanthines :-

Theophylline have mild diuertic effect.


Anti diuretics :-

Anti – diuretics [ inhibit the water excretion without affecting salt excretion ] are drugs that reduces urine volume
particularly in diabetic insipidus.
Classification :-

a. Antidivretic hormone [ADH] :- vasopressin, desmopressin, lyprpssin


b. Terlipressin.
c. Thiozide diuretics – aniloride
d. Miscellaneous – indomethacin, chlorpropanic carbamozepine
1. Antidiuretic hormone :-

ADH secreted by the pdsterior pituitary along with orytocin. It is synthesized in the supro optic & poraventricular
nueleie of the bypothalamus, transported along the hypothalamo – hypophyseal treact to the posterior & is stored there.

ADH is released in response to two stimuli dhydration & size in plasma osmolarity.
MOA :-

Antidiuretic hormance enhaces water reabsorption by acting on the collecting duct. ADH activates the V2 receptor
present on the cell memb. Of the collecting duct & se the water permeability of these cells. ADH causes
vasoconstriction & raise BP mediated by receptor. It also acts on other smooth muscles to se peristalsis in the gut &
contracts the uterus. Vasopressin is given parenterlly as injection – subeataneous IM/IV.
Does :-

a. Lypresin :- inj. 20 Iv/ ml, 10 IV IM or SC 20 IV diluted in 100 – 200 ml of dextrose. Solution & infused IV in 10 –
20
b. Terlipresin :- 2 mg repeat 1 – 2 mg every 4 – 6 h.
c. Demopressin :- IV/SC - 2.4 mg / day
oral – 0.1 – 0.2 mg/TDS
ivdronasal – adult – 10 – 40 mg/ day in 2 – 5 divided doses, children 5 -10 mg / day at bed time.
Indications :-

Diabetes insipidus of pituitary origin :-

Desmopressin in the preparation used. It should be used lifelong.


Bleeding esophageal varices :- ADH contracts mesenteric blood vessles CV receptor & may help anlogs like
desmopressin, terlipressin & lypresssin can be used.

Before abdominal radiography :- expels gas from the bowel.

Hemophilia & van willebrond’s disease :- may release factor VIII & prevent bteedi
Contraindications :-

Individuals suffering from vascular disease

Especially disease of coronary artories .


Adverse effect :-

when used interansally ADH cause nasu irritation allergy, rhivitis atrophy of nasal mucosa.

Other effects include nasue abdominal cromps & backache [due to constriction of the uterus.
NSG responsibilities :-

Monitor 24 output of the it.

The ADH therapy is lifelong required like in dc.

Assess any nasal irritation, atrophy of nasal musoa in local application


Thiazide diuretics :-

Diuretics thiazide para doxically exert an antidiuretic effect in DI. High ceiling diuretics are also effective but are less
desirable because of their short & action
MOA :-

Diuretics thiazide paradoxically exert on antidivertic effect in DI. Thiazide reduce, urine volume in both pituitary origin
as well bolume in both pituitary origin as well as renal by an unkown mechanism.
Indication :-

Diabetes insipidus

Nehrogenic (DI)

Mobilization of edema fluid.


Dosage :-

Hydrochlorothazide 50 – 150 mg in daily divided dose


Contraindications :-
Hypokalemia, hypersensitivity

Penal purdoing impairment.


Side effects :-

Depletion of K+, inhibition of insulin secretion, risk of otherosclerosis, hyperglycemia.


NSG responsibilities :-

Monitor I/O chart serum electrolyte & BP

Assess for effects of hypokalmia

Moderate restriction of Na+, Cl- intake has been show to enhance the avtidioetic effect

Monitor he client for hyperglyeemia.


Miscellaneous :-

A. Chlorpropamide :-

Chlorpropamide has a long duration of action oral hypo glycemic found to reduce urine volume in DI of pituitary origin
but not is renal DI, it sensitize the kidney the ADH action its efficacy depends on small amount of the circulating home
one it is not active when ADH is totally absent. It also directly prene salt reabsorption in the ascending limb c may
contribute to its antidiuretic action.
MOA :-

The principle action is B – cells of islets stimulate insulin secretion, reducivg plasma glucose one.
Does :-

Initially 250 mg / day [ 100 – 125 mg / day in eld pt.]


Indications :- to lower blood glucose level.

Contraindications :-

Mild renal impairment liver dysfunction, fever, infection / trauma.


Side effects :-

hypoglycemia, nausea, vomifing diarrhea, constipation, headache, het, gain, cholestatic jaundice, dilutional
hyponatremia iutolernce to alcohol.
NSG Responsibilities :-

Carefully observe the pt. for sings of hypos glycemia.


Pt. should be taught the cause of hypoglycemia reaction & how to avoid having excessive response to oral
hypoghlycemia drug .

Watch for sign of hyperglycemia & ketoacidosis

Pt. should learn not to skip planned meals or snacks.


B. Carbamazepine :-

it is an antiepileptic antiemuulsant drug which reduces urine volume in DI of pituitary origin.

It has been show to stimulate ADH secretion however. It is not voluable in the treatment of DI.
MOA :-

It has a stabilizing influence on neuronal membrane. It can inhibit voltage dependents Nd + channel.

Probably of greater importance is its ability to facilitate Na+ extrusion from nerve cells & to prevent intracellular
acumens action of this cation during repetitive stimulation. Thus it selectively inhibits high frequency discharge which
little effect on ward neuronal discharge.

Influence of Ca+2 during depolarization is also used.


Indications :-

Partial & generalized epileptic seicres.

Preventing pain of trigeminal neuralgia.


Doses :-

On the Ist day of epilepsy treatment a total dose of 200 mg is administered for trigeminal neuralgia the uneidl dose is 100
mg.
Contraindication :- liverdayspemetion

Side effects :-

Adation, dizziness, vertigo, ataxia, diplopia.

Hypersensitivity rexn

Water retention & hyponatremia

Hepatitis

Vaniting, diarrhea.

Acute intoxication cause coma, convulsions.


NSG Responsibilities :-

Treatment is started with, a single durgs selected for its known effectiveness in controlling the kind of seizures.

Small doses are administered first & dosage is gradually reused at intervals of 5 -7 days, until the pt. is seizures are
controlled.

If the drug is effective, but causes minor signs & symptoms of over dosage, its dose is slowed redveed to a level that the
pt. can tolerate.

Also instruct the pt. never discontinue drug abrupty.

Pay attention to the pt’s emotional needs & make. Sure that he understands the nature of his / her illness.
Urinary antiseptics :-

Urinary antiseptics are substances, white prevent bacterial infection in urinary tract.

They cannot be used to treat systemic infections because effective conn are not achieved in plasma with safe doses.

Further more, effective antibacterial con’s reach the renal peluis & bladder. Treatment with such drugs can be though of
as local therapy only in the kidney & bladder. Their wefulness is limited to lower urinary tract infections.
1. Methenamine :-

methenamine is a urinary antibacterial agent whose action & formal dehyde in an urine, methenamine is most often used
in the form of an acide salt [ hippurate, modulate] which helps to maintain a low urinary PH.
MOA :-

In an acidic urine [ PH 5.5 / lower]

Drug hydrolyzed to form ammonia & formaldehyde

Later being bactericidal

Acid liberated from salt

Exert weak antibacterial action


Indications :-
Treatment of chronic bacteiuria associated with cystitis pyelonephritis.

Prophylaxis before urinary instrumentation

Adjunctive treatment of pts with anatomic abnormalities of urinary tract.


Doses :-

Methenamine →tab 0.5 g [ adult 1g hour times a day ] Children – 500 mg four times a day

Methenamine hippurate [ hiprex, urex] ⇒ tab 1 g [ adults – 1g twice a day ] children 0.5 – 1 g twice a day.
Adverse effects:-

Cremping, vomiting, diarrhea, stomatitis, anorexia, urinary urgency, bladder irrigation, dysuria, proteinuria, hematuria,
hypersensitivity rexn addeminal pain.
Contraindications :-

Renal insufficiency sever hepatic disease & sever dehydration.


NSG responsibilities :-

Do not use alone for acute infections.

Use cautionary in pregnant or NSG mothers and in pt. with gout

Monitor I / o

Provide adequate fluid.

Monitor urinary PH prouide supplementary.

Acidification of urinary Ph exceeds 5.5

Be aware that methenamine can interfere with caboratory urine determination.


Dietary precaution :-

Advise pt. to avoid excessive intake of alkalinizing foods as milk or citrus fruits.
2. Nitrofurantion :-

A synthetic nitroforan derivates nitrofuration is a specific urinary antibacterial agent.


MOA :-

Bacteriostatic in low conn & bacterium cidal in higher conn . its probably mechanism to interfere with carbohydrate
metabolism by inhibition of acetyl co – enzyme. A may also impair bacterial cell wall formation.
Uses :-

Treatment of UTI due to susceptible organism. Prophylaxis against recurrent bacteria.


Dosage :-

Oral adult → 50 – 100 mg 4 times a day, chronic therapy 25- 50 mg four times a day

Children → 5 – 7 mg/ kg / day in 4 divided doses.

Proxphyloxis of recurrent injection → 50 mg daily / bed time last 6 months.

IV infusion ⇒ over 120 I.b / 80 mg twice a day.

Infusion solution is prepared by adding 20 ml. 5 % dextrose injection to the vial containing 180 mg nitrofurantion
sodium each ml of this solution is added to at least 25 ml of parentral fluid.

Find solution is administered at ratio of 2 – 3 ml / min.


Adverse effects :-

Diarochoea, abdominal pain, pancreatitis, parotitis,

Chills, Cough, chest pain, pneuneitis / fibrosis

Rashs, fruritis, urticaria, alopecia,

Hemolytic anemia, leucopenia, megaloblactic anemia, thrombocytopenia.

Drug fever, asthmatic attack, jaumide ortholia.

Dizziness, paresthesia, headache, periupherol neuropathy.


Contraindications :-

Anuria, oliguria, renal impairment, pregnancy at tern. Infects under 3 months.


NSG responsibilities :-

Administer oral drug with meals or milk to reduce GI distress & possibly to improve absorption.

Ensure that drug is taken at evenly spaced intervals

Instruct pt. rinse mouth though after use of oral suspension to prevent staining of teeth.

Be alert for sign of VTI

Protect drug from strong light


Note that drug can cause false positive tests for sr. grouse, bilirubin, BUN, alkaline phosphical
Other drugs :-

Other drugs used in UTI are sulfonamides, contrimoa zole, nalidixic acid, fluoroginolones, aminoglyeosides,
tetraeyelines, cephalosporinset.

Urinary analgesics → phen a zophyridine has analgesic actions on the VI. It relieves burning symptoms of dysuria &
urgency.
Acidifiers :-

Acidifiers are the agents or drugs, which are used to treat acid – base imbalance in body or for the treatment of
metabolic alkalosis acidifiers are the agents, which are used to neutralize the PH which has been sed due to certain
causes like excess alkali intake.
Metabolic alkalosis :-

It is a process in which plasma bicarbonate level is sed. This is usually the result of se loss of acid from the stomach
or kidneys, potassium depletion accompanying diuretic therapy, excessive alkali intake, or severe adrenal gland
hyperactivity. If alkalosis is severe it may cause epathy. Confusion tetnay.
Classification :-

- Ammonium chloride
- Arearbic acid
- Calcium chloride
- Phenezophyridine
1. Ammonium chloride :-

It is primary used as a systemic & urinary acidifier to treat metabolic alkalosis to correct chloride depletion & to assist
in urinary excretion of certain basic drugs. The drug has been used as an expectorant is found in a member of over the
counter cough preporations. Although its efficacy is subject to considerable doubt & its use in this manner should be
discourged.
MOA :-

Ammonium chloride may se flows of respiration, fluid by reflex irrigation of the gastric mucosa.
Indications :-

Metabolic alkalosis

Hypochloremia

Adrenal gland hyperactivity


Contraindications :-

Severe renal disease hepatic & pulmonary diseases


Doses :-

Expectorants – adults – 20 – 400 mg every 4 hour

Children – 50- 75 mg/ kg in indeed doses

Urinary acidification → 3 – 12 g a day n divide doss 4 – 6 hr. introduced


Side effects :-

Metabolic acidosis [ vomiting, thirst, weakness, hyperventilation, lethargy, drousiness, confusion]

Headache, hyperglycemia, hypokolemia, hypocalemia,

Too rapid IV administration com result in arrhgthmias, tonic conualsions & coma.
NSG responsibilities :-

Note rate & depth of respiratory rate during drug thrapy, hyperventilation, weakness & shortness of breath are possible
early signs of acidosis

Use cautions in pts with chronic heart disease & in small children.

Do not use enteric – coated tablets or expectorants, because gastric irrigation, the desired action is stimulated.

Avoid administration of milk or other alkaline solution with NH4Cl.


2. Ascorbic acid :-

Vit – C or ascorbic acid is an essential dietary substances that plays a major role in many metabolism rexn. as well as the
formation & maintenance of collagen & intracellular ground substances, it is also used as supplement to treat metabolite
alkalosis or alkli exces.
MOA:-

Ascorbic acid acts as an acidifier, which helps to neutralize the alkali excess thus help to reduce the PH towards its
normal valves.
Uses :-

Prevention & treatment of & curvy & other vit. C deficiency stagtes.

Deep burns & delayed wound healing

Acidification of urine, usually in conjunction with a urinary anti – infective


Contraindications :-

Use of sodium ascorbate, injection in its with Na restricted or calcium ascorbate in pt’s receiving drugs.
Doses :-

Oral → treatment of deficiency state – 100 – 150 mg / day as needed.

Prophylaxis – 50 – 100 mg / day

Urinary acidification – 4 – 12 mg / day of ascorbic acid in divided doses every 4 hours.

IM. IV, SC → upto 2 g/ day as needed for severe deficiency states, maintenance does is 100 – 200 mg once or twice a
day.
Adverse rexn. :-

Usually with large does – Diarrhoea precipitation of oxalate or urate renal stones, soreness at IM / SC injection site &
dizziness or faintness with 100 rapid IV injection.
NSG responsibilities :-

Use coutionly in pts with glucose – 6 phospchate dehydrogenize deficiency, hyperuricemia, renal impairment &
pregnant women.

Be aware that large doses may result in false reading in certain laboratory tests like urine glouse, sr. uric acid & urinary
steroids determinations.

Inject slowly IT or avoid dizziness & possibly fainting.

Do not inject calcium ascorbate sc & avoid IM injections in infants, as tissue necrosis conoceur.
Alkalinizers :-

Alkalinizers are the agents or drugs which are used to neutralize the PH, which has been sed due to certain causes the
like metabolic acidosis.
Metabolic acidosis :-

It is a process that causes a se in PH of body as a result of retention of acids, or loss of bicarbonate buffers. It may be
categorized by presence or abseve of an abnormal anion gap.
A. The anion a gap onset :-

Acidosis include diabetic, alcoholic & lactic acidosis, the acidosis of renal failure & acidosis that result from
consumption of exceus acids such as salicytates, methanol or ethanol.
B. Non – onion gap onset :-
Acidosis occurs in diarrheq, renal tubercular acidosis &multiple myeloma among other conditions.
Classification :-

1. Sodium bicarbonate
2. Sodium acetate
3. Sodium citrate
4. Potassium citrate
5. Acetazolanide
1. Sodium bicarbonate :- it acting systemically

MOA :-

Neutralize gastric acidity & usually gastric PH above 3 – 4

When PH is lowered due to metabolic acidosis

Alkalizes are alkaline drugs

Which helps to neutralize the acids

Thus raise the PH toward normal range


Indications :-

Treatment of GI systems associated with hyperacidity [ heart burn, acid indigestion]

Treatment of hyperacidity associated with gastritis, peptic ulcer & esophagitis

Metabolic acidosis
Contraindications :-

Cardiae & renal pts, hypertension


Doses :-

about 0.3 – 2 g as needed one to four times a day.


Adverse rexn :-

Systemic alkalosis

Sodium overload

Milk – alkalosis syndrome

Rebound hypersecretion
NSG responsibilities :-

Administer alkaliniers in liquid form if possible because effeicacy is greater than with tablet or capsure formulations.

If given in a tablet form instruct pt. to chew before swallowing & follow with water.

Note that food acts as a buffer to gastric acid for approximately 60 min & that the presence of food can enhance the
action of alkalinizers. Thus, alkalinizers taken on an empty stomach have action of 30 min. where as if they are taken 1
hour after meals, their duration is approximately 3 hours

During chronic therapy administer alkalinizers 1 hour before or 3 hour after meals.
2. Potassium citrate & sodium citrate :-

It may be used to control uric acid & cystive kidney stones.


Uses :-

Effective in reducing pain & frequency of maturation when these are caused by highly acidic urine.

Widely used to treat urinary caleuli [ kidney stone] & in pt with cystinuria.

Citrates are used to make the urine more alkaline.


Contraindication :-

Cardiae disease

Hypertension
Dose :-

Tablet → to make urine more alkaline

Adult → at first, one to four tablets after meals & at bed time

Children → dose must be determined by pediatrician.

Solution → adults, 2 – 3 steps of solution mixed with water or juice four times day, after meals & at bed time
NSG responsibility :-

Advice the pt. to keep this drug as a stand by for emergency treatment of acute pain, but should not use it routinely.

Milk should be avoided with drug so as to avoid milk alkali syndrome.

Flush nasogastric tube with water after administration

Drink plenty of fluids.

Instruct client to take drug as directed not to exceed maximum dose.

Antacids should be taken at least 2 hours a part from other drugs as drug interaction may occur.

Warm clients not to use if diagnosed with hear disease.


3. Acetazolamide :-

Acetazolamide is a carbonic inhibitor. The drug has been employed as a mild divretic also for relief of migraine,
headache & chronic open angle glaucoma.
MOA :-

It inhibits the enzyme carbonic anhydride reducing formation of H + & CO3- ions, appears to retard excessive or
abnormal discharges from central neurons.
Uses :-

Adjunctive treatment of absence seizures, metabolic acidosis,


Dosage :-

8 – 30 mg / kg day in divide doses, usual range is 100 – 400 mg / day in combination with anticomualsants.

Contraindication :-

Renal & hepatic dysfunction

Acidosis

Adrenal insufficiency narrow angle glaucoma

Sulfa allergy, severe pulmonary obstruction

Early pregnancy
Adverse rexn. :-

poly uria, hematuria, glycosuria drbussiness, hepatic dysfunction, confusion, myopia, urticaria, rash.
NSG responsibilities :-

Cautions pt. to reportsion of hyokolemia muscle weakness, cramping, cardive, irregularities, & metabolic acidosis [
nausea, vomiting, abdominal pain, weakness, malaise, dehydration] & adjust dosage as needed

Use parenteral solution with 24 hours after reconstitution because if contain no preseruatives.

Observe diabetic [Link] because acetazolamide may other antidiaditie drug requirements by using blood glucose
level.
Unit - 07

Miscellaneous Drugs –

Introduction –

Emergency drugs are chemical compounds used in pts during life threatening condition so that the symptoms can be
controlled and the life of a pt can be saved.

for a drug to be useful in emergency, it must have a short onset of action and be administrated in such a way as to
facilitate repidonset of action.

CPR (cardio pulmonary resuscitation) is an immediate therapy that may be initiated for cardio respiratory failure .

Evidencethat an individual is breathless and pulseless is sufficient to warrant immediate resuscitation effects .

CPR is technique Of basic life support for oxygenating The brain and heart until appropriatedefinitive medical
treatment can restore normal heart and ventilatory action. CPR technique can used to Artificially maintain both
circulation and ventilation in persons suffering from cardic cardiac arrest It involves .

1. External cardiac message(manual heart compression ).


2. Artificial ventilation by either mouth to mouth, mouth to nose or Mounted to airway technique.
3. Management of foreign body or airway obstruction,corcothyroidotemymay be Necessary to open the airway before
CPR can be performed.
Specific medical therapy

Definative medical therapy commences once the pt. Has either been admitted to the emergency room or a special
resuscitation Team heads arrived to take over the pt's care. It will be based on .

1. The underlying cause of the cardiac arrest and whether it can be corrected.
2. Types of arrest have ocurredasystokor veutricular fibrillation present .
Drugs used in CPR –

Epinephrine –

Route – Administration directly into myocardium with 3.5 inch & 2 garge needle (intracradiac or Iv puch ).
Action –

1. Stimulates heart action .


2. Strengthens contraction of heart .
3. Converts fine ventricular fibrillation to coarse ventricular fibrillation. Thus allowing for easter defibrillation.

Isoproterenol(Isuprel ) –

Route –IV drip

Action –Tsw irritability& contractility of myocardium. Beneficial in treatment of complete arystole.

10% calcium chloride or calcium glutamate route –IV

Action –

1. Strengthens the cardiac contraction .


2. It is a potassium antagonist
3. Indicated in cases of hyperkalaemia
Sodium bicarbonate –

Route –IV

Action –corrects metabolic acidosis that develops due to tissue anoxia .

Metaraminalaramine –

Route–IV

Action – correctsevere hypotensim shock and cardio vascular collapse.

Lidocaine (xylocaine ) 17.4% –

Route –IV

Action – Used to treat ventricular arrhythmias, central ventricular arrhythmias.

Dopamine (Intecopin ) –

Route – IV drip

Action –

1. Tse B.P. by using the strength of myocardium contraction .


2. Produces mild vasoconstriction in skeletal mussels selecting dilated mescutric and renal vessels .
Bretyliumtosylate (bretylol) –
Route – IV push /IV drip

Action –

1. For ventricular fibrillation which are not responsive to normal antiarrhythmic therapy .
2. For ventricular tachycardia unresponsive to normal antiarrhythmic therapy .
Post resuscitation measures –

1. Skilled after care is essential for the pt who has suffered an arrest .
2. Continuous vigilance must be ensured by a skilled person for 48-72 hours.
3. If the pt is not in the intensive care unit ,shift him thare for construct watch.
Drugs used in emergency –

1. Injection adrenaline
2. injection atropine
3. Injection digxine
4. Injection sodium bicarbonate
5. injection dopamine
6. Injection efcorlin
7. Injection decardron
8. Injection avil
9. Injection calcium gluconate
10. Injection laxis
11. Injection aminophylline
12. Injection tsoptin
13. Injection calmpose
14. Injection deriphylline
15. Injection 20% destrose
16. Local anaesthetic drugs (xylocaine 2%& 4%)
Adrenalin –

Indications – Ventricular fibrillation, pulseless ventricular tachycardia.

Dose - 1mg 1ml (1:1000) every 3mintues ,IV

Adult –1mg in 9ml normal saline (1mg /10 ml) pediatricdosage: 0.01 mg /kg (10 mg/kg) in normal saline (up to 5ml)

Anaphylaxis ( 5 minutes ,IM ,10 dose may begins )

Adult -0.5 mg

Pediatric - 0.01 mg /kg ,glucogen 1-2mg ,IV.


Lignocaine –
Indications – ventricular fibrillation, pulseless ventricular tachycardia.

Dose -1mg/kg
Atropine –Asystole or severe bradycardia

Dose- 1.2 to 3.0 mg (adult )

20 iug / kg (child)
Oxygen –

Indication–

Asthma of bronchospasm - 8L/min

Acute coronary syndrome - 8L/min

Acute pulmonary edema - 8L/min

Status epilepticus- 8L/min


Injection dopamine–

Indication – Shock -cardiogenic ,hypovdene&septic shock ,

Dose- 5ml -200mg ,2-10 ug/kg body weight.

Pentozoeine–

Indication – Post operative & chronic pain.

Dose – 1ml -30 mg ,50-100 mg oral; 30-60 mg IM

Verapamil –

Indication –Supraventricular ,tachycardia atrial flutter ,fibrillation, hypertrophic cardiomyopathy.

Dose -2ml -5mg ,120-240 mg daily in divided doses or IV 2.5 to 5mg slow IV bolus upto10 mg.

MgSo4 –

Indication- prevention of seizures ,pre eclampsia

Dose- 4g over 5-15 minutes IV followed by IV infusion.

1g 1hour for at least 24 hour after last seizure .


Nitroglycerin –
Indication – Acute myocardial infarction ,unstable angina , coronary artery spasm, pulmonary edema following LVF
,infarct limitation intraoperative hypertension.
Dose– Diluted in NS (5mg 150 ml ) infused.

Lorazepam–

Indication – status epilepticus ,anxiety erinsomnia

Dose –0.1 mg/kg ,status epilepticus, anxiety 1-6 mg od in divided doses 1-2 mg /day in insomnia with anxiety 1-2 mg
hsparenteral ; IM or IV injection into a large vein .
Dextrose –

Indication – hypoglycaemia maintenance fluid in new born , fluid replacement without significant electrolyte deficit,
management of hyperkalaemia.
Dose – 5% ,10% isotonic solutions of 500 ml bottles 10% &20 % solutions 1000 ml for parenteral nutrition, 25% ,50%
hypertonic solutions as 25 ml ampules 25%dextrose 2ml/kg with insulin for correction of hyperkalaemia.
Injection sodium bicarbonate –

Indication – Alkalinize the urine in poisoning

Dose – 1-2 mg /kg /h IV infusion needed to maintain urine ph b/w 7.5 &8.5.

Metabolic acidosis – 7.5 % -25 MI 1-2 mg/kg hIV infusion.


Sorbirate –

Indication – chronic angina pectoris prevention of acute episodes of angina

Dose – 10-30 mg ,3 times a day .

Nifedipin–

Indication -Angina &ectorissystemic hypertension raynaud's phenomenon .

Dose – 5mg ,10mg ,20mg tablets 20mg once daily .

Normal saline –

Indication –Anaphylactic shock ,hypovolemic

Dose – 20 mg/kg

Hydrocortisone –

Indication – anaphylaxis, asthma & bronchospasm


Dose – adult -250mg (4mg/kg ) IV paediatric-4mg /kg IV .

Salbutamol nebulization –

Indication – asthma & bronchospasm

Dose – adult - 10mg by O2 ,8L/min every 15 minutes paediatric-5mg 125 ml by O2 ,8L/min.

Ipratropium –

Indication– asthma & bronchospasm

Dose –adult- nebulization 500 ug 2hourly

Paediatric- 20ug 1dose inhaler (MDI) w9 spacer ,2-4 puffs every 20 minutes in 1st hour.
Aspirin –

Indication –a ate coronary syndrome

Dose - 30mg orally .

Glycerltrinitrate (GTN ) spray –

Indication – Acute coronarysyndrome (CAD ,MI angina )

A cute pulmonary edema


Dose- 1 dose repeated after 5 minutes if no improvement.

Morphine –

Indication -Acute coronary syndrome

Acute pulmonary edema.


Dose – 2.5 mg IV every 5 mint as requirement max of 15 mg .

Frusemide–

Indication -Acute pulmonary edema

Dose - 20-40 mg IV

Diazepam –

Indication – Epilepticus rectally in febrile convulsion .

Dose - Adult dose – 5 -10mg IV or 10-20 mg per rectum (dilute with 5ml of saline podiatry: diazepam IV 10mg /2ml
,0.10 ml/kg diazepam per rectum 10mg 12 ml,0.10 ml/kg.
Midazolam–

Indication – IV anaesthesia, sedation of intubated & mechanically ventilated pts epilepsy .

Dose – adult dosage : 5-10mg IM or 2.5 -5 mg IV

Paediatric dosage : 0.2 mg/kg IM or 0.1 mg/ kg IV .


Observation & expert care –

 Monitor ECG ,CVP &blood pressure .


 Check the oral cavity and Jow position as his tongue may falland obstract the airway.
 Temperature is taken every hour a high temperature usually indicates cerebral damage or cerebral edema.
 Blood gas and pH determination are done to detect metabolicacidosis, Which may have developed owingto poor
oxygenatia.
 Amobarbital sodium is given IV in convulsions.
 A chest X Ray film is obtained using portable equipment. Ribs often are accidentally fractured during cardiac
massage.
 Insert an endotracheal tube If not already in place. This maintained an open airway for the unconscious PT. who
cannot clear secretion by coughing.
 Give O2continuously for 20 hours following resuscitation by endotracheal tube or mask. This is required because
respirations are depressed for sometime after arrest .
 Insert Foley’s catheter urine output is one of the measure of the cardiovascular status report if the urine output is
below 30 ml per hour .
 Start IV infusion to administer enough fluids in the pt.
 Record the procedure on the nurse’s record with the date and time
 Time the victim was discovered.
 Type of arrest .
 Any complications developed during CPR
 Time at which spontaneous respiratory & pulse returned .
 Time at which CPR started & discontinued
 Vital signs when the CPR team left the pt.
 A nasogastric intubation & aspiration of contents of stomach are necessary for a pt with a full stomach to prevent
vomiting &aspiration of vanities into lungs .
 Common immunosuppressant drugs –
Group Name of Uses Nursing
drug action
Caleineurin Cyclosporine Most effective Initial dose till
Inhibitor Oral IV 10- for Prevention 1-2 weeks
15 and treatment after
mg/kg/day for graft transplantation
rejection in maintenance
renal hepatitis dose 2-6mg
cardiac born /kg /day
marrow and medicine
transplantation administer
rheumatoid with milk or
brenehial fluid, juice pt
asthma should be
,inflammatory monitored for
zowel disease injection
etc.

Tacrolimus –

Useful in pts with rejection is not suppressed by cyclosporine & suitable for a cute rejection; it is very much useful for
liver transplantation &fistulising crohn's disease .
Dose – oral /IV 0.05 –0.1 mg / kg for renal transplant, 0.1 -0.2 mg/kg for liver transplant.

Nursing action –

 Regular blood level monitoring


 Monitor vital signs regularly, follow strict aseptic technique.
Mycophenolatemofetil – It is the add on drug with the cyclosporine to reduce the dose &its toxicity in graft
transplantation.
Dose - 1g ,250mg ,500mg tablet /capsule

Nursing action –

 Monitor the pt for GI bleeding


 Check vital sign periodically
 Follow aseptic techniques
MTOR Inhibitors –

Sirolimusevorulimus– useful for prevent & treatment of graft rejection by alone or with combination of cyclosporine
or tacrolimus; it is useful for stem cell replacement .
Dose - tablet 1mg

Nursing action –
 Monitor vital sign regularly
 Use aseptic technique to be followed while taking care of patient

Cytotoxic drugs / antiiproliferativedrugs –

Azathioprine –

It is used in combination with cyclosporine Prevention of graft rejection, it is also useful for progressive rheumatoid
arthritis, inflammatory bowel disease Alternative to long term steroid in autoimmune disease
Dose - 1-5 mg/kg

Nursing action–check for hypertensive reaction.

Methotrexate- Useful as faster line drugs in autoimmune diseases such a rheumatoid arthritis severe psoriasis,
pemphigus ,myasthenia gravis ,uveitis , chronic retive hepatitis .
Dose – 10 -25 mg oral ; if IM /IV will be a single dose.

Nursing action – Regularly check for renal functions any signs of bleeding ,presence blood in urine &haematological
monitoring.
Chlormbucil – It is a weak immunosuppresses autoimmune disease

Dose – 0.1 -0.3 mg /kg/day

Cyclophosphamide – It is very much useful in bone marrow transplantation and as a maintenance therapy in
pemphigus systemic lupsis erythematous , thrombocytopenia purpura.
Nursing action –

Regular monitor vital signs, BP, blood sugar, blood level drug end provide iPod genic care and infection prevention
precautions.
Glucocorticoids —

Corticosteroids– these are companion drugs to cyclosporine ; It is useful in graft rejection and autoimmune disease.

Nursing action–

 Provide hygienic care


 Cheque blood sugar periodically .
Antibody reagents –

TNF inhibitors –
Mainly used in autoimmune disease
Nursing action-

 Cheque for cytokine release syndrome


 continuous monitor of vital science
 provide side rails
 Although Institute protocol while administered drug
Anti CD3 antibody –

Useful in acute transplant rejection, steroid resistant cases ,depletion T-cells from the donor bone marrow before
transplantation.
Nursing action –

 Cheque for cytokine release syndrome


 Continuous monitoring of vital signs
 Provide side rails
 Follow Institute protocol while administering drugs.
Anthymocyte globulin –

It is used to suppress acute allograft Rejection episodes among steroid resistant cases.
Nursing action –

 Cheque for cytokine release syndrome


 Continuous monitoring of vital signs
 Provide side rails
 Follow Institute protocol while administering drugs.
Immunostimulating :-

Immunostimulation & immunomodulation agents are drugs that modulate the immune response & can be used to se the
immune responsiveness.
Thalidomide:-

It is a teratogenic drug, It enhances cell-mediated immunity by action on T-cells. Thalidomide is used in multiple
myeloma, lepra rex4 & in lupus erythmatasus .
Interferons are cytokines with antivird & immunomodulatory properties. Recombinant interferons α,β and γ bind To
specific receptors & binding about immune activation & these host defenses leading to an these in the no. & activity of
cytotoxic & helper T-cells & killer cells.
Immunization :-

Vaccines & antisera are used for immunization against bacterial & viral infections.

Vaccines stimulate the host immune system while autisera supplement & support the immune system with readymate
antibodies.
Immunoglobulins :-

Ig are human gamma globuline that carry the antibodies – like normal human gamma globulins. Tetanus Ig, rabies Ig,
antidiptheria Ig & hepatitis B Ig, Allergic rex4 including serum sickents & anaphylasix [Link] with sntisera, while it
is uniommon with Tg.
VACCINES & SERA :-

Substance, which provide immunity either actively or passively are called immunizing agents, they can be classified as
vaccines, Ig antisera. Immunity can be active or passive.
Immunity :-

1. Live attenuated
2. Inactivated or kied
3. Toxoids
All immunities are done in Ist year micro-biology.
Immunization schedule:-

Immunization schedule done in community health nursing.


Anitdote & Anitsnake venom :-

Management of common poisoning :-

A poisen may be defined as any substanies which if administered or comes in contact with a living being produces ill-
health , disease or beath, every drug in a high dose can cause poisoning .

Poisoning could be accidental, suicidal or homicidal, Millions of poisoning cases are seen every year with several
hundreds dying, but several more are unreported.

Mortality rate varies form country to country . In india it is around 35%, it is around 35,% while in
America, it is 2% when treated on time with appropriate drugs, treatment of poisoning can be successful.
Paracetomol poisoning :-

Sign & symtctans :-

First 24h- normal, vomiting , Anorexia, & abodeminal pain.

Within 1-4 days, I’sed serum transanina Jaundic, liver tenderness & prolonged.

Protherambin time, liver failure, nephrotoxicity acute renal failure.

Dose:- 10-15gm in adult con cause serious toxicity.


Management :-

Stomach wash is given, activated chareod prevents further absorption

Antidote is N-acetyleyrtein [150mg/ kg TV] infusion over 15 minutes,

Oral loading dose-140 mg/ kg followed by 70 mg/kg every 4 hour- 17 does


Salicylates poisoning :-

Sing& symptoms –

 Dehydration
 Hyperpyrexia
 Gastrointestinal
 Irritation
 Vomiting
 Acid-base imbalance
 Restlessness, tremors, delirious
 Hallucination
 Metabolic acidosis
 Convulsions, coma 4 death.
Management :-

Treatment is symptomatic gastric leuage correat acid base imbalance

Dehydration :- IV fluids , Na+,k+, HCO3- & glucose, blood ph should be monitored,

Tempr is brought down.

Blood transfucion & are needed.

Alkaline divresis with sodium bicarbonate & divretic like frusemide is given along with IV fluids.
Morphine & other opioids poisoning :-

Sing & symptens :-

Respiratory depression

Shallow breathing, pinpoint pupils

Hypotension, shock, cyanosis

Flacidity, stupor, hypothermia,

Coma & respiratory failure & pulmonary edema.


Dose:- Lethal dose of mouphine in non-addiets is about 250 mg.

Management :-

Positive pressure respiration .

Maintenance of B.P., Gastric lavage with potassium permanganate or renove unabsorbed drug,

Specific antidote is naloxone-0.4-ob mg, IV repeated every 10-15 minutes.

Organophosphorous poisoning :-
Sing& symptoms : -

Vomiting, abdominal lramps, diarrhea miosis, sweatin, Tsed salivary

Tracheobraonchial and gastric seretions, and bronchopasm ; hypotension muscular tritchings weakness, convulsion and
coma death is due to repiratory paralysis.
Management :- Maintain BP

Patent airway if poisioning is through remove clothing skin wash the skin with soap and water gastric lavage is given

Drug of choice is atroping IV 2 mg every 10 min tall pupil dilates; maximum dose can be anything from 50-100 mg or
more depending on the severity of the poisoning cholinesterase reavitvators, pralidoxime, obidoxime and
diacetylmonxime; thus they reactivate the cholinesterase enzyme the should be given within mintues after poisoning is
severe poisoning 1-29 of IV parlidoxime given within 5 minute of poisoning gives best results.
Atropine poisoning :-

Sing and symtoms :- Dry skin fever dry mouth, dysphagia, dilated pupils muttering delirium palpitation restlessness
excitement, hallucinations, hypotension difficulty in possing uring and passing shools. Convulsion and coma may result
in death .

Scoplamine Cause central nervous system (CNS) depression instead of CNS stimulation .
Management :- Gastric lavage with tannic acid if the polsoning is by oral route saline purgatives to prevent absorption
of the poison.

Tepid sponging to reduces tem small sips of water to moisten the mouth sterile saline to be installed into to eye to
prevent drying physostigmine 1-2 mgIV is the antidote, it is an anticholinesterase drug physostgmine eye drops to over
come myelrasis, catheteigot of the bladder.
Barbiturates :-

Sing & symptoms :-

 Respiratory depression
 Shallow breathing
 Hypotension, skin eruptions
 Eardiovasullar collapse & renal failure .
Nursing Action :-

Gastric levage followedge adminilteration of actinated charcoal to prevent further absorption of barbitwater.

Maintenance of pt airray, adequate ventilation & O2 administration general supportive measures like maintenance of BP
& fluid blance.

Forced Alkaline aiversis & IV fluids hill hasten the excertion of long- acting barbitwater through the kidney since they
are acidic drugs.

Henodiylysis should be done especially there is renal failure.


Digitalis :-

Sing & symptons ;-

Extracrdiac :- Anorexia, nausea, vomiting & dearrhea, weakness, confusion, Halluition, blurred vision.

Cardiac toxicity – Brodycardia, arrhythmia, pluse bigeminy, AV block, hypokalemia,


Nursing action :-

Stop digitalis

Oral or parentral K+ supplements given

IV phenytoin given for ventrivular arrhythm

Atuopine for bradyeardia,

ProPanabol given for supraventrialur arrphar


Antidigoxin immunotherapy given if severe poisoning.
Methanol :-

Sing & symptoms :- Vomiting , vertigo, headache

Severe abelomicanal pain

Hypotension

Dolirium, Acidosis & coma

There are reports of even 15 ml of methnat causing blindness, death is due to respiratory failure.
Management :-

Correct acidosis with sodium bicarbonate infusion helpsin prevetions Bindness.

Pt, should be kept in a dark rum to prodect the eyes.

Gastric lavage should be given

BP& ventilation should be maintained ethyl alcohol is given immediately


Anticlote:- Pomepizole inhibits the enzyme alcohol dehydrogenase

Hencodialysis to enhance the4 elimination ob methanol.

A loading dose of 0.6 gm/ kg is followed by an infusion of 10 mg / hour


Acute alcohol intoxication :-

Sign & symptoms :-

Blood alcohol con4 exceeds 200 mg %

Fatal alcohol con4 Varies b/w 500&600 mg%

CNS depression , dilated pupils, slured speech, nausea, vomiting, tachycoralie circulatory collapse, hypothermia,
stupor& coma.
Management :-

Stomach washing using NS

Maintain circulation & Respiratory 50 ml ol glucose given IV to teat hypoglycemia

100 mg thiamine IV to prevent wernicke’s encephalopathy.

Maintenance of fluid & electrolyte balance


Hemodialysis – clearane of ethonal can be enchaneed by hencodialysis.
Heparin :-

SIS – Bleeding due to overdose of heparin


Management

Stop heparing because heparing is short- acting

Antidote of heparin- protamine sulfate are given IV [ 1 mg for every 100 unitesof heparin ]

Absense of heparine, protamine sulfate can itself act as a weak anitcoagurrt its overdose should be avoided.
Warfarin :-

SIS – Haemorechage ocuur due to overdoase

Bleeding in the intestine or brain.

Minor episiodes of opistoxis & gluns bleeding.


Management :-

Depends on the severity –

Stop the anticoagulant

Fresh blood transfusion of given to supply clotting factors

Antidote - v1+ -k¹ allow the synthesis of clotting factors .

Fresh whole blood is necessary to counter the effects of oral anticoagulation’s .


Insulin –

S/S –

 Hypoglycaemia
 Sweating ,palpitation , tremors
 Blurred vision ,weakness ,hunger
 Confusion ,difficulty in con.
 Drowsiness
 Convulsion, coma & death.
Management – Lyrical to convert to oral glucose or fruit juice like orange juice or in serve cases, IV glucose promptly
reverse the symptoms
50ML off 50% glucose is given IV followed by dextrose infusion depending on the requirement.
Iron –

S/S –

 Vomiting, abdominal pain


 Hematemesis,bloody diarrhoea
 Shock , drowsiness ,cyanosis
 Acidosis ,dehydration
 Cardiovascular collapse & comma
Management –

 Gastric lavage is given with 2% sodium bicarbonate solution ,


 Desperriexamine is the antidote .
 5-10gm is instilled into the stomach at the end of the stomach wash , to prevent iron absorption, IM 2 gm every
12 hour or IV 10-15 mg/kg /hour .
 Correction of acidosis & shock .
 Haemodialysis or exchange transfusion help in severe cases .
Cyanide –

S/S –

 Inhibition of cellular respiration


 Block the utilization of O2
 Fatal occur
Management –

Amyl nitrite is given by inhalation &sodium nitrite by IV ( 10ml of 3% solution ), sodium thiosulfate is given IV (50ml
of 25% solution ) . It react cyanomethemoglobin to form thiocyanatewhich is easily excreted by the kidney , nitrates
convert haemoglobin to methelneoglobine .
Iodine over dosage–

Signs &symptoms –

 Acute toxicity with iodine can be fatal (3-4 fatal dose ) .


 Nausea & vomiting
 Diarrhea
 An unpleasant metallic taste
 Vesication& desquamation
 Corrosion of skin & mucous membrane with brownish -yellow stains
 Perforation of mouth ,throat & GI mucous
 Nephritis & renal failure, delirium stages
 Inhalation produces edema of glaltis& pulmonary edema.
 Anaphylactic reaction can occur iodine is a term used to denote chronic poisoning with iodide salts &is
characterized by erythema , urticaria, aene, stomatitis, conjunctivitis, rhiharechea parotid ,swelling ,
lymphadenopathy , anorexia &insomnia.
Management-

 Administer starch or flour solution (30 gm per literof water ).


 Milk is also helpful
 Solution thiosulfate is the antidote.
 A solution of 1 -5% sodium thiosulfate is given orally . This will convert iodine to iodide , which is relatively
harmless
 Skin lesions can be treated with 20% alcohol supportive therapy.
 Treatment involves liberal intake of sodium chloride ,which promotes excretion of iodide
 Induction of vomiting or stomach wash are contraindicated.
Treatment of snake bite –

In all case of snake bite ,the pt. Is in great fear & is in a stage of neurogenic shock . The pt. Is in a semiconscious state
with cold , clammy skin ,feeble pulse , rapid &shallow breathing. Other symptoms very a/c to the type of snake. The
skin & symptoms to systemic toxicity appear in about half an hour .
1. Elapid bite (cobra ,krait etc. – neurotoxic ) –local reaction ate pain ,burning ,swelling , discolouration of the
site , oozing of blood stained fluid are seen in 1-3 hours .
Blisters &local neurosis may occur systemic effects include vomiting, headache ,loss of consciousness, ptosis ,
ophthalmoplegia ( eyes become fixed in central position ) conversion followed by flaccid paralysis .
2. Viper bite – hematoxic –local reaction are prominent with swelling, discoloration, blister formation
&bleeding from the site. Bleeding from the gums , haematuria, disseminated IV coagulation are seen.
3. Sea snakes (hydrophids) –local reaction are mild swelling &pain systemic myotoxic effects include muscle
pain, stiffness ,renal &hepatic necrosis
Treatment –

First aid –

 Reassurance
 Immobilize the bitten part .
 Measures like local incision ,suction ,application of ice are all found to be harmful &no more recommended.
Supportive therapy –

B.P. ,respiration & urine output are to be monitored ECG & blood gas analysis are needed. Fresh blood transfusion may
be needed to correct coagulation parameters.

Analgesics like paracetamol for pain , prophylactic antibiotics as required &tetanus toxoid injection are to be given in
all cases .

Anti snake venom (ASV ) is indicated in presence of signs of systemic envenomation miotin as depicted in
Level of envenomiaton dose of antivenom

Mild enenomination 3-5 vials.

Moderate 5-10 vials.

Severe 10-20 vials

Infusion should be done after test dose. Watch for rex. To ASV. Hypersensitivity rex. Including anaphylaxis con occur.
Clean the bite site with providen iodine.
Food poisoning :-

Food poisoning can occur on consumption of food that is contaminated with micro- organism toxins or chemicals.

Nausea, vomiting abdominal pain. Fever, weakness & diarrha are the conimon symiztoms of food poisoning,
othersymptoms depend on the causative agents.
Cause for food poisoning :-

Micro organism :-

 Bacteria
 Protozoa
 Varusis
Toxins :- present in certain fish, plauts & mushrooms

Chemicals.
(1) Micro organism :- Bacteria including salmenalla typhi, staphylococaus aureus, shigella, vibriocholerae, vibro
perphemolytive bacillus cereus, clostridium botulinumm, streptococcus , campylobacter & esegrichie coli can cause
food poisoning. Vriral gastritis may be caused by rotovirem parvirus & adenovirus.
Fungi:-
The spores of moulds grow on food and can release mycotoin. These mycotoxins are heat stable.

Aspergillus flauus can produce aflatoin penicillin islandicum can produce islanditorm.
Others :- Protozoa like entamoeba histolytia [Amebiasis] & Giardia lancbia [Giardiasea] are commen cause of food
poisoning, metronidazole is the DOC in both.

Mushooms & T of the large varity of mushrooms, only about 5% are poisomuus consumption of such mushrooms can
cause a variety of toxic effects depending on the toxin- they can cause cellular destruction, affect central are autonomic
nervous system , Gastrointestial system or the kidney.
Chemicals :- Arsenic, Mercury, autimary or insecticides in fruits & vegetables can cause poisoning

Unit - 08
Drugs used on skin & mucus Member
Several drugs are available for topical skin therapeutics, but
occasionally some drugs may be used systemically for effects on
the skill. Skin preparations may contain preservatives, anti-
oxidants, & coloring agents that may give rise to adverse
reaction.

#Emollients – Emollients/barriers are occlusive agents or


moisturizers used to prevent or relieve the signs & symptoms of
dry skin. Emallients are used to rehydrate & soothe the skin &
are effective in all conditions characterized by dryness, scaling &
crackling of the skin. The most common emollients used are
olive oil, arachis oil, sesame oil, coco butter, hard & soft
paraffin, liquid, paraffin wool fat & spermaceti.

#Demulcent’s
Demulcents are substances that smooth the inflamed
mucosa by preventing the contact of air/irritants with skin.

(1) Glycerine –
It is one of the most common hydrating agents, which are
clear, sweet & viscous. In addition to its hydrating effects it acts
as lubricast for skin surface.
- It is indicated for use in the treatment & prevention of dry skin
applied to anal canal as suppository to induce evacuation. It can
also be used as skin protecting agent & as a solvent for different
pharmaceutical agents. The only contradication for use is
hypersensitivity to glycerine.

(2) Methylcellulose:-
It is used as bulk purgative, as nasal drops &in contact lens
solutions.

(3) Propylene glycol –


It is used in cosmetics & as occlusive dressing for ichthyosis
etc.

#Absorbants & protective –


Absorbents & protective are finally powdered insert &
insoluble solids, which are adsorbent in nature magnesium/zine
stearare, tale, calamine, starch & suralfate [topical] are its
examples.

#Caustics & Escharotics –


Caustics are Escharotics are chemical substances which
causes local tissue destruction & sloughing.
- They are used to remove moles, wartes & papillomass, silver
nitrate phenal & tricholaro actic acid are its examples.
#Counter irritants –
It is applied to the area of skin supplied by nerves from the
same segments as the deeper organ from which pain impulses
obscure the deeper sensation.
It is massaged to relieve headache, pain & muscles joints
pain & colic.
Olive oil, evcalyptus oil, methyl salicylate Iodex, vicks
vaporv bare its examples.

#Keratolytics –
Keratolytic dissolve the intercellular substance in the horny
layer of skin. The epidermal cells swell, soften & then
desgramate, It is used for hyperkeratotic lesions like corns,
warts, proridsis, ring warm chronic dermatitis.
- Salicylic acid is effective when as an occlusive dressing.
- Propylene glycal acts as keratolytic. In lower conn it can also
act as mild antiseptic & antifungal.
- Resorcinol – It is used in eczema, ring warm, seborrheic
dermatitis etc due to its entiseptic antifungal & eratolgtics
prefertics.

#Antiborrhics –
#Anti-seborrheics –
Anti seborrheics are effective in seborrheic dermatitis,
which area rich in sebaceous gland [scalp, face, trunk] dandruff
caused by pityrosporum ovale is common.

Selenium sulfide –
Applied to scalp as 2.5% slows epidermal proliferaction &
sealing it is also anti-kerato lytic & fungicidol to P. ovale.
Imidozole antifungals – Ketocanazole given orally 200
mg/day for 4 weeks is effective against P. ovale.

#Melanizing Agents –
Melonizing agents increase sensitivity to solar radiation &
promote repigmentation of utilligious area of skin they also
stimulate melanocytes & induce their proliferation.

Methoxsalen –
Macsoralen 10 mg tablet orally is effective. Topical form is
also available.

#Psoriasis – Proriasis is a chronic recurrent disease


characterized by dry silvery scaling plaques of various sizes
under which red/pink lesions are present. These lesions appear
small area of the body for short period of time with
unpredictable remissions & exacerbations.
Characterized the dry skin with pruritis.
Topically applied emollients, kerotolytics, antifungals & topical
corticosteroids may help to relive itching & remove the scales.

i) Calcipotrial :- Drug combined with steroid to relieve


smymptoms of psoriasis. Skin irritation erythema & scaling
common side effects.
ii) Tozarotene:- It has antiproliferative & anti-inflammatory
actions to relieve proriasis applied in topical gel form burning
sensation & peeling (side effects.)

iii) Photochemotherapy – Oral methoxasalen followed 1-2 hour.


Later by VVA exposure to alternate days but relapse occurs
when treatment is stopped. It causes skin cancer, cataracts &
immunological damage.

iv) Acitretin:-
0.5 to 0.75mg/kg/day, orally adverse effects –
* Dryness of skin & eyes
* Gingivitis
* Erythema & scaling of skin.
* Alopecia
* Liver damage

#Sunscreens –
Efficacy of a sunscreen formulation is quantified by its sun
protaction factor SPF. Which is ratio of the dose of UVB
radiation that produce erythema on protected skin.
It is effective in vitilligo therapy, drug induced photo
toxicity &to facilitate. Tannigs while preventing sunburn.
Physical sunscreen: titanium dioxide, zinc oxide & calamine
lotion or its common examples.

#Drugs for Acne outgrips


It is common skin disorder in adolescents in which sebaceous
follicles of face & neck produce excess of sebum & gets
colonized by bacteria: Benzoyl Peroxide is most effective. Which
kill anaerobic organisms.
Available in Cream get or lotion.

Adverse effects –
* Dryness of skin
* Marked scaling
* Erythema & contact sanitation

Retinoic acid –
It is keratolytic & comedolytic it promotes the lysis of
keratinocytes.
It is 0.25% - 0.05% get or cream For systemic therapy,
tetracycline, erythromycin may be used for 2 months.
Topical steroids –
Glucocorticoids have anti-inflammatory,
immunosuppressive, vasoconstrictor & anti proliferative
actions. Atopic eczema, seborrheic dermatitis, hypertrophied
scars keloids & psoriasis are common indication.
Betamethasone benzoate 0.25% Topicasene cream.
- Flucorton – 0.5% labate cream.
Hydrocortisone butyrate 0.01% locoid creams.

*Adverse effects –
- Hypopigmentain & easy bruising.
- Adrenal pituitary suppression
- Cushing’s syndromes.
- Thinning of epidermis.
*NSG responsibilities –
- Remember young child’s skin is more permacable therefore
there is increased risk for medication absorption & result in
systemic effects monitor systemic effects.
- Apply thin layer cream or ointments confine it to portions of
skin where it is essential.
- Watch for adverse reaction closely.
- Teach the pt. how to identify the adverse & stop usage
immediately.
- Never apply undiluted glycerin.
- Talcum should never be sprinkled on open wound as they can
form granulomas.
- Use volatile oils are mildly irrants, is normal.
- Use escharotics carefully have ulcer forming tendency.
- Drinking alcohol is prohibited in proriasis therapy.
- Rubbing alcohol can be used for back care but never use once
bed sore is farmed highly irritating to open wounds.

#Drugs used on the eyes –


The following types of drugs are in frequent use in the
treatment of eye disorders.

1. Antibiotics
2. Steroids & other anti-inflammatory drugs.
3. These which affect pupil size.
4. Those used in the treatment of glaucoma.
5. Local anesthetics.
6. Stains
7. Miscellaneous preparations.
- Drugs can be administered to the eye either by local or
systemic routes.

#Local use of drugs on the eye –


*Types of application –
The following preparations are used in the local treatment
of eye diseases.
(1) Eye lotions
(2) Eye drops
(3) Eye ointments
(4) Subconjuctional injection
(5) Ampoules for injection into the anterior chamber at
operation.

#Eye lotions prescribed as collyrium:-


These are used to wash foreign material from the eye &
some have a mid antiseptic action.
- They are applied an [which is a small glass container with a
fine spout].
- The pt. should be lie back or sit in a chair with the head
extended.
- Lotion should be warmed to 35 C.
- Before washing the eye, the lotion should be run up the check
into the medial can thus.
- The lids being firmly separated by the fingers.
- A small basin held by the pt. close to his face to catch the
effluent.
- This is less unpleasant than pouring the lotion directly onto the
cornea.
- The lotion should be steadly poured from the undine.
- The pt. being instructed to move the eye in all directions.
- There are many types of lotion but simple normal saline is
satisfactory for the removal of foreign material or dirt from the
eye.
- In emergency cases, however as in chemical contamination, it
is better to use cold tap water than to lose time in starting the
treatment.
- In case of contamination by time or cement an irrigation with
dihydrogen sodium ursenate is recommended.
- This substance is a chelating agent and converts an insoluble
heavy metal salt such as calcium hydroxide into a soluble
complex anion which can be removed in solution.

*Eye drops prescribed as Guttae:-


A No. of drug can be applied to the eyes by means of drops
which should be instilled into the lower conjunctiva sac.

(1) The pt. is told to look upwards away from the dropper.
(2) The lower lid is held down with the finger.
(3) Only drop is instilled into the lower fornix.
(4) The pt. is then told to dose the eye for a short while & the
excess is wiped away.
- All drops & ointment should be sterile when supplied and once
opened can no longer be considered so.
(5) There is an increasing tendency for them to be dispensed in
single dose containers which can be disordered after use.
This is particularly useful for pt. who require medication over
long periods & who may develop sensitivity to bemalkanium
chloride the preservative present in most eye drops.
- Drugs or preservatives in eye drops may become absorbed
into hydrophilic contact lenses & cause irritation. Therefore
lenses should be removed before eye drops are instilled & not
worm again. Until the treatment is finishes. Similarly, contact
lenses should not be used with eye ointments.

*Eye ointments prescribed as Oculentum:-


- These can be applied similarly either on a glass rod or from a
single dose container.
- The lower lid is pulled down & the ointment is placed in the
lower fornix.
- About half inch of ointment as squeezed from the tube, should
be used at each application.
- This should be delivered onto the end of O sterile glass rod or
prepacked plastic spatula.
- A separate applicator should be used for each eye if both are
to be treated.

#Drugs which affect Pupil size:-


These can be divided into –
1) Those which enlarge the pupil [mydriatics]
2) Those which contract pupil [Miotics]

1) Mydriatics – These are of two types –


A) Antimuscarinic drugs – These drugs paralysis of the muscular
sphincter of the iris, the sphincter muscle is innervated by the
PNS.
B) Sympathomimetics drugs –
These stimulate contractive of the radial dilator pupillae
muscle, which is sympathetically innervated.

#Antimuscarinic drugs –
(1) Atropine:-
Atropine is the active principle in the poisonous berry of
the deddly night shade plant.
Its main use is to dilate the pupil in pts with iris is
[Inflammation of iris goes into spasm & adheres to the lens of
the eyes causing blindness.]

*Therapeutic use –
It is commonly used as eye drops of 1% or 0.5% strength &
in the form of oixtment. It action last for 18 days & it is Not
reversible by means of miotics. It is therefore unsuitable for
dilating the pupil for fungal examination.

#Adverse effect –
Acute angle closure glaucoma in pts with narrow anterior
chamber angles. This will not respond to miotic treatment & will
almost certainly require an emergency operation.

(2) Ham atropine –


It is a homologue of atropine, can be used in 1% or 2%
strengths. It produces pupillary enlargement in 5-10 minutes
and its effect lacts for 24 hrs.

(3) Cyclopentolate:-
A synthetic drug commonly used as a mydriatic &
cycloplegic for sight tests in young children. It has a very short
duration of action [about 4 hrs.] Its action is reversed by
physostigrnine eye drop.

(4) Tropicamide –
Short acting mydriatic. It is a rapid pupillary dilator, is a
week cycloplegic & cause less blurring of vision.
It is therefore useful for clinical fundal examination as it has
only a side effect on the pt’s ability to read afterwards.

#Sympathomimetic Drugs –
A typical drug is phenylecphrine, used as eye drop in 10%
strength.
- Ephedrine is another & also cocaine, which can be combined
with homatropine to make up guttae ‘H’ & ‘C’.
The cocaine is used at a connection of 2% which is sufficient for
it to be a controlled drug.
Sympathomimetic drugs can be used synergistically to assist
those of the ant muscarinic group in cases where dilation is
difficult.

MIOTICS:-
Miotics drugs all act on the sphincter muscle of the iris, either
directly or indirectly constricting the pupil.
i) Pilocarpine is used to treat chronic glaucoma. It is available in
strengths of 1-9% in the form of eye drops.
ii) Eathiophate is a synthetic miotic which has been widely used
when strong pupillary constriction is required.
- It’s prolonged use produces cysts of the iris epithelium which
may largely oculude the small miotic pupil, there by severally.
Reducing vision. It can now only be used under expert
supervision.
- Acetylcholine is used during intraocular surgery such as
cataract extraction where a rapid miosis may be required.
- This can be achieved by the injection of acetylcholine directly
into the anterior chamber.
- It is marked as miochol – E, a dry powder in a sterile ampule
containing its own diluent fluid.
- Mixing is done by breaking on inner seal but as the
preparation has limited stability. It should be made up just
before use it’s affect is dramatic but short lived after the
insertion of an iris – supported acrylic replacement’s a longer
acting miotic is often admirable.

#Anti Infective Eye & Ear preparations –


(1) Sulpha Acetamide Sodium –
It is white, colorless crystalline watery soluble compound
having the bitter taste.
It is we topically for controlling the infection of eye & ear.

MOA:-
It inhibit the bacterial cell wall synthesis & kill them, it have
bactericidal action.

Indication –
1. Corneal ulcer – Conjunctivitis
2. Pre & post operative opthalamic surgery.
3. Blepharitis [Eye lids inflammation]
4. Opthalamic Neonaturum.
#Dose:- 1-2 drop in the affected eye or both eyes 5-6 times a
day.

#Contraindications –
- Hypersensitivity
- Local Redness – Irritation, Itching & burning of the eyes.

(2) Nor Floxacin eye & ear Drops –


It is a brand spectrum antibiotic drug of Quinolana drugs.
It is used locally to control the infection of eye & ear.

MOA –
Locally it control the bacterial infection it inhibit enzymatic
activity & required for bacterial cell wall synthesis & kill them.

Indications –
- Pre & post operative surgery of eye.
- Conjunctivitis.
- Keratitis, corneal ulcer, mastoid surgery otitis externa, chronic
supportive otitis media.
Dose –
- For acute eye infection:- 1-2 drop in affected eye ½ hourly.
- For moderate eye infection – 1-2 drop 3-4 hourly.
- For ear infection – 1-2 drops in the both ears 3 hourly.

(3) Ciprofloxacin ear & eye Drops –


- Ciproflaxacin is a broad spectrum antibiotic.
- It is used in otitis media, mastoid surgery procedure before the
surgery & chronic supportive otitis media.
- It is prepared in eye & ear drop preparation.
Dose – 1-2 drops in the affected eye 2-4 hourly 2-3 drops 4
hourly in the bath affected eyes.

Contraindications – Hypersensitivity.

Side effects –
- Local redness, Itching, burning of eye & ear.

Chloramphenicol:-
- It is a brand spectrum antibiotic.
- It effective against gram +ve & gram –ve bacteria.
- Administration of chloramphenicol in the pregnant female
may cause “Grey baby syndrome” in the developing fetus & also
in neonates.
- 2-5 drops or 1 occular 2-4 times a day of capsule to central the
severe eye infection.

Soframycin & Tobramycin:-


- It is also belong to aminoglycosides category of the drugs.
- It has antibacterial action, effective again gram+ve & -ve
bacteria.
- It’s ear & eye preparation more effective against ear & eye
infection.
- These drugs also may be used in the combination with steroid.
- 1-2 drops in affected eye part 3-4 hourly.
- 2-3 drops in the affected ear 3 hourly are most commonly
used.

Gentamycin:-
It is aminoglycoside category drug which is very cheap &
potent.
- It has antibacterial action.
- It is preparation used for the treatment of infected eye & ear.
- 2-3 drop in affected eye 3 hourly.
- 2-3 drop in both ear 3 hourly.

Steroidal eye drop –


Steroidal eye drops are these local preparation which may
contain steroids only & these preparation are also in
combination with antibiotic preparation.
- An steroidal preparation have anti-inflammatory effect so it
effectively control eye infection, they may contain
betamethasone, beclomethasone & Dexemethasone
preparation dose varies from 0.1-1%.

Indications –
Severe occur infection which are not controlled by planned
topical antibiotic.
Dose – 1-2 dropin the affected or both eye for 3-4 times a day.
Contraindications – Decrease immunity of host because
steroids decrease circulating WBC count.
- Hypersensitivity

Side effects –
- Itching, redness, Burning of eyes.
- Delayed healing of wound in eyes if any.

#Drugs used for Nose –


Drugs may be instilled into the nose. It must be
remembered however, that their effect is every transient, the
cilia lining the nasal cavities completely remove them about 20
min, Further more medication with strong solutions of
antibiotics or vasoconstrictors will pralyse the cilia & thus
impede rather than help the of injected material from the nasal
cavities.
#Applying Nose Drops –
Nose drops are best gives us follows.
The pt. should lie back on a couch or bed with his or her head
extended over the end. About 5 ml of appropriate drops is
instilled to breath through the mouth. Thus closing the nose &
holding the nose drops in the nasal cavities. This position should
be maintained for 5 min. this method of administration may be
too strenuous for elderly pts. There are a no. of nose drops in
use among the most useful is ephedrine nose drop.

#Epheditine Nose drops –


It is useful in sinus infection because the ephedrine causes
shrinkage of the swollen & inflamed mucosa & thus clears the
nasal airway & allows proper drainage from the nasal sinuses.
Overuse, however may damage the delicate ciliated epithlium
lining the nasal passage & the drops should not be used for
more than a week.

#Drug interaction –
Ephedrine nose drops should not be given to pts taking
monoamines oxidase inhibitors [MAOIS] or within 2 weeks of
stopping the drugs, owing to the risk of a hypertensive crisis,
corticosteroids [B-metasone 0.1%] can be given as Nose drops
two or there times daily or Beclomethasone is available as a
nasal spray, the dose being two sprays into each Nostril twice
daily.
- Sodium cromoglycate can be given as a Nasal spray, as drops
or as an insufflation.

*Allergic Rhinitis –
It can be treated locally with preparations which relieve
congestion or by oral antihistamines. Local steroids appear to
be the most effective.
- Azetastine, which is an antihistamine also be given as a Nasal
spray local antibiotics have little place in the treatment of Nasal
infections, but a cream containing chlorhexidine & Neomycin
[Naseptin] can be applied locally in pts who are carriers of
stephylococus, especially MRSA. This is a wise procedure in
these pts before they undergo surgery since it may reduce the
risk of cross infection to other pts.
- Mupirocin or polyfax ointments are used for the eradication of
MRSA.

Ephedrine Nasal drops 0.5% W/N


Although the instilling of drops into the ear may be useful in
relieving symptoms, It is often done without any consideration
of the underlying disease & thus proves fruitless & sometimes
even dangerous.
The use of ear drops will be considered under individual
disorders of ear which can be helped this method of treatment.

#Instillation of drops –
1. Warm ear drops to approximately blood heat.
2. The head is turned so that the affected ear is uppermost.
3. Discharge is gently mopped away.
4. Two or there drops are instilled & the head is help in position
for a minute or two.
#Wax in the ear –
Way may become hard & impacted in the ear & may resist
effort to move it by syringing. A 50% solution of sodium
bicarbonate or warm almond or olive oil instilled for a few drugs
will usually it satisfactorily.

*Otitis externa –
Severe infection is best managed with expert guidance as
regular aural cleasing & medication is required.
Ear drops will only be effective if the meatus is cleared of
debris. The following agents may be used three times daily if
bacterial infection is suspected.
1. Clioquinol 1% with flumetasone 0.02% [Locortenvioform] has
a mild antibacterial & antifungal action, but stains the skin &
cloths.
Gentamicin 0.3% with hydrocoectisone 1% is anti-inflammatory
& antibacterial.
- Other combination of antibacterial drugs with steroids are
available.
The following precautions should be observed.
1. Treatment with antibiotic ear drops should not be contained
for longer time than 1 week owing to the risks of drug
sensitization & the development of fungal infection.
2. Gentamicin or neomycin ear drops should not be used if the
ear drum is perforated as deafness may result.

It eczema of the ear, local steroids should be used to reduce


irritation & inflammation prednisolone 0.5% or betamethasone
0.1% are satisfactory.

#Otitis media –
If the drum is not perforated the instillation of antibiotics
into the external ear is useless as it will not reach the site of
infection many infectious are viral & require only an analgesic.
Bacterial infections which are usually due to strep to cocus
pneumonia or haemophillus influenza should be treated by
systemic antibiotic. Amoxicillin is usually effective &
erythromycin can be used for those who are sensitive to
penicillin.
#Application of Drugs to the skin –
When drugs are applied to the skin, the term topical
treatment is often used.
A topical application generally consist of an active application.
The drug, in a base or vehicle. The type of topical application
that is used depends on the type & state of the skin disease & it
is just as important to use. The correct base as it is to use the
correct active agent. The base consist of one or more of the
following powder, water & grease.

#Ointment –
The distinction b/w modern ointment & Creams is no
longer so obvious because of the wide range of bases that are
used for both ointment & creams, ointments are generally more
‘gr easy’ & creams are thinner & consist of emulsions of various
types. These are of 3 types.
1) Water soluble ointments
2) Emulsifying ointment
3) Non-emulsifying ointment.

(1) Water soluble ointments –


These bases have the advantage that they do not stain.
(2) Emulsifying ointment –
These emulsify with water An example is lanolin [Hydrous
heal fat], which is still very commonly used. Prolonged use of
Non-medical grade lanolin in some pts can lead to sensitization
to the lanolin. These bases are useful for retaining active agents
in contact with the skin for as long as possible.
(3) Non-Emulsifying ointments –
These do not mix with water. The paraffin’s form the basis
of most of the very greasy ointments with the addiction of a
suitable active agent they are a good treatment of chronic, dry
skin discovered such as chronic atopic enzyme, psoriasis,
ichthymosis [dry skin with fish like scales]

#Creams –
Creams are emulsions which are either water dispersed in oil
[oil creams or oil dispersed in water [aqueous cream]]

The water are generally very acceptable to pts cosmetically &


are used to moisten & soften the skin surface.
- Barrier creams protect the skin agonist physical agents such as
water or sunlight.

#Pastes –
Pastes can be greasy or dying & they contain a large
amount of powder. They are particularly useful for localized
lesions.
Ex – In psoriasis in this disorder active agent should not be
applied to the Normal skin & therefore a paste is used for
abnormal areas. Pastes is used for abnormal areas. Pastes can
also be used to protect inflamed or excoriated skin & can be
applied very freely.
Ex – Compound zine paste.

#Lotions –
Lotions are used to cool acutely inflamed skin & may have
to be frequently reapplied.
Potassium permanganate lotions is very helpful for acute
exuding lesions of the hands & feet lotions cool by evaporation
& leave on inert powder on the skin surface.
- They are useful & safe for sub acute lesions.
Ex – Calamine.

*Dusting powders:-
Act as drying agents & increase the effective evaporating
surface. These are useful in the folds of skin. Tale, starch & zine
oxide are commonly used powders & active agents are added all
to need.
Eg. – Antiseptics for bacterial infections & antifungal agents for
athelet’s foot *Tinea paedis+

#Ingredients in preparations –
*The Base –
When formulating a skin preparation the first decision to
make I the type of base. That will be used many lesions derive
more benefit from the base than form the active agent. The
active ingredient to be added generally implies a diagnosis of
the skin disorder.
Preparation Sensitizer
1) Bexswax Isopropyl palmiatate
2) Benzyl alcohol Poly sorbates
3) Butylacted hydroxy Propylene glycol
anixole
4) Hydroxybenzoates
[Parabens]

*Active Ingredients –
Local Corticosteroids –
These are most widely prescribed & useful ingredients to
be added to various bases. They should not be used alone
where the cause of the skin disease is a bacterial, fungal or viral
infection as they may cause spread of the infection by lowering
local resistance. They are very useful for acute & sub-acute
disorder such as the eczemas & they are excellent for itching.

Eg. – Hydrocortisone 1%
Clobotasone butyrate 0.05%
Betamethasene Valve rate 0.1%
Clobetasol propionate 0.05%

Unit - 09
Drugs Acting on Nervous System

#NSAID’s *Non-steroidal Anti-inflammatory drugs, Anti-pyretic


Analgesics] –
Non-steroidal anti-inflammatory drugs are also called Non-
Narcotic, Non-opioid or aspirin like analgesics as they do not
depress the central nervous system & do not produce physical
dependence.
- Anti-inflammatory agents are drugs that alleviates symptoms
of inflammation but do not necessarily deal with the cause.
- Analgesics are drugs used to relive pain, also known as pain
killers.
- Antipyretic activity results in lowering the temp. & is
considered to involve the hypothalamus.

#Classification –
I. Non-selective Cox Inhibitors:-
1. Salicylates – Aspirin
2. Prop tonic acid derivatives – Ibuprofen, ketoprofen.
3. Fenamate – Mephenemic acid
4. Enolic acid derivative – Piroxican, Tenoxican.
5. Acetic acid derivatives –
Ketorolac,,Indomenthain&Nabumetone

II. Preferential Cox Inhibitors:-


1. Nimesulide
2. Diclofenae
3. Acelofenac

III. Selective Cox inhibitors:-


1. Celecoxib
2. Etoricoxib
3. Parecoxib

IV. Analgesics, Antipyretics with poor inflammatory Actions:-


1. Par aminophenol derivate – Paracentamol
2. Pyrozolone Derivate – Metamizol
3. Benzoxazoine Derivatives – Nefopam.

I. Non-selective Cox inhibitors:-


1. Salicylates –
#Aspirin – Aspirin is a salicylate that helps to relive headache,
muscular & joint pains & reduces inflammation.
- Acetyl salicylic acid has been considered the drug of choice in
the treatment of arthritis but it anti-inflammation action occurs
only when given in large doses [3-4gm/day] but at larger doses.
It produces side effects that are the main disadvantage when
they are used for treatment of arthritics condition.
- Non-steroidal anti-inflammatory drugs tend to be more
appropriate for arthritis condition.
- It is available in form of tablets.

#MOA:-
Aspirin inactivates cyclooxygenase irreversibly & inhibit
prostaglandin synthesis & platelet aggregation.

Indications –
- Used for pain & inflammatory condition such as Rheumatoid
fever, Rheumatoid arthritis, osteoarthritis, dysmanorrhocu&
symptomatic relief of the common cold pain & fever.

It is used for reducing the risk of recurrent transient ischemic


attacks [stroke] or MI/heart attack at low doses.
# Contraindication –
- Hypersensitivity to drug.
- History of asthma.
- Peptic ulcer pt.
- Bleeding disorders pt.
- Also contraindicated in children with chicken pox & dengue pt.
#Doses –
- 0.3 – 0.6gm, 6-8 hourly for minor pain.
- 4-5 gm or 75-100 mg/kg day in divided doses for 1-3 days &
after 4-7 days dose is reduce to 50mg/kg/day in case of acute
rheumatoid fever.
- 3-5 gm/day in case of rheumatoid arthritis.
- 60-100 mg/day in case of post MI & post stroke.
Child – Use not recommended, unless for certain conditions.

#Adverse effects –
- Dizziness cirehonism, skin-eruptions, epigastric, discomfort,
pepticulcer& bleeding hypersensitivity reaction.

*Salicylate overdose – Antidote sodium bicarbonate –


- Salicylate overdose can be fatal, particularly in children.
- Acute lethal dose is approximately 10-30 gm for adult & 4gm
in children.
- It requires immediate hospitalization.
- Pt. presents with symptoms of confusion, rapid deep
breathing, sweating, tinnitus in severe cases by
unconsciousness.
- Vomiting should be induced if possible (pt is conscious) with
syrup of in case.
- Activated charcoal can also be given as it decrease absorption
if given within 2 hour. After ingestion.

#NSG Responsibilities –
- Take with or after food to avoid GI disturbance.
- The ASA should not be used for self-medication of pain for
larger than 10 days in adults or 5 days in children unless
directed by a physician.
- Avoid ASA for at least 1 week prior to surgery.
- Pt. should inform the dentist or dr. of taking this medication
before doing any lab or dental work.
- Avoid alcohol while taking this medication since it increase the
risk of GI ulceration & bleeding.

3. Propionic acid derivatives –


#Ibuprofen:-
It has analgesics, anti-inflammatory effect Ibuprofen
inhibits platelets aggregation & prolonged bleeding time but
does not affect prothrombin or whole blood time.

Drug Plasma half life Dosage


Ibuprofen 2-4 hr. 400-600mg [5-10mg/kg]
Naproxen 12-16 hr. 250 mg BD-TDS
Ketoprofen 2-3 hr. 50-100 mg BD-TDS
Flubipuofen 4-6 hr. 50 mg BD-QID

#Pharmacokinetics –
Ibuprofen is well absorbed orally metabolized by liver &
excretion urine as well as bile.

Indications:-
- Dysmenorrhea
- Rhematoid arthritis, osteoarthritis
- Other musculoskeletal disorders
- Soft tissue injury fractures vasectomy, tooth extraction,
postpartum & post – operative surgery.
Contradictions –
- Hypersensitivity to Ibuprofen.
- Urticaria, rhinitis, bronchospasm.
- Angioedema
- Active peptic ulcer & bleeding abnormal.

*Adverse effects –
- Gastrointestine disturbance heartburn dyspepsia, Nausea,
abdominal distress, gastritis & ulceration.
- Dizziness, drowsiness, jaundice, fatigue epilepsy.

*NSG Responsibilities –
1. Drug should be precautionly used in pregnancy & with renal
& liver disease.
2. Closely observe the fluid retention & edema & history of
cardiac decompression.
3. Report immediate dark tarry stool, coffee cloured emesis,
blood & protein in urine.
4. Use of precaution if skin rash, itching headache, visual
disturbance, hypertension chronic renal failure.
5. Pt. do not drink alcohol.
6. Avoid Increased risk of GI ulceration & bleeding.

3. Fenamate –
*Mephenamic acid –
Analgesics, antipyretic & weaker anti-inflammatory drug.
Which inhibit the prostaglandin synthesis.
It is absorbed orally & excreted in urine as well as bile.
Indication –
- Muscle pain Joint pain & soft tissue pain.
- Dysmenorrhea
- Rheumatoid arthritis & osteoarthritis.
Dosage – 250 – 300mg, TDS.

Adverse effects –
- Diarrhea, epigastria distress, skin rashes, dizziness.

4. Enolic Acid derivative –


#Piroxicam –
Long lasting drug, antipyretics, analgesics & anti-
inflammatory drug.

Dose – 20mg, OD.


It is used for rheumatoid arthritis, osteoarthritis ankylosing
spondylitis, acute musculoskeletal pain & post-operative pain.

- GI intolerance, rashes, pruritus&edema side effects.

5. Acetic Acid Derivatives –


#Ketorolac –
Analgesics & anti-inflammatory inhibit the prostaglandin &
relieve pain it is rapidly absorbed after oral or In administration
&oxcretodin urine.

Dose –
15-30 mg IV or IM every 4-6 hr. Post-operative, dental &
acute muscle skeletal pain.
- 10-20mg, 6 hr. orally for management of pain.
- It can also be used in renal colic, migraine & pain.
- Nausea, vomiting, abdominal pain, dyspepsia, ulceration, loose
stool, drowsiness headache, dizziness, Nervousness & pain at
the infection site.

#Indomethacin –
It is a very potent aryl acetic acid NSAID derivative. It has
higher potential to cause serious side effect when used in high
dose.

It inhibit prostaglandin & well absorbed orally & excreted by


kidney.

Uses – Inflammation or tissue injury related pain.


Dose – 25-30 mg BD, qid in alkylosing spondylitis. Psoriasis,
arthritis & Rheumatoid arthritis.

IV, 0.1 – 0.2 mg/kg for 12hrs.

Contraindication –
Psychiatric pt., epileptics, renal disease, pregnant woman,
machinery operators & drivers.

Side effects –
GI & CNS side effects are common.
- Gastric irritation, Nausea, Anorexia, gastric bleeding, frontal
headache, mental confusion, Ataxia, hallucination, depression &
psychosis, Increased risk of bleeding.

IIPreferential Cox-2 inhibitors :-


Nimesulide :-
Nimesulide weekly inhibits prostaglandins synthesis & has
analgesics, antipyretic & anti-inflammatory action.
It is used in painful inflammatory condition like sports
injury, ear, nose & throat disorders, dental surgery, low
backache, post operative pain & arthritis.
It is completely observed orally & excreted in urine.

Side effects –
- Heart burn, nausea, loose motion, rashes, pruritus & dizziness.
- It causes hepatic failure so is banned in many countries like US,
USA, America.

*Diclofenae sodium –
Acetic acid derivative& has Analgesic, antipyretic & anti-
inflammatory properties.
Therapeutic dose it has little effect on platelet aggregation.
Pt. not responding to IBP can be given diclofenae instead.
Do not co administer with other NSAIDS or salicylates.

Uses–
Rheumatoid, osteoarthritis, bursitis, too thache,
dysmenorrhea, renal colic post-operative inflammatory
conditions.
#Dose –
50 mg TDS, then BD oral, 75 mg day. IM
#Adverse effect –
- Mild epigastria pain.
- Nausea, headache.
- Dizziness, rashes
- Gastric ulceration & bleeding.
- Increase risk of heart attack & stroke.

[Link] Cox inhibits –


#Celecoxib –
Similar to Diclofenae.
*Side effects –
- Abdominal pain.
- Dyspepsia.
- Mild diarrhea, rashes, edema.
- Rise in BP

It is used for osteoarthritis & Rheumatoid arthritis in a dose of


100-200 mg, BD

*Etoricoxib –
60-120 mg, OD for ostro/ Rheumatoid acute gouty arthritis,
ankylosing spondylitis, dysmenorrhea, acute dental surgery
pain.
Side effects –
- Dyspepsia.
- Abdominal pain, pedal edema.
- Risk in BP, dry mouth.
- Taste disturbances & par aesthesia.

IV. Analgesics – antipyretic with poor anti-inflammatory


action:-
# Para aminophenol derivatives –
#Paracetamol –
Analgesics, good anti-peptic anti-inflammatory properties.
It is equivalent to aspirin in relieving pain reducing fever, but it
has little effect on platelets function, does not affect bleeding
time.
It reduces fever by direct action on the hypothalamus heat
regulating center with consequent peripheral vasodilation,
sweating & dissipation of heat.
It is easily absorbed orally & is well metabolized by the
hepatic microsomal enzymes.
It is safe & well tolerated drug, nausea & rashes
occasionally occur due to it is intake.

*Indications –
Pain & fever.
#Contradictions –
Pt. with history of hypersensitivity.
- Pt. with severe liver & kidney damage.
#Dosage–
Tablets, capsules, suspension & suppositories.

#Nursing responsibilities –
- Do not exceed recommended doses.
- Chronic excessive use [>4gm/day] eventually may lead to
transient hepatotoxicity.
- It pain or fever persists for more than 3 days consult a
physician.
- use caution when pts are taking other drugs that might affect
the liver.

#Acute paracetamol poisoning –


It occur if large dose [>150mg/kg or 10gm in an adult] is
taken Acute poisoning symptoms include nausea, vomiting,
drowsiness, confusion, liver tenderness low BP, cardia
arrhythmia jaundice & acute hepatic & renal failure.

Treatment –
(1) Induce vomiting or gastric lavage done.
(2) Oral N – acetyl cysteine [150 mg/kg IV infusion over 15 min]
is a specific antidote for specific toxicity.

#Opioid Analgesics –
Opioid analgesics are mainly centrally acting [Brain & spinal
cord] which are used for severe pain.
The drugs used to alleviate moderate to severe pain are other
opiates [Derivate from the opium poppy] or opiate like.
[Synthetic drugs].
- These drugs are together as opioids.

#Classification –
(1) Natural opium Alkaloids –
i) Morphine
ii) Codeine
(2) Semisynthetic opiates –
i) Diacetylmorphine
ii) Pholcodeine
iii) Ethyl morphine
(3) Synthetic opioids:-
i) Pethidine
ii) Fentanyl
iii) Tramadol
iv) Methadone

1. Natural opium alkaloids –


I. Morphine –
*Pharmacological action:-
- CNS –
It is strong analgesics & depress respiratory center in dose
dependent manner.
- It has cloning effect.
- Cough center, temp., regulating center & vasomotor centers
are depressed by morphine.

- Cardiovascular system–
It causes vasodilation due to depression of vasomotor
center & histamine release.

- GI tract –
Secretions are used the due to reduction in movements of
water & electrolyte from mucosa to the Human. This results in
constipation.
- Urinary bladder:-
Tone of sphincter muscle & detractor muscle increased
which cause urinary urgency & difficulty in micturition.

-Bronchial smooth muscle –


Therapeutic doses have no effect. High dose may produce
constriction.

#MOA –
Opioids generally produce inhibition if neuronal activity &
inhibit the release of neurotransmitters.
- They activate descending inhibiting systems.

#Pharmacokinetics –
- Morphine is readily absorbed from all site of administration 7
distributes to all tissues.
- Morphine is poorly transported across the blood, brain barrier
[BBB] it is metabolized in liver & excreted in urine.

#Indications–
- Chronic pain arising from terminal illness can be relieved by
opioid drugs.
- Post operative pain.
- Diagnostic procedures.
- Myocardial infarction.
- Pre anesthetic medication [Fentonyl-derivative]
- Dyspnea
- Cough suppression [Codeine, Dextromethorphan]
- Diarrhea & dysentery.

#Contraindications –
- Decreased respiratory Reserve – Emphysema, Asthma.
- Biliary colic.
- Head injury.
- Reduced blood volume.
- Hepatic insufficiency.
- Consultant states.

#Acute Morphine poisoning –


- Toxicity develops with 50 mg morphine, induced IM & its lethal
dose is about 250 mg.
- Stupor or Coma, flaccidity, shallow & occasional breathing,
cyanosis, pin point pupil, fail in BP, shock & convulsions are
manifestation.
Death may occur due to respiratory failure.

Treatment –
Respiratory support & maintenance of BP are priorities.
- Nalaxone 0.4 – 0.8 mg IV repeated every 2 – 3 min is a specific
antagonist till the respiratory picks up.

*Physical dependency –
Abnormal physical state in which the drug must be
administered to maintain normal function.
- Physical dependence is manifested by with drawl symptoms
when administration of the drug is stopped physical
dependence is a powerful reinforce cement for continued drug
taking behavior.

Symptoms–
- 8-12 hours – Carination, Rhinorrhea, Yawning, sweating.
- 12-14 hour – Restless sleep

48-72 hours – Symptoms peak, dilated pupils, Anorexia,


Gooseflesh [cold turkey], restlessness, irritability, tremor,
Nausea, vomiting, intestinal spasm & diarrhea, muscle spasm.
- 7-10 days – Symptoms end.

#Codeine –
Codeine is less potent than morphine & is mainly used as
antitussive.
- It is effective orally & is well absorbed.
- It produces less respiratory depression & is less constipating.
- Codeine has less addiction liability & tolerance is uncommon.
- It is less potent [1.6] than morphine as an analgesics [60 mg
codeine – 10mg morphine]
- Duration of action is 4-6 hours, 10-30mg is the antitussive
dose.
- Constipation is the most common side effects.

#Meperidine or Pethidine:-
MeperidinePethidine is has similar properties like Morphine,
but is less potent than morphine.
- High doses of pethidine produce excitation & convulsion it has
less smooth muscle spasm &miosis than morphine & has little
antitussive action.
It has also Anticholinergic effects, which can cause dry mouth &
blurring of vision.

#Fentanyl –
It is 100 times more potent than morphine in analgesia &
respiratory depression.
- It has shorter duration of action.
- It is also used in anesthesia.

*Pentazocine:-
It is mixed agonist & antagonist & is less potent than
morphine.
- it will precipitate withdrawal in dependent individual & may
produce dysphonia.
- It can be given both pass metabolism.
- Its dose is 50-100 mg oral, 30-60 mg IM.
- It is commonly used opioid analgesia specially in post
operative& chronic pain.
- Sedation, sweating, dizziness, Nausea, dysphonia with anxiety,
Nightmares & hallucinations are its common adverse effects.

*Opioid antagonistic:-
(A) Naloxone:-
Eliminated first pass metabolism half-life, 60-100min.
Readily reverse the coma & respiratory depression of opioid
overdose.
- Rapidly displease all receptors bound opioid molecules.
- Therefore, it is very effective reversing heroin overdose given
orally it under goes first pass metabolism & is metabolized by
the liver.
- Hence, it is given IV in dosage of0.4 mg IV duration of action 3-
4 hours.

*Naltrexone –
It is another pure opioid antagonist & is more potent than
naloxone, orally, it is effective & has a longer duration of action
1-2 days used for opioid blockade therapy in post addicts.

Sedative Hypnotics –
Sedative –
A drug that subdue excitement & calm the subject without
inducing sleep through drowsiness may be produced.

Sedation refers to decrease responsiveness to any level of


stimulation is associated with some, decrease in motor activity.
*Hypnotics –
A drug that induce or maintain sleep similar to normal
erasable sleep.
This is not to be confused with hypnosis meaning a trans like
‘stent’ in which the subject become passive & highly
suggestible.

#Classification:-
Sedative Hypnotics

Barbiturates Benzodiazepines Newer non


Benzodiazepine
- Long lasting - Hypnotics - Zopiclone
- Shout acting - Anti anxiety - Zolpidem
- Ultra acting - Anti convulsant

[Link] –
Clinically useful barbiturate have been categorized into 4
groups based upon their duration of action.
- Long acting [6-8 hr] – phenoborbitone
- short acting [2-4 hr] – Pentobarbitene, Butobarbitene
- Ultra short acting – Methahexitone, thiopentan [10-30 min.]

MOA of barbiturates –
Act at several sites in the CNS

Interfere with transmission of impulse at synapse.

Decrease over all impulse transmission to the cortex.

Increase threshold for electrical excitation of motor cortex

Depress the respiratory center


- Pentobarbital [Nembutal]
- Phenobarbitone – [refer anti epileptics]

#Pharmacological action –
1. CNS – They produce dose dependent effects sedation sleep
anesthesia coma.
- Hypnotics Decreases time to get into sleep & Increases the
duration of sleep.
- Sedation if administered at day time can produce drowsiness,
reduction in anxiety & excitability.
- Barbiturates have anti convulsive properties also.

2. Respiratory system –
It gets depressed by the higher doses of barbiturates.
3. CVS –
They produce slight decreases in BP & heart rate. They can
also produce reflex tachycardia.
4. Skeletal muscles –
When used in anesthesia dose it can reduce muscle
contraction.
5. Kidney –
Decreases in BP can cause. Increase in ADH release & thus
reduces the urine output.
6. Pharmacokinetics – Drug is metabolized in liver & excreted in
urine.

-Preparations –
Capsule – 30mg, 50mg, 100mg.
Elixir – 20mg/5ml
Suppositories – 30mg, 60mg, 120mg, 200mg.
Injection – 50mg/ml
Usual Dosage Range–
Oral –
Sedation adult – 30mg, 3 to 4 times/day child – 2mg/kg to
6mg/kg/day.
Hypnosis adult – 100 mg
Rectal – Adult – 150 – 200mg, child – 25-80mg
IM [adult] – 150 – 200mg, child – 25-80mg

NSG responsibilities –
- Be aware that use for prolonged periods of time even at
therapeutic levels is associated with a high incidence of
addiction.
- Counsel chronic users to note & report that appearance of
sore throat, fever brushing, rash, Jaundice are signs of possible
hematological toxicity.
- When giving IV administer slowly to prevent respiratory
depression & hypotension.
Recognize that barbiturates given to pts in severe pain produce
anxiety & restlessness & may intensity, the person’s reaction to
the painful stimuli. Always given in combination with an
analgesic in the presence of pain.

II. Benzodiazepines [Antiepileptic]:-


They produces lower degree of neuronal depression than
barbiturates.
- Higher doses of hypnotics can cause respiratory depression,
but in lower doses, it does not affect body parts.

MOA –
Benzodiazepines enhances the effect of gamma – amino butyric
acid [GABA]by increasing GABA affinity for the GABA receptor.
- Binding of GABA to site opens the chloride channel, resulting
in hyper polarized cell mouth that prevents further excitation of
cell.
Indications:-
Benzodiazepines can be used as anti anxiety, muscle
relaxant & anti convulsion drug. It also help to hasten sleep,
reduce intermittent awaking & increase total sleep.

*Dose & Duration of action of some commonly used


hypnotics:-
Hypnotics Dose Duration

- Long acting –

Diazepam 5-10 24-48 hr.


Chlordiazepoxide 10-20 24-48 hr.
Nitrozepam 5-10 24 hr.
Atprozolam 0.25-0.5 24 hr.

Short acting –
Tricoolam 0.125-0.25 6
Micloolam 7.5 – 10 6
Lorezepam 1–2 12–18 hr
Temazepam 10 – 20 12–18 hr

Newer Agents –
- Zolpidem 5 – 10 4
- Zoleplen 5–20 4
- Zopiclene 7.5–10 4

*Adverse effects – Benzodiazepine’s are generally well


tolerated.
- The common side effects include drowsiness confusion,
amnesia, lethargy, weakness headache, vision, ataxia.
Day time sedation & impaired motor coordination such as
driving skills, therefore while on BIDS driving should be avoided.

- In somepts, it may cause paradoxical irritability & anxiety.

*Benzodiazepine antagonist –
*Flumazenil –
Flumazenil reverses the depressant & stimulants effects of
benzodiazepines.
It is absorbed orally on IV injection, it starts its action in
seconds & lasts for 1–2 hours.
It is used to reverse BID anesthesia effects within 1 minute
of an IV injection.
- In case of BZD overdose flumazenil 0.2 mg 1 min can be
injected till the pt. gains consciousness.
- It is sale & well tolerated drug by pts with little agitation &
discomfort.
[Link] Non-Benzodiazepine–
Zopiclene – It is the first Non – BTD hypnotics & is indicated for
less than 2 wks for treatment of insomnia.
It is given in dosage of 7.5 mg tablet one tab let at bed time
for not more than 2–4 weeks.
- It can cause bitter or metallic taste, Psychological disturbance,
dry mouth & impaired judgement.
*Zolippidem –
Zolippidium Increase the duration of sleep, but does not have
anti action, antianxiety & music relaxant effects.
- Presently it is one of the most prescribed hypnotics.
- Its dosage is 5–10 mg [maximum 20mg] at bed time, dose
should be decreased to half in case of elderly &pts with liver
disease.
- Side effects are less & even large doses do not depress
respiration.

Anesthesia – The term anesthesia is derived from the greek


word anesthesia which mean “no sedation.”
- Anesthesia is an artificially induced state of partial or total loss
of sensation with or without loss of consciousness.
- Anesthesia agents can produce muscle relaxation, block
transmission of pain impulses & suppress reflexes. It can also
temporarily decrease memory retrieved a recall.
- The depth & effects of anesthesia are monitored by observing
changes in respiratory, saturation & end tidal levels, heart
rate urine output & BP.

*Classification –
Anesthesia

General Anesthesia Local anesthesia

I General Anesthesia –
General anesthesia are agents that, in sufficient accounts
are capable of producing analgesia, decreased muscle reflex
activity & intimately loss of consciousness.
I. General Anesthesia –
General anesthesia are agents that, in sufficient amounts
are capable of producing analgesia, decreased muscle reflex
activity & intimately loss of consciousness.
General anesthetics are drugs that are bring about a state
in which painful surgical procedures can be perform painful &
safely.

*Stages of General Anesthesia –


#Stage of Analgesia:-
It is from the beginning of inhalation of the anesthetic to
loss of consciousness.
- Consciousness become progressively clouded.
- The pt’s awareness of sensory stimulus’s disrupted hearing &
other perception are distorted. Feeling floating & numbness.
- Analgesia [loss of pain sensation] may be profound with same
anesthetics for Eg. – Ether, Methoxyflurene

- Complete loss of consciousness marks the end of this stage.

#Stage of Delirium or Excitement –


Stage of delirium or excitement stage is from loss of
consciousness to beginning of surgical anesthesia.
Pt. is unconscious, but may show sign of psycho motor
excitement, which are the result of drug induced depression of
inhibiting areas of the CNS, Respiratory & cardiovascular
reflexes may be hyperactive. It may be associated with
excitement – shouting, crying & violent behavior.
*Surgical Anesthesia:-
Begins with a change from irregular to regular breathing &
a loss of eyelid reflexes.
- It is divided into 4 planes to indicate increasing depth of
anesthesia.

#Plane – 1 – Eyeball movement regular breathing.


#Plane – 2 – Eyeball fixed, breathing less, deep, full, skeletal
muscle tone reduced.
#Plane – 3 – Chest breathing shallow, abdominal respiration
deeper no wink response when the cornea is touched.
#Plane – 4 – Chest breathing stops, Abdominal breathing
become increasingly shallow.

*Medullary paralysis –
Respiration ceases cardio vascular collapse may occur if
respiration arrest is not corrected by resuscitative measures.

*Classification of general Anesthesia –


General Anesthesia

Inhalational Intravenous

Gas Volatile liquid Fast acting Slow acting


- Nitrous oxide - Doflurane - Thiopentone - Diazepam
Ether Halothane - Desflurane sodium
- Lorozepam - Seuoflurane - Methohexitene
- Ketamine sodium
- Fentayl - Propofol
- Etomidate

I. Inhalation Anesthetic –
MOA –
After inhalation

Rapidly enter in circulation

Blood stream then goes to

Central nervous system [CNS]

Causes muscle relaxation

*Nitrous oxide [N2O] –


- It is colorless, odorless, Non-inflammable & non irritating gas.
- It produces light anesthesia with minimal muscle relaxation.
- It does not cause significant depression of respiration or
vasomotor center.
- It has little effect on respiratory, heart & B.P. N2O (50%) has
been used with for dental & obstetric analgesia.
- Prolonged exposure to gas can depress bone marrow & can
cause peripheral neuropathy.

*Ether –
It is highly volatile liquid & can be inflammable & explosive.
*Halothane –
It is non-irritating, Non-inflammable, volatile liquid with
sweet odor.
- It is a direct myocardiac depressant.
- Cardiac output & B.P. start faling & heart rate may decreased
and it also causes respiratory depression.
- Pharyngeal & laryngeal reflexes are abolished early.
- It is preferred in asthmatic pts. It also causes intestinal &
uterine contractions.

Indications –
- Anesthesia, specially in pts with cus complication reduced
arterial tension or impending shock.
- Obstetrical analgesia.
- Induction anesthesia.
- Dental analgesia.

*Contraindications –
- Simultaneous use of adrenergic agents.
- Asthmatic condition.
- Use of electro coutery equipment during administration.

*Adverse reaction –
- Post operative, Nausea, vomiting, headache, bradycardia,
confusion, convulsions & cyanosis or its adverse reaction.
- Malignant hyperthermia is also possible.

#NSG responsibilities –
- During administering gases as inhalation anesthesia use
adequate precautions to prevent explosion when drug is
present.
- Be alert for sign of arrhythmias & have proper materials &
equipments on hand to quickly treat arrhythmias if occurs.
- Position pt. properly to reduce danger of aspiration of vomit
during administering nitrous oride.
- In pneumothorax pts, use cautions because pulmonary
pressure may be elevated with nitrous oxide.
- Do not administer undiluted [without O2] N2O for more then
few breathe.
- Hypoxia may occur if nitrous oxide is used in greater con.
[more than 80%] rany length of time.

*NSG Alert –
- Always pre treat pts with ant cholinergic agents prior to ether
anesthesia to reduce the volume of secretions produced by
anesthesia.
- Turn pt’s head towards one side to avoid aspiration of the
vomits us.
- Have vasopressin available treat hypotension if it develops.
- As with any general anesthetic remember that the sense of
hearing is one of the earliest to return during recovery avoid
remarks that may be upsetting to the pt during this time, even
though be may still be unconsciousness.
II Intravenous Anesthesia:-
*MOA – After injection of general anesthesia it goes into
circulation & rapidly taken up by brain where, it cause
anesthetic [effect].
- It is rapidly redistributed to other parts of the body. There for
within 5 minutes after injection barbiturate level of brain has
decline to about one half of its peak affined shortly [30-45 sec.]
after injection.
*Thiopentone sodium:-
It is generally used for induction because of rapid one set of
action.
- When it is injected IV (35mg/kg) as a 2.5% solution it produces
unconsciousness in 15-20 sec.
- It is poor analgesic & weak muscle relaxes Immediately after
injection BP. falls due to vasodilatation.
- If hypovolemia, shock or sepsis are present then
cardiovascular collapse may occur.
- It can also be used for rapid control of conclusions.
- Laryngospasm can occur after administration of drug, which
can be prevented by atropine premedication & administration
of surgical choline immediately after thiopentone.

*Methohexitone sodium –
It is 3 times more potent but similar to thiopentone.
- It has quicker & brief action usually within 5-8 minutes.
*Propofol:-
- It is used as IV anesthetic for induction & maintenance.
- It’s action starts within 15-45 see & lasts for 5-10 minutes.
- It does not cause bronchopasms & preferably suited for out
patient surgery.
- In sub anesthetic doses [25-50mg/kg/min] is the choice of drug
for sedating. Incubated pts in intensive care unit.
*Benzodiazepines –
Benzodiazepines, lorazepam & midazopam are used to
induce or supplement anesthesia.
- They cause sedation, amnesia & reduce anxiety, which are
beneficial in such pts.
- The BZDs may be employed alone in procedures like
endoscopies, reduction of fractures, cardiae catheterization &
cardio version.
- The BIDS are also used as preanesthetic medications.

*Ketamine:-
- It is also called dissociative anesthesia.
- It can cause profound analgesia, immobility & amnesia with
light sleep.
- pt unable to process sensory stimuli, but can open his/her eyes
& can do swallowing.
- Respiratory is not depressed but heart rate cardiae output &
BP are elevated.
- A dose of 1-2 mg/kg/IV or 3-5 mg/kg IM is given, it can be used
for short surgeries & burn dressing.

#Indications –
- Induction Anesthesia.
- Short surgical procedures with minimal painful stimuli.
- Induction of hypnotic anesthetic.
- Supplementation of other anesthetic.
- Aid to Nare analysis & nareosynthesis is in psychiatries
disorders.
- Production of tranquilization & analgesia for diagnostic &
minor surgical procedures.
Eg. Treatment of burn.

#Contraindications:-
- Latent or suitable porphyry.
- Absence of suitable veins for IV administration.
- Status Asthmatics.
- Sever CVS disease, myasthenia gravis.
- Increase blood urea, Increased ICP.

#Side effects –
Pain at injection site, intensified muscle tone hallucinations,
confusion, transient venous pain, myodenic skeletal muscle
movement respiratory depression, hypotension, tachycardia
arrhythmias, larhyngospasm & hiccough its common side
effects.

*NSG Responsibilities –
- Use only clear, colorless diffusions.
- Be alert for signs excess pain/swelling at the site.
- Follow diluting instructions carefully sterile water for injection
is the preferred diluents.
- Note that solutions in sterile water are suitable for up to 6 wks
at room temperature but saline or dextrose are stable only for
24 hr.
- Have appropriate resuscitative& respiratory aids on hand in
case of extreme respiratory depression.
- Observe vital signs carefully during administration.
- Give small test dose initially determine sensitivity.
- If shivering or facial twitching occurs warm pt. with blankets.
- Give IV injection slowly to minimize muscle rigidity.
- Recognize that fluids & vaso depression agents may be needed
to manage hypotension & agent available.

II. Local Anesthetics –


A local anesthetic is a medication that causes absence of pain
sensation.
- In the context of surgery, a local anesthetic creates an absence
of pain in a specific location of the body without a less of
consciousness as opposed to a general anesthetic.
*Classification:-
Local Anesthetics

Injectable Anesthetics Surface Anesthetics


1) Low potency [procaine] - Lidocaine
short duration
2) Intremediate (Lignocaine) - Cacaine
potency & duration
3) High potency, [Bupivaccine, - Benzocaine
Long duration Ropi vocaine]

MOA:-
Local Anesthetic
Not channel of local nerve memb.
Prevent the development of action potential as well as the
propagation of action potential
The nerve fiber will not be stimulated
Conduction via sensory as well as motor even
The autonomic stops

Indications –
Relief of pain, soreness, irritation & itching associated with
various skin & mucous memb. disorders.
Minor burns, rashes, wound, allergic conditions, fungus
infection, skin ulcer, hemorrhoids, fissures.
Production of corneal & conjunctiva anesthesia to facilitate
ophthalmic procedures such as gonioscopy tonometry removal
of form bodies & minor ocular surgery.
Production of infiltration nerve block, spinal epidural or
caudal anesthesia in surgery obstetrics or dental work.
Management of cardiac arrhythmias.
*Contraindications –
- Topical history of allergic reaction.
- Injection history of hypersensitivity, severe injection & heart
block.
- Procaine is contradicted in Methemoglobinemia.

*Common side effects –


Topical –
- Sensitization reaction stinging or burning in the eyes, allergic
contact dermatitis, with fissuring of fingertips, urinary &
cutaneous lesion, edema anaphylastic swelling, irritation
sloughing neurosis.

Injection – [Mainly due to systemic reaction.]


- CNS stimulation [dizziness, blurred vision, confusion,
irritability, convulsive.]
Followed by CNS depression, muscle twitching, Drowsiness,
unconsciousness, bradycardia, myocardial depression.
*Epidural/Caudal Injection –
May Provoke renal black, urinary retention, incontinence,
parenthesis, headache/backache.

(A) Cacaine
It is good surface anesthetic & rapidly absorbed from
squeal mucous memb.
It stimulates CNC & effect mood behavior of an individuals.
It also stimulates vagal center & causes nausea & vomiting.
Marked Increase in BP is seen along with pyrexia.
It can be induced during ocular anesthesia.
(B) Lidocaine –
- It can be used as surface anesthetic or injectable anesthetic.
- When injected it can block, nerve within 3 minutes &
vasodilation occurs at that area.
- It is used for surface application infiltration, nerve block,
epidural spinal & IV regional block anesthesia.
- It also works as an antiarrhythmic agent.
- Drowsiness, Mental clouding, dysphorrea altered taste &
tinnitus arits common side effects.
- Its overdose may cause muscle twitching, convulsions
arrhythmias, hypotension, coma & respiratory arrest.

(C) Bupivacaine –
It has longer duration of action & can be used for
infiltration, nerve block, epidural & spinal anesthesia.

*Uses of local Anesthesia –


(1) Surface Anesthesia –
It can be applied topically on mucous memb. Abraded skin.
- Loss of motor function is not seen.
- It’s onset & duration depends on the site drug its conn. &
form.
Eg – Lidocaine [10%] sprayed in the throat arts in 2-5 minutes &
produces anesthesia for 30-45 min.
- It is used for tonometry, surgery, Nasal lesions, stomatitis, sore
throat, tonsillectomy, endoscopies intubation, gastric ulcers,
burns & proctoscopy.
(2) Infiltration Anesthesia –
It is infiltrated under the skin at the time of operation to
block sensory nerve ending.
It’s onset of action is fast.
It is used in minor operations where area to be
anesthesized is less like in case of incision, excisions, hydrocele
etc.

(3) Condition block –


Area distal to injection is anesthesized & paralyzed. In this
after injecting local anesthesia.
Field Block – Subcutaneous injection of LA solution proximal to
the site tube anesthetized blocks nerve transmission in the
region distal to injection site – fur arm, scalp, arteries
abdominal wall & lower extremity are field block.

(4) Nerve block –


Injection of a solution of o/A about/around individual
peripheral nerve or nerve. Plexuses produces larger areas of
anesthesia with a similar amount of the drug than the above
technique.
- Anesthesia starts a few centimeters distal to the infection.

(5) Spinal Anesthesia –


In this LA is injected in subarachnoid space b/w L2 & L3 or L3
& L4.
- It’s primary site of action is Cuda equin which lower portion of
body is anesthetized paralyzed.
- It is used for operations on the lower limbs, pelvis, lower
abdomen.
Eg. – Prostatectomy, fracture, obstetric problems & cesarean.
- It is safer than genral anesthesia & produces good analgesia &
muscle relaxation without loss of consciousness.
- Respiratory paralysis, hypotension, headache cauda equine
syndrome, septic meningitis & nausea vomiting are its common
complications.
(6) Epidural Anesthesia:-
Local anesthesia is injected into the spinal extradural (SA)
space. It acts on the nerve roots while small ancounts diffur into
SA space.
- It is technically more difficult & comparatively larger volumes
of the anesthetic are needed.

(7) IV Reginal Anesthesia –


This type of anesthesia is useful for rapid anesthetization of
an extremity.
Limb is elevated to ensure venous drainage through gravity
& a tourniquet is applied to prevent the re-entry of the blood.
- A dilute solution of the local anesthetic is then injected IV.
- It diffuses into extravascular tissues.
- Onset of anesthesia is in 2 minutes because of the anesthesia
is used for procedures casting less than 1 hour.
- About 25% of the drug enters into the systemic circulation.
This type of anesthesia is generally used on the upper limbs
through it can also be used on the legs & the thighs.

NSG responsibilities –
- Do not inject local anesthetic into areas of injection because
effectiveness in greatly diminishes & systemic toxicity may be
enhanced.
- Use lowest dose resulting in effective anesthesia to minimize
dander to systemic effects.
- Give injection slowly to decrease danger in case of allergic
reaction.
- Place pt receiving spinal anesthesia proper position to avoid
diffusion of drug towards respire muscle.
- Counsel pts receiving spinalor epidural anesthesia that
sensation in tower areas of body may not return for an hour or
two. Be prepared to assist movement as needed.
- Use caution in giving solutions with vaso constrictors in pt.
with peripheral vascular disease of hypertension.
- Do not auto clave solutions of local anesthesia containing
epinephrine.
- Discard unused partions of solutions not containing
preservations.

*Cholinergic Drugs –
Cholinergic drugs are the drugs which have action similar to
that of acetyl choline [Ach]. They are also called as
Parasympathomimetic drugs. They act similar to the
parasympathetic nerve stimulation.
*Classification –
They are divided into two groups.
i) Esters of choline –
Eg. – Acetyl choline
Meth choline
ii) cholinomimetic Alkaloids –
Eg. – Pilocarpim.
Muscarine
*Acetylecholine [Ach] –
Ach is an ester of the choline. It was isolated from adrenal
medulla. It is a parasympathetic neurotransmitter. It has
following action.
A) Muscarinic action
b) Nicotinic action
c) Ant curare action

A) Muscarinic Action – The action of Acctyl choline produced on


the organs innervated by post ganglionic parasympathetic
nerves is called as muscarinic action.
- This action is inhibited by the atropine.
- The following actions are included in muscarinic action.

i) Action on smooth muscles –


The action of acctyl choline produced on the organs
innervated by post ganglionic parasympathetic nerves is called
as muscarinic action.
- This action is inhibited by the Atropine.
- The following actions are included in muscarinic action.

i) Action on smooth muscles –


Ach causes contraction of the smooth muscle of the GII,
Bronchi & urinary bladder.
ii Action on blood vessels –
Ach causes dilatation of the smooth muscle of blood
vessels.
iii Action on Heart – It produces fall in heart rate, decreases
face of contraction of heart, decreases cardiac output. In high
does, it may produce cardiac arrest also.
iv Action on the secretion – It increases all GI secretion like
saliva, gastric juice, pancreatic juice etc.

v) Action on eyes – Injection of Ach in Carotid artery produces


miosis [constriction of pupil]. It also causes spasm of
accommodation & decreases the intraocular pressure.

(B) Nicotinic action – This action is produced by the stimulation


of sympathetic & para sympathetic ganglion, skeletal muscles &
adrenal medulla. This action reasonable with administration of
Nicotin so is called as Nicotinic action.
- Large dosage of Ach after Atropine causes Tachycardia & Raise
is blood pressure.
It is Nicotin action of Ach.
- This action is blocked by Hexamethonium which is a ganglion
blocker drug.

C) Anti-Curae Action –
Ach while acting on the NMI Causes contraction of the
skeletal muscle. This action is opposite to that of curare, so
called as ant curare action. It is blocked by the curare.
Ach is not effective for any therapeutic purpose. It is only use
for experimental purpose.

#Cholinergic Alkaloids –
Cholinergic Alkaloids are these which either contain Ach or
have action similar to that of Acetyl choline.

Pilocarpin –
It is an active alkaloid obtain from “Pilocarpus
Microphyllus”. It has cholinergic affect. It have resustained
muscarinic action. It produces miosis & mainly used in the
treatment of glaucoma.
It is used in a dose of 1 – 2 drops in both the ages 4 to 8
hourly .

*Cholinergic drugs used in GI system & urinary system –


*Bethanechal –
Devoid, Myotonachol, urccholine, vosicholine.
Uses –
- Treatment of acute, non-obstructive urinary retention.
- Relief of post operative abdominal distention & paralytic ileus.
Dosage – Depends on types & severity of condition.
Adult – Per oral [PO], 10-30 mg, 3 to 4 times/day.
SC, 2.5 to 25mg, 3 to 4 times/day.
Children – 0.6 mg/kg/day in divided doses.

*Common side effects –


Sweating, flushing, salivation, abdominal discomfort.
*NSG responsibilities –
Administer when stomach is empty of given following
meals, nausea, vomiting can occur.

*Neostigmine [Prostigmin] –
Uses
– Relief of post-operative abdominal distention.
– In urinary retention.
Dosage – Urinary retention & abdominal distention 0.5mg 5C or
IV repeated every 3 hour.

Common side effects – Nausea, Diarrhea ram pins, salivation,


urinary urgency, sweating, muscle twitching.
Contraindications –
Intestinal or urinary obstruction, mega colon, Peritonitis,
acute peptic ulcer, hyperthyroidism.

*NSG responsibilities –
- Give Drugs before meals if pts. Experiences dysphasia when
eating.
- Keep careful rescrubs of pts daily conditions, nothing change
in muscles strength respiratory & BP, to assist in developing on
optimal therapeutic regimen.

*Anti choline Estrase Drugs or choline esterase inhibitor


drugs:-
Anti-choline esterase drugs are those group of drugs which
inhibit the action of acetylcholine esterase enzyme.
They are also called as Acetylecholine esterase inhibitors. They
inhibit the action of the enzymes which break the acetylcholine.
So accumulation of Acetylcholine occurs at the cholinergic site.
These drugs are mainly divided into two groups depending on
the mature of action of the drugs.

1) Reversible Anti choline esterase drugs –


Eg – Rhysostigmine
Neostigmune

2) Irreversible Anticholinesterase Drugs –


Di – Isoprophyl Fluorophosphate.
Tera ethyl pyrophosphate.
Pharmacogically only reversible anticholine esterase drugs are
used.
#Physostigmine –
It is an active alkaloid obtained from the plant physostigma
venosema. It is obtained from it’s seeds.
MOA – Physostigmine is a reversible Acetyl choline esterase
group of drug, it increases ach at the cholinergic nerve endings
so it’s action increases.

*Indications –
- To reverse the CNS effect of Diazepam.
- Hereditary Ataxia.
- Antidepressant
- Alzheimer’s disease

Dosage – IM/IV 2 mg
Contraindications –
- Hypotension
- Cardiovascular disorders
- Asthma
- Hypersensitivity.
- Diabetes mellitus
- Pregnancy
- Lactation

*Side effects –
- Headache
- Sweating
- Drowsiness
- Nausea & vomiting
- Diarrhea
- Cramps
- Bradycardia
- Anorexia
- Hypotension
- Respiratory depression
- Hypersensitivity reaction [rash skin, pruritis urticaria]

*Neostigmine:-
It is an anticholine esterase drug. It inhibit the destruction
of ach at the cholinergic nerve endings.
Indications –
- Myasthenia gravis
- Alzheimer’s disease

Doses – 15-30 mg daily orally, 1 to 5mg IV with atropine.


* Contraindications
Same as Physostigmine
* Side effects

*Atropine –
Atropine is a naturally occurring belladonna alkaloid.
Uses –
- To treat motion sickness.
- To treat bradycardia.
- As an antidote to cholinergic.
- As an antidote in insecticide poisoning.
- To stimulate many medullary centers vagal, respiratory,
vasomotor.
- To suppress rigidity & tremors in Parkinson’s.
- It cause vasodilation.
- To decrease sweat, salivary Tracheobronchial & lacrimal
secretions.
- It has a mild anesthetic action on the cornea.
- Relaxation of smooth muscles.

Dosage –
- Systemic:-
Adults:- 0.4 to 0.6 mg every 4-6 hours.
Children:- 0.01 to 02 mg/kg.

- Ophthalmic:-
Adult: 1 drop 1% 3 times a day.
Children: 1 drop 0.5 to 1% to 3 times/day.
For refraction 1 drop 1 hour before examination.

*Note – When injected into human during pregnancy atropine


has reported to increase the heart beat of fetus. Do not use in
children under 6 year of age.
*Anti Depressants Drugs –
These are group of drugs which are used for the treatment
of depression disorder they are also called mood elevators.
They may relieve the depression effects of temporary
situational stress.
The first antidepressants imipramine, a tricyclic &
iproniazid, a monoamine oxidose inhibitor were discovered in
the 1950. These drugs were found to have the side effects of
improving pt’s mood.
Anti depressants are the medication that prevent or relieve
depression. It is used to correct neuro chemical imbalances that
affect mood.
Antidepressants are also used for disorders characterized
principally by anxiety. They can block the symptoms of panic,
including rapid heart beat, terror dizziness, chest pains, nausea
& breathing problems they can also be used to treat some
phobias.
Anti depressants are used most widely for serious
depressions, but they can also be helpful for some milder
depressions, Antidepressants, although, they are not ‘uppers’ or
stimulants take away or reduce the symptoms of depression &
help the depressed person feel the way he/she did before he
become depressed.

#Mode of Action –
Antidepressants Drugs

Enhance the Neurotransmission of transmitter by blocking the


reuptake of neurotransmitters at pre-synaptic neurons.
Inhibit metabolism & subsequent deactivation & affect the
activity of the receptors on the post synaptic neuron.

Regulate the balance b/w the neurotransmitter.

*Classification –
1) Tricyclic Antidepressants :-
* Amitriotyline [Endep]
* Desipramine [Norpramin]
* Imipramine [Tofranil]
* Nor-triptyline [Aventyl]

2) Monoamine oxidose inhibitors –


*Tsocarboxazid [Morplan]
* Phenelzine sulfate [Narolil]
* Tranyl eypromine sulfate
* Eldepryl

3) Selective Serotonin Reuptake inhibitors –


* Fluvoxamine [Luvax]
* Fluoxetine [Prozae]
* Paroxetine [Paxil]
* Serative [zoloft]
* Citalopram
4) Atypical Antidepressants –
* Mianseril [Tetradep]
* Maprotiline [Ludiomil]
* Mirtazapine

1) Tricyclic Antidepressants –
- These are heterocyclic compounds used primarily as
antidepressant.
- The TCAS were first discovered in the early 1950s.
- They are named after their chemical structure which contains
three rings of atoms.

MOA – P.T.O

MOA –
Tricyclic Drugs

Block reuptake of Non-epinephrine & serotonin by neurons

Uptake centers has inhibition of ruptake at receptor site.

Antidepressant effet
*Indications –
- Major depression epidodes – unipolar & Bipolar.
- Secondary depression – Associated with organic syndrome.
- Panic Disorder/Panic attack.
- generalized anxiety.
- Eating disorder
- Pain.
- Other – Childhood enuresis, peptic ulcers, of reaction,
adjustment disorders.

#Contraindications –
- Arrhythmia/MI.
- Hyperthyroidism.
- Impaired Renal & hepatic function.
- Pregnancy & lactation.
- Not recommended for children under 12 year.
- History of Past seizures.
- BPH.

#Side effects –
- Dry mouth, constipation, urinary retention, blurred vision.
- Postural hypotension, tachycardia, arrhymia ECG charges.
- Drowsiness, sedation, delusion, delirium, tremors, speech
blockage, par aesthesia, atoxia, Akathisia.
- Nausea, vomiting, loss of appetite.
- Skin rashes, jaundice, leukocytosis, eosinophilia.
- Hyperglycemia, Hypoglycemia.

#Special Considerations while Administration


- Caution the client to be careful working around. Machines,
driving cars & crossing streets because of possible altered
reflexes, drowsiness & dizziness.
- Refrain the client from drinking alcohol as it can block the
affect of anti depressants drugs.
- Advise the client to take full dose at bedtime to reduce the
experience of side effects during day time.
- Sudden stoping of TCAS. Can give rise to symptoms like
nausea, altered heart rate nightmares, cold sweats.
- Inform the client & relatives that mood elevations may take
place for 7-28 days.

2) Monoamine oxidase Inhibitors [MAOTs] –


These drugs are not widely used at they have dangerous side
effects. They can cause death due to severity of interaction.
These drugs are generally used when the TCAs fail.

MOA –
Increase amount of nor-epinephrine.

Release Catecholamine

Release of large amount of Nor-epinephrine to react with


receptors

Antidepressant effect.

*Indications –
- Panic disorder or Anger.
- Social phobia.
- Generalized anxiety disorders.
- Observe compulsive disorder [OCD]
- Post Traumatic stress Disorders
- Building Nervosa
- Parkinson Disease.
- Hypersomnia.

#Contraindications –
- Hypersensitivity.
- Pheochromocytoma [Adrenal gland tumor]
- Congestive heart failure.
- Severe hepatic & renal impairment.
- Hypertension.
- Pregnancy & lactation.
- Not use in age above 65 years.

*Side effects –
Orthostatic hypotension, wt. gain, edema, constipation,
urinary hesitancy vertigo, weakness, fatigue, change in cardiac
rate & rhythm, sexual dysfunction.

*Adverse effects –
Intracranial hemorrhage, hyperpyrexia, convulsions coma,
Tremors dryness of mouth, blurred vision, death.
#Alcohol particularly beer & wine, aged cheese, chicken liver,
bananas, spinach, tomatoes, coffee, chocolates, tea should be
avoided while using MAOTs.
# Overdose of MAOT’s can cause hyperthermia hypertension.
Tachycardia, dilated pupils, hyperactive reflexes, involuntary
movement of face & jew.

3) Selective serotonin Reuptake Inhibitors –


They have antidepressants affects as comparable to other
classes of antidepressants effects without significant
cardiovascular, anticholinergic & sedative effects.
- These drugs are specific to serotonin & have little or not ability
to block the other receptors. They are fairly safe in over does.

*MOA –
SSRIs

Block the reuptake of serotonin into pre – synaptic cell from


which it originally released

Results in reduction in destruction of transmitter

Results in the in its connection at postsynaptic cell.

*Indications –
- Bulimia nervosa
- Hypochondriasis
- Premenstrual dysphonic disorder

#Contraindications –
- With simultaneous use of MAOIs.
- People taking pimozide [a Diphenylmethyl peuidine
depurative], analgesics, tramadol hydrochloride.

#Side effects –
Nervousness, over activation, drowsiness, Headache,
Insomnia, irritability, Anxiety, sleeplessness.

#Special Considerations while administration –


- Tell the client that these side effects are of short term.
- If the pt. cannot tolerate one of the SSPIs or receives only
minimal effectiveness, several choices can be considered.
- Pts should start at a low dose, which increased over a period
of 5-10 days.
- Side effects usually diminish within 1-4 week exceptions may
be weight gain & sexual dysfunction.

(4) Atypical Antidepressants –


It contains 4 rings of atoms are a closely related group of
antidepressant compounds.
*MOA –
Atypical Antidepressants drugs
Block the transporter site for nor epinephrine & serotonin

Thus Increase synaptic connection these Neurotransmitter.

Anti depressant effect


*Indications –
- Obsessive convulsive disorders.
- Major depressive disorder.
- Post traumatic stress disorder.
- Generalized Anxiety.
- Panic disorder with Agoraphobia.

*Side effects –
- Dry mouth, Constipation, sedation, light headaches.
-Tetracyclic drugs are less likely to cause sexual dysfunction,
significant long term. gain, sleep disturbances.

- Amoxapine can lead to cause –


Agitation, delirium, convulsions, hyperactive deep tendon
reflexes, bowel & bladder paralysis & over death.

*NSG responsibilities –
- Anti depressants can cause side effects but most of than are
mild & go away after taking the medicine.
- Taking an antidepressants at least smooth after gives better
feeding & can help keep away from getting depressant again.
- Pt. should start at a low dose, which is increased over a period
of 6 days.
- Pt. should see their doctor every 1-2 wks until substantial
improvement occurs.
- Anti depressants should be taken only in the prescribed &
should be kept in a away from children.
- When used with proper care, following the doctor’s
instruction, antidepressants are useful. Medications that can
central of the symptoms of physical of depression while laxis on
changing the life stressors that contributed to its cause.
.
*Anti-Anxiety Drugs –
Anxiety – State of uneasiness characterized by apprehension &
worry about possible events.
It is a collection of unpleasant feelings identical to a fearful
feelings experienced under conditions of actual danger.

Types:-
1) Exogenous anxiety.
2) Enologenous anxiety.
Anti-anxiety agents are the drugs which are used to treat
anxiety also called as anxiolytics & minor tranquilizers.
- A comprehensive classification of anti-anxiety drugs is below.
#Classification –
I. Benzodiazepine :-
i) Clonazepam [Klonopin]
ii) Diazepam [valium]
iii) Larazepam [Atium]
iv) Clabozam

II. Azapirones:-
i) Buspirone [Buspar]
ii) Ispapirone
iii) Anti histamines
- Hydroxyzine [Atarax]
iv) Propanediol –
- Meprobamate [Miltown]
I Benzodiazepines –
Benzodiazepines most commonly used now a days & is the
drug of choice used to treat anxiety.
- It includes – Diazepam, chlordiazepamxide, alprazolam,
clonazepam, lorazepam & oxazepam.
- It has high – therapeutic index chance less suicidal potentials.
- It has lower abuse liability, mild tolerance less marked
dependence & withdrawal symptoms.
- Diazepam also is used as a muscle relax out.

*MOA –
Speed of impulse from a presynaptic neuron is influenced by
chloride ion in postsynaptic neuron.

GABA released

Opens CI channels known as benzodiazepine GABA receptor CT


phase complex

CT flow in neuron

Cell become hyperpolarized

Reduces neuronal activity & leads to slowed nerve impulses

BDZ molecules attach to BDZ receptor & enhance GABA effect

Decrease calcium ion flow & slow/Stop impulses

#Pharmacatherapeutic –
Generalized Anxiety, sedative & hyponotic effects.
- Seizures disorder, major depression.
- Skeletal muscle spasm, insomnia, panic attack, preoperative
anxiety.

#Adverse Drug Reaction –


- Dependence in duration of therapy exceeds smooth.
- Birth defect if taken early in pregnancy.
- Excitement [Destructive behavior]
- Nauseal/vomiting, Diarrhea, epigastric pain, urinary
incontinence

#Diazepam –
It is available in the forms of tablet, injection & oral solution
it is rapidly absorbed from GIT meta bolized in liver & oxcreted
primitive in urine.
- It is used in anxiety, alcohol with drawn skeletal muscle
spasms & status opilepticus & is contraindicated in pregnancy &
hypersensitivity.

Dose –
Anxiety:-
2-10mg bid, oral capsule – 15-30mg moderate anxiety – IM,
IV – 2-5mg, repeat in 3-4 hour.
Severe – IM/IV – 10mg, repeat in 3-4 hr if needed.
Status epilepticus –
Adult – 5-10mg, if needed then repeat at 10-15 interval up
to 30 mg IV/IM.

*Adverse effects –
Drowsiness, Fatigue, Confusion, Headache, slurred speech,
blurred vision, diplopia, nausea, constipation Tachycardia,
Hypotension.
#Alprazolam:-
It is available in form of tablet & oral solution. It is oxidized
in liver & renal eliminations occurs.
- It is used in anxiety associated with depression & panic
disorder & contraindication in pregnant or breastfeeding
mother, pulmonary depression & hypersensitivity.

Dose – po – 0.25 to 0.5mg tid is used in anxiety disorder.


Adverse effects – Light headache, dizziness, depression
restlessness, Tachycardia, sedation.

#Lorazepam –
PO – 2-6 mg/day in divided doses.

#NSG responsibilities –
- Monitor for the possible side effects of drug.
- Tablet may be crushed before administration & taken with
fluid or mixed with food.
- Monitor intake & output ratio including bowel elimination.
- Alprazolam may be used without regard to meals.
- Provide family education.
- The client should –
* Not stop taking drug abruptly
* Not consume other CNS to depressants.
- Not take Non-prescription medication with approval from
physician.

II. Antihistamine –
* Hydroxyzine –
It is available in the form tablet & syrup.
- It causes CNS depression & can be used sedation & reactive
anxiety in doses of 25-100 mg tid or grid Po & 25-100 mg.
- Contraindicated in hypersensitivity & depressant.

*Adverse effects –
Drowsiness, Dry mouth, Dizziness, Blurred vision, Hypotension.

III. Proponediols –
- It is available in form of tablets & causes CNS depression.
- It can be used as sedative in PO 1-2 – 1.6 mg in 3-4 divided
doses & as hyponotic PO 400–800 mg.
- It is contraindicated in hypersensitivity pregnancy.

*Adverse effects –
Drowsiness, Dizziness, vertigo weakness, slurred speech,
Headache, Tachycardia, Hypotension, Nausea vomiting.

*NSG responsibilities –
- Meprabamate may be administered with food to minimize
gastric distress.
- Caution to avoid driving a car or engaging in other hazardous
activities until drug response has been determined.
- Instructed the pt. to take drug as prescribed.

IV. Azapirones:-
*Buspirones Hydrochloride –
- It is first Anxiolytic in new class of agents & is loss sedating.
- They are available in form of tablets & used. PO 5-10 mg Hd in
case of generalized anxiety states.
- It is contraindicated in breast feeding pts, impaired renal or
hepatic function & hypersensitivity.

*Adverse Drug reaction –


- Dizziness, light headness, insomnia, Tachycardia, palpitation,
Headache.

*NSG responsibilities –
- Instruct the pt. to take the last dose of buspirione several
hours before bedtime to prevent insomnia.
- Advise pt. to ask the physician to recommended an analgesics
if headache occur.
- Monitor pt. for adverse reaction & drug interaction during
buspirone therapy.
- Help the pt. to explore alternative methods for including sleep
if insomnia occurs such as warm bath or quit mediation.
#Anti Psychotics Drugs – Or Neuroleptics
The drugs which are used to control or treat major psychoses
are called as anti-psychotics drugs.
- They reduces agitation & disturbed behavior of the pt.
- Psychosis are serious mental disorder with distortion of
thoughts behavior & functional capacity to recognize reality &
perception.
- They have change in personality also.
Eg. – Schizophrenia.
Definition:-
The anti-psychotic drugs represented by several chemically
distinct groups of compounds are capable of improving the
mood & calming the disturbed behavior of psychotic pt without
causing marked sedation/habituation psychotropic drugs can
also be defined as chemical that affect the brain & nervous
system after feeling & emotion.

MOA –
Typical Neuroleptics like CPA, act by blocking the dopamine
D2 receptors in the CNS. Since dopaminergic over activity is
thought to be responsible for schizopem DA receptor blockage
helps.
Dopamine receptor blockage also is responsible for the classical
side effects of these agents.

#Classification:-
*Classical/typical Neuroleptics
1. Phenothiazines:-
- Chlorpramizine
- Triflupromazine
- Thioridazine
- Mesoridazine
- Fluphenazine

2. Butyrophenones –
- Haloperidol
- Droperidol
- Trifluperidol
- Penfluridol

3. Thioxanthenes:-
- Thiothixene.
- Chloroprothixene
- Flupenthixole.

*A Typical Neurolaptics:-
1. Clozapine.
2. Risperidone
3. Ziprasidone
4. Remoxipride
5. Olanzapine
6. Quetipaine
7. Anisulpride.

#Miscellaneous:-
1. Reserpine
2. Loxapine
3. Pimozide.

#Chlorpromazine:-
Pharmacological action –
* CNS – It reduces irrational behavior, agitation &
aggressiveness & controls psychotic symptom tology. It lower
seizure threshold & can precipitate fits in untreated epileptics, it
has D2 receptor blocking action.
*Local Anesthetic:- Like procaine, it has local anesthetic action
but has irritation action so not used for the same.
*CNS –
Neuroleptics produce orthostatic hypotension due to -
blockage action & reflex tachycardia. It has a direct myocardial
depressant effect like quinidine & some anti-arrhythmic action
also. In higher doses it directly depress heart & produce
electrocardiographic [ECG] changes.

*Skeletal Muscle –
In site of action in basal ganglia or medulla oblongata, it
reduces certain types of spasticity. However it does not have
direct effect on muscle fibers.
*Pharmacokinetics –
Single dose effects usually last 6-8 hours. The elimination T
½ is variable but mostly is in the range of 18-30 hours.
Therapeutic effects may be seen at 30-200 mg/ml. After
discontinuing the drugs metabolites are excreted in urine & bile
for months.

*Triflupromazine:-
It is mainly used as anti-emetic & is more potent than CPZ.
When injected it produces muscle dystonia’s in children.

*Thioridazine:-
It has anticholinergic action & incidence of extrapyramidal side
effects is low. It can cause cardiac arrhythmia & eye damage are
common side.
*Penfluridol – It is used for chronic schizophrenia & social
adjustment dosage is 20-60 mg oral [120mg maximum] once
weekly.

#A typical anti-psychotics –
*Clozapine – It is an effective antipsychotic & it has very low
incidence of extrapyramidal side effects [EPS] sedation is low &
no endocrine side effects, no galactorrhea & gyneconastia are
seen with its use. It is effective in patient is not responding to
chlopramazine [Resistant] cases. The most important
disadvantages with clozapine is that it may cause
Agranulocytosis in some pts. Which can be fatal.

Risperidone:-
It is most commonly used anti-psychotics. It blocks -
adrenergic & histamine H1 receptors 7 is effective against both
positive & negative symptoms of schizophrenia.

*Haloperidol – Haloperidol is a potent anti-psychotic with


actions similar to chloropremazine. It differs from
chloropromazine in that it has lever incidence of autonomic side
effects & is preferred in older pts.
Haloperidol is useful in acute schizophrenia & is the drug of
choice in Gilles Tourette’s syndrome & Huntington’s disease.

#Atypical Anti-psychotics –
The newer atypical anti-psychotics like clozapine & others
have the advantages of:-
1. Causing fever side effects – like less sedation & loss anti-
cholinergic side effect.
2. Being effective in suppressing both positive & Negative
symptoms of schizophrenia.
3. Being effective in.

#Clozapine:-
It is an effective antipsychotic. It has the following
advantages over CPZ & other typical antipsychotics.
1. Very low incidence of involuntary movement.
2. Sedation is low.
3. No endocrine side effects, no Galactorrhea & gynacomastia.
4. It is effective in pts not responding to conventional
antipsychotics.

Drugs Dosage
* Phenotiazines Adults –
(i) Chlorpumazine - Initially 50-100mg IM.
[Thorazine] - Maintenance 10-200 mg ever 4-6
(ii) Triflupromazine hour orally or IM.
[Vesprin] As required children [over 12]
*Eiperazines Adults:-
*20mg 3 times [80-100mg day in
hospitalized] children
* Dosage - 1.6mg 1kg/day
*Thioridazine Adults –
- Psychosis
- Initially 50-100mg 3 time/day.
- In 2- 4 divided dose
- Depressive neurosis
- Initially 25 mg 3 times/day
- Maintain 20-200mg/day in 3 to 4
divided doses children [1-2 year.]

* Thioxanthenes Adults:-
* Thiothixene [navane] - Oral initially 25-50mg, 3 to 4
times/day, increase to optimal
level [maximum 600mg/day.]
- Im 25-50mg, 3 to 4 time/day
substitute oral therapy as soon
as possible.
Children –
- Oral 10-25 mg, 3-5mg two 3
time/day, maintenance 20-
60mg/day in divided doses.
- IM over 12 year, same as
adult.
- Oral initially 2-5 mg, 2 to 3
time per day, maintenance 20-
60 mg day in divided doses.
- IM 4 mg to 4 times/day.
- Dibenzoxazepine - Initially 10 mg orally twice a
- Clozapine day. [Maximum 250mg/day]
[Clozaril] - IM 12.5 to 50mg every 4-6
hour to control acutely agiated
pt.
- Butyrophene - Oral 0.5 to 5mg two to
- Olanzapine time/day depending on
[Zyprexia] symptom [maximum
100mg/day]
- IM 2-5mg, repeat at 4-2 hour
interval as needed.

#Indications –
- Management of acute & chronic psychosis either organic or
drug induced.
- Control of manic phase of man depressive.
- Relief of severe nausea & vomiting.
- Control of intractable hicoups.
- Anxiety, apprehension & agitation.
- Somatic disorders or prior to surgery.
- Facilitation of alcohol withdrawal adjunctive treatment of
tremors & acute intermittent porphyria.
- Control of aggressive in disturbed children.

#Contraindications –
- Bone marrow depression.
- Blood dyscrosis.
- Parkinsonism
- Jaundice
- Liver damage
- Renal insufficiency
- Cerebral arteries derosis
- Coronary disease
- Circulatory collapse.

#Adverse reaction –
*CNS:- Hyperpyrexia, confusion, bizarredream, insomnia,
depression, cerebral edema, hyperactivity.

*Neuromuscular:-
Extrapyramidal reaction, dystenias Aksthisia, pseudo
parkinsonism, tardive dyskinesia, hyperflexia.

*Cardiovascular –
Tachycardia, fainting exchanges, cardiac arrest.

*Hematologic:-
Blood dyscrasis, ageanulocytosis leukopenia, leuko cytosis,
anemias, thrombo cytopenia, pancytopenia.

*Hypersensitivity
* Endocrine – abnormal lactation, breast engorgement,
gynecomestia, change in libido, amenorrhea, glycosuria,
hyperdycemia, increased appetite.

#Antiparkinsoniam Drugs –
Parkinsonism – Parkinsonism is a chronic, extrapyramidal motor
disorder with these manifestations defective posture & gait,
mask like face, excessive salivation & dementia may occurs. It is
not cured then it may progress into end state disease in which
the symptoms becomes worsen & includes inability to walk &
breathing difficulty.

Antiparkinsonian Drug

Drug Acting on brain Drug Acting on brain


Deminergic system chotinergic system
Depamine pressor: Central anticholinergic
Leuodopa, Biperiden, Antihistamines
Trihexyphenidyl

Antiparkinsonian Drug

Drug Acting on brain Drug Acting on brain


Deminergic system chotinergic system
Depamine agenists,
Bromocryptine, Ropinirole
MOA – B – inhibitor:
Selegilline, Resagilline

#Dopamine precursor –
*Leudopa – Leudopa is drug of choice for pt. having
parkinsonism, as it crosses the blood brain barrier (13BB) & is
taken up by the surviving nigrostriatal neurons. It is converted
to dopamine [DA] in the dopaminergic neurons in the striatum.

MOA –
• CNS – On administration of leudopa symptoms rapidly in
individual hypokinesia & rigidity resolves first followed by
tremors as well.
• CNS – It can lead to tachycardia, postural hypotension.
• Endocrine – They inhibit prolautine release.

#Pharmacokinetics –
Pharmacokinetic absorbed from small intestine & excreted
in urine.
*Adverse effects –
• At initiation of therapy – Nausea, vomiting postural
hypertension
• After prolonged therapy –
Dyskinesias, Anxiety depression, mania & mental confusion.
#Dose –
- Start with 0.25g bd after meals, gradually increase till
adequate response is obtained usual dose is 2-3g/day.
- It should be cautiously used in pts with ischemic heart
disease cardiovascular disease, peptic ulcer, hepatic or
renal disorders, gout & glaucoma.

#Peripheral Decarboxylase inhibitors –


*Carbidopa –
Carbidopa do not penetrate BBB & do not inhibit
conversion of leuodpa to DA in brain.
Nausea, vomiting & cardiac complications are less
prominent with its use. They are extracerebral dopa
teearboxylase inhibitors. It causes postural hypotension,
involuntary movements & behavioural abnormalities. The usual
daily dose of leudopa is 0.4 to 0.8 g along with 75-100mg
carbidopa, given in 3 to 4 divided doses.

*Dopaminergic Agonists –
*Bromocriptine –
Bromocriptine are ergot derivatives having dopamine
agonistic activity at receptors.
Bromocriptine is a partial agonist while pergolide is an agonist
at receptors.

Symptoms resolve within ½ to 1 hour of oral dose & lasts for 6-


10 hours. It causes vomiting hallucination, hypotension &
conjunctiva infection. It is used in dose of 1.25mg once at night
& increase up to 5 mg +DS.
*MAD – B inhibitor –
# Selegiline –
Selegiline has mild anti-partisenian action, but when
combined with levodopa its action prolongs. It causes postural
hypotension, nausea, confusion, psychosis, & is contraindicated
in pts with convulsive disorders.

Symptoms resolve within ½ to 1 hour of oral dose & lasts for 6-


10 hours. It causes vomiting hallucination, hypotension &
conjunctiva infection. It is used in dose of 1.25mg once at night
& increase up to 5 mg +DS.
*MAD – B inhibitor –
# Selegiline –
Selegiline has mild anti-partisenian action, but when
combined with levodopa its action prolongs. It causes postural
hypotension, nausea, confusion, psychosis, & is contraindicated
in pts with convulsive disorders.
# Selegiline –
It is given 5mg with breakfast with launch. Either along or
with levodopa after 2-3 days, levodopa dose is reduced to one-
fourth.
It is metabolized by liver into Amphetamine.
*Rasagiline –
Rasagiline is five time more potent longer acting & not
metabolized to amphetamine. It is given as 1 mg OD in the
morning.

#COMT inhibitors –
*Entacapone –
Entacapene is a catechol methyltransferase [COMT]
inhibitors, which acts as adjuvant to levodaps/caraidopa so they
enhances & prolongs its therapeutic effects for advanced
parkinson disroder. It is given in 200mg with each dose of
levodopa/carbidopa, maximum 1600mg/day.
Nausea, vomiting, dyskinesia, postural hypotension
hallucination etc are its adverse effects.

*Glutamate Antagonist –
#Amantadine –
Amantadine is an antiviral drug used for prophylaxis of
influenza. It enhances the release of DA in the brain &
diminishes the reuptake of DA. About 100mg bd is used in pts &
effect of single dose lacts for B-12 hours.

*Side effects [classic] –


- Bluish discoloration
- Edema ankles
- Insomnia, restlessness, confusion & Nightmares [serious
side effects].

#Central Antichalinergic –
It is DOC for parkinsonian. It is helps to releive tremor,
hypokihensia & rigidity are affected the least. Its efficacy is
lower than levodopa, but is cheaper & produce less side effects
than leuodopa. Impairment of memory, organic confusonal
states, blurred vision & urinary retention are its common side
effects.

*Mood Stabilizers:-
Mood stabilizer are the drugs used to treat mood disorders,
generally characterized by rapid unstable mood shifts
alternating b/w mania [Emotional highs] & depression [lows].

*Mood Stabilizers:-
These are a diverse group of drugs used primarily in the
treatment of bipolar disorders [manic depressive illness] &
other conditions related thematically through the presence of
mood abnormalities.
Eg. – [Mood swings, volatility [Violence & explosiveness],
impulsivity, impulsive aggression & affectivity unstable
personality disorders [Bordeline personatliy Disorder].

*Mood Stabilizers:-
In general, in bipolar disrorder, Mood stabilizers are more
effective in the memic, them the depressive phase of illness.
Mood stablizers [Also called antimanic drug] central the
mood swings or mood changes that are seen in bipolar mood
disorders. Lithium has been used for several decodes but
several antiepileptic's like carbomazepine, valproic acid &
gabapentin are now being tried.
*Classification:- Mood stabilizers have B classes.
1) Lithium – This is an alkali metal & is the oldest & best
known mood stabilizer.
2) Anti convusants –
These are atypical drugs used as mood stablizer with these
include carbamazepine, sodium valporate, lamatrigine &
gabapent.

*Classification:- Mood stabilizers have B classes.


3) Anti psychotics –
These drugs have been recently tried as mcod stablizers,
these include risperidone, topirancelar & olanzapine.

*Lithium:-
Lithium has been used for so year as a mood stabilizer. The
US food & drug administration [FDA] has authorized the
therapeutic use of lithium. It has given shown superior in
controling depression mania & long term mood stability.
MOA – subsititues for the there compromising the
ability of neurons to release, activate or respond to NIMS.

*Lithium:-
Based on recent findings it has been put forward that
inhibits hydrolysis of inotal – 1 – phosphate in neurons. As a
result, the supply of free inosital for regeneration of much.
Phosphatidylixositides is reduced. The inositides are the source
of inositol – 3 phosphate [IP3] & Diacylglyceol [DAG] which
directly lead to mobilization & protein kinase C activation
that produces. Response in neurons.

*Lithium:-
Lithium also stablizers channels & decreases Neurenal
activity via effects on secondary messenger systems, all of
which may add to its therapeutic profile.

*Lithium:-
Blocks the hydrolysis of inositol – I phosphate.

This reduces the supply of free inositol.

There is a decreased level of phosphatidyl inositides lowering


synthesis of & DAG.

Anobilization & protein kinase C activation is thus


inhibited.
Thus finally the neuronal response is supported

Thus finally the neuronal response is supported indirectly signal


transduction is dampened in overacting Neurons.
[Hyperactivative neurons may prefer, be affected.]

*Indications –
- Bipolar disorders
- Manic depressives psychosis
- Recurrent Mania.
- Cyclic depression
- Acute hypomania.

*Contraindications –
- Pregnancy & lactation.
- Cardiovascular disease.
- Renal impairment
- Thyroid disorders.
- Severe dehydration
- Psoriasis
- Hepatic disorders
- Obesity
- Diabetes
- Brain trauma.

Eg –
- Lithium carbonate [ ].
- Lithium chloride [Licl]
- Licl causes gastric irritation & thus less preferred.

*Dosage –
- Adults 900-1600mg/day.
- Therapeutic blood level of 0.6 to 1.2meq/L.
- Dose should be increase gradually 900-1.8mg/day starting
from 300mg/day.
- Children: 15–20mg in 2–3 divided doses to achieve blood level
of 0.4 to 0.5 meq/L.

II. Side effects –


• CNS – Headache, drowsiness, dizziness, ataxia, tremors,
seizures, confusion, slurred speech & restlessness.
Alter electroencephalography [ECG] in children.
• CVS – Hypotension, Circulatory collapse edema. Changes in
ECG, alter conduction system arrhythmias.
• Dermatological – Psoriasis, drying of hair, Alopeia, pruritus.

II. Side effects –


• GI – Dry mouth, metalic taste, nausea & diarrhea.
GVT – Polyuria, albuminuria, renal toxicity & edema.
• Systemic – Hyponatremia & leukocytosis.
• Other – wt. gain, tinnitus & blurred vision.
#Drug interaction –
• - Diuretics increase level in body. Furdsemid &
chlorothiazide.
• - NSAIDS increase in body.
• Eg. – Ibuprofen & celecoxib.
• - Antihypoertensive drug may worsen the side effects of li,
• Eg. – channel & ACE inhibitors.
• - Decrease the amount of
• Eg. – Caffeine & theophylline.
- Assess for minor li toxicity such as vomiting diarrhea, poor Co-
ordination & major li. Toxicity that is tremor timitus & severe
thirst.
- Monitor serum level weekly two-3times for first 2 months
& afterward once weekly.
- Monitor sodium & fluid intake, decreased & fluid intake
may lead to excesive level in the body.
- Monitor urine for albuminuria, glycosuria & uric acid.
- Assess the wt. & check for edema in legs. Ankles & wrists.
- Administer reduces dosage to elderly as they have decreased
renal & CV function.
*Pt. education –
- Advise client to monitor urine specific gravity.
- Educate & the inform the client about symptoms of minor
toxicity & major toxicity, provide a written document detailing
these effects.
- Tell the client about blood li levels.
#Anti epileptics or anti-Convulsant Disease
Anti epileptic drugs are those which are used to control
different types of epileptics.
Epileptics are a group of disorders of CNS characterized by
paraoxymal cerebral dysrhythmia leading to episode of seizures,
loss or disturbs of consciousness with or without body
movement.
Epileptic may occur due to idiopathic causes, in same cases it
may occur due to following causes.
- Head injury.
- Surgery to the head.
- SOL [Space occuping lesions]
- Intracranial tumors.
- Tuberculemia
- In elderly person due to degneration of Nurons.
- Antipileptic drugs include following.

i) Iminostilbune –
Eg. Carbamazepine, oxacarbonezepine.
ii) Aliphatic Carboxylic acid –
Eg. Valproic acid sodium Valprote.
iii) Hydentoin –
Eg. Rhenytoin
iv) Pregapalin

v) Benzodiazepines –
Eg. – Clenazipam
- Diazepam
- Lorazepam etc.
vi) GABA pentene.
vii) Barbiturates – Phenabarbitene
viii) New drugs like –
- Vigabatrin
- Topiramate
The folloiwng anti-epileptic drugs are commonly used
*Carbomozepine –
It is the most important & common used antiepileptic drug.
It is a white colorless, crystaline, water soluble compound
having a bitter taste,
The psychotropic action of carbamazepine helps the pt become
more sociable & to intogecate himself more easily into the
society. It prevent paragimal attacks of the pain in the
trigeminal neuralgia.
It control the release of Neutrauma mitters so decrease
convulsive actions. It also have a role in depression producing
sleep or tranquilizing action.
In DI, it rapidly decrease urinary volume & relieve the sense of
thirst.
*Indication –
To control different types of epilapsy like –
- Partial seizures
- Primary generalized epilopsy.
- Secondary generalized epilepsy with tonic clonic type seizures.
- MOP
- Trigeminal Neuralgia.
- DI etc.
Doses –
Initially 200mg OD or BD orally gradually increase to 400mg
BD or TDS.
#Contraindications –
- Hypersens
- Pregnancy
- Lactation
- A.V block
- Severe CVS disorders

*Side effects –
- Anorexia.
- Dryness of mouth
- Itching
- Headache
- Nausea, vomiting
- Dizziness
- Ataxia etc.

Valporic acid & sodium Valporate:-


- It is a broad spectrum anticonvuhion drug. It is more potent in
blocking the seizures. It also produces sedation. It inhibit the
restablishment of chronic experimental seizures & prevent it.
*Indications –
- Petit mal epioapsy.
- As adjust drug for grand mal epilepsy.
- Psycho-motor myotenic epilapsy.
Valporic acid & sodium Valporate:-
Doses –
Initially 600 mg/day in divided doses orally than gradually
increase 200mg per day at 3rd days interval until response
occurs.
*Contraindications – Same as carbamzapine.
*Side effects – Same as carbamzapine.

*Phenytoin –
It is an important anti drug. It depress the CNS & control
epileptic. It also control epileptic. It also control the release of
NIOs. from the CNS.
Indications –
- Grand mal epilepsy
- Psychomotor epilapsy
- Trigeminal Neuralgia
- Migocaines

Doses –
- 100 mg 2 to 3 times a day orally after meals.
- Contraindication
- Sides effects

#Pregapacin –
It is an analog of NIMs. It bind 2 subunits ressulting in
modulates of channels & reduction in the release of
excitatory NIMS like glutamine, Nor-epinephine, serotonin
dopamine etc.
It control different type of neuropathic panis in adults after
convulsion or epilapsy.

*Indications –
- Post epileptic pains.
- Neuro epileptic pains.
*Doses –
75-150mg orally per day.
- Contraindication – Same as carbamzepine
- Side effects – Same as carbamzepine

#GABA pentene:-
It is an analogue drug with GABA. It central neurophethic
pains in adults.
*Indications –
Neuropathic pains.
*Doses –
Initially 300mg orally OD, gradually it is increased to 300 to
600 mg orally TDS for effective control.
*Contraindication – Same as carbamzepine
* Side effects – Same as carbamzepine
*Management of status epileptics –
Status epileptics is a condition in which a seizure lasts for
more than 30 minutes or 2 or more seizure occur with recovery
of consciousness. It is a emergency condition.
- It should be managed by following way.
(1) Diazepam 10 mg IV bolus state followed by fractional doses
every 10 minutes larozepam can also be given in place of
diazepam in a dose of 0.1 mg/kg. body weight. IV, larazepam
has less redistribution on so it is more effective than diazepam.
(2) Phenolarbitone 100 to 200mg IM or IV or phenytoin 25 to
50mg/ml IV in suming saline drip [it should not be mixed with
glucose because it precipitus.]
(3) Thiopentone as general anesthesia [If the seizure it not
controlled.]
*General measures –
- Oxygenation should be done.
- Airway intubation should be done.
- Fluid & electrolyte balance should be maintain by IV assess.
- Cardiac care should be done.
- B.P. should be controlled.
- B/w sugar regulation euglycemia maintained.
- Isolate with the pt. in a dark & calm environment.
- Place him in a soiled cat bed.
- Treatment of the underlying cause should be done.
- Proper care of the unconscious the should be done.
*De-addiction –
#Drugs used in De-addiction –
Many drugs are habit fuming or additive. A person has
control over his/her choice to start asing drugs but once started,
the pleasurable effect of drugs makes one went to keep reusing.
Drug addiction is a condition characterized by compulsivness for
drug & abuse of drug which long lasting chemical changes in the
brain.
*De-addiction –
#Drugs used in De-addiction –
De addiction includes assessment, pharmacology
treatment, individual & family counseling psychotherapy &
follow up 2 rehabilitation.
Medications are used to contract withdrawal detoxici cation
relief of symptoms, reduce craving for drug & produce aversion.

Drug Indications Dose


Diazepam Sedation in Alcohol 5-10
& benzodiazepine mg
with drawal is also
helpful in detoxi
fication for other
drugs such as
amphetanies
cocaine & benzo
diazepines

Action
Long acting benzapine reduce anxiety & produce sedation
amnoxia & cause muscle relaxant.
Drug – Lorazepam
Indications – Alcohol detoxification with suspected liver
dysfunction.
Dose – 1-2 mg

Action – Short acting cause sedation amnexia & reduce anxiety.


Drug – Buprenorphine
Indications – Opioid withdrawal the detoxification
Dose – 4-16mg daily
Action – Suppress same withdrawal symptoms

Drug – Clonidine
Indications – Opioid withdrawal & detoxification
Dose – 0.1 – 0.2 mg every for 10 days the dose is tapered
Action – - 2 agonists symptoms tachycardia anxiety vomiting.

Drug – Methadone
Indications – Adjunct intratment of opioid dependence
Dose – 10-40 mg daily incrased up to 10mg daily, usual 60-120
mg daily.
Action – Effective orally route no is long time.

Drug – Thiomine
Indications – Alcoholism
Dose –100-150 mg/day.

Drug – Niotine chewingums


Indications – Severe tobacco withdrawsym.
Action- similar to nicotine in tobacco, but less effect.

Drug – Dissul firam


Indications – Adjunct in the treatment in the treatment of
chronic alcohol dependence.
Dose – Tablet 250mg, 0.75-0.25 gm daily
Action- Aldehyde dehydrogonous inhibitor

*Drug Addiction –
Drug addiction is a state in which an individual is not
capable of performing normal physical & mental function
without taking that particular drug or without the presence of
drug.
- The form drug addiction is now replaces by drug dependence.

*Drug Addiction –
The drug dependent person continuously take the drug &
substance for following reason
1) We want to escape from reality.
2) He want to have dreamy state.
3) He want to relax from stress & strain at the life.
4) He want to have new strangers & dangerous expriences.
5) He uses firstly for medicinal purpose.
6) He want to know curiously the action of the drug.
The following drugs causes CNS depends
(1) Narcotics –
Opium – Morphine
Heroin – Pathidine
(2) Stimulants –
- Amphetamin
- Tobacco
- Cocaine
(3) Sedatives –
- Tranquilizers
- Barbiturates
(4) Alcohol
(5) Hallucination
- Cannabias
- LSD [lysergic acid diethyl]
(6) Hypotics
- Methyquinolone [Methaqualone]

#Drug dependences is of two types –


1) Physical dependence –
In the physical dependence the body adopt the drug if the
drug suddenly withdrawal then withdrawal symptoms appear
such as pain, body ache, fatigue, anorexia, constipation, tremor
& clowding of consciousness.
- In the psychological dependence he is unable to perform daily
routine work without taking the particular drug.
- The drugs which are used to manage the drug dependence or
drug addiction are called de addiction drugs.

*Disulfiram –
It is most commonly used de-addiction drug in the chronic
alcoholic person. It is a white or colorless, odourless, crystaline
O soluble compound having the bitter taste.

MOA – Disulfiram is used as an aversion therapy in the pt. he


willingly want to leave the drinking of alcohol.
- Disulfirm inhibit the acitivity of enzyme oldchyde
dehydrogenase which is required for alcohol metabolism.
- It interfere oxidation apaddhyde formed as an intermediate
break down product of alcohol as a result aldehyde get
accumulated in the body it results in unplesant reaction after
ingestion of alcohol bleeding to nose vomiting.
*Indications –
Chronic alcoholic pt.
- Adjuvant therapy such as opium addiction.
*Dose –
Instruct the pt. not to take alcohol with disulfiram therapy
otherwise life threatening complication may occur.
The Disulfiram therapy should be given under psychrities
guidliness.
- Dose may very acc to wt. of pt. & chronicity of alcohol &
amount of alcohol consumption.
- The standard dose is following –
* On first day 800mg orally OD.
* On second day 600mg. Orally OD.
* On third day 400mg orally OD.
* On fifth day 200mg orally OD.
* On the sixth day 100mg orally OD on to be continue until the
therapy.
- The treatment can be given upto months to years
- Contraindications.
- Hypersensitivity
- Lactation
- Alcohol intoxificatd person
- Pregnancy
* Adverse effects –
- Headache
- Neurotoxicity
- Hepato toxicity
- HS reaction such as skin rashes pruritus & urticaria.
- Restlessness
Disulfiram Reaction –
- The adverse effect with occur in the pt. if disulfiram drug
should taken after or with alcohol are called disulfiram reaction.
- It should be simple reaction to life threatening complication.
- This reaction occur when the pt. take alcohol knowingly or
unknowingly after taking dissulfiram drug.
- It is characterized by flushing of face thrombing headache,
respiratory difficluties, palpitation, tachycardia, hypotension &
cardivascular disturbances.
In severe reaction there may be respiratory depression.
Myocardical infraction, acute congestive heart failure or even
death.
*NSG responsibilities –
1. Always administer in those of willingly avoid the consumption
of alcohol.
2. It should not be given to disulfiram intoxical person.
3. There should be about 12 hours gape b/w the alcohol,
consumption & dose administered.
Drug should be given cruched & powder form liquid.
4. Before starting the drug administration written consent
should be taken from the pt. & his family members.
5. Drug should be given once in a day the nurse because the
more chances of also not consuming.

Unit – 10
Drugs used in Cardiovascular System

THROMBOLYTIC FIBRINOLYTICS DRUGS:-


→ Thrombolytic drugs cause lysis of formed clots both artery and vein and restablish tissue
perfusion.

*Drugs –
→ Streptokinase
→ Urokinase
→ Atteplase (re-PA)
→ Reteplase

1. Streptokinase →
→ It is a bacterial protein produced by group C (Beta) hemolytic streptococci.

* Mechanism of Action –
→ It binds to plasminogen producing an ‘activator complex’ that lyses free plasminogen to
the photolytic enzyme plasmin.
→ Plasmin degrades fibuin clots as well as fibrinogen and other plasma proteins (Non-fibui
specific)

* Pharmacokinetics –
→ The T/2 of the activator complex is about 23 min
→ The complex is inactivated by ant streptococcal antibodies and by hepatic clearance.
→ It produces hyperfibrinolytic effect c se plasma fibrinogen levels for 24-36 hrs.
→ A prolonged thrombin time may persist for up to 24 hours due to the se in plasma level
of fibrinogen.

*Clinical uses –
→ Acute Nyocardial Infection
→ Pulmonary Embolism
→ Deep vein thumbosis
→ Arterial thrombosis or embolism
→ Occlusion of arteriovenous cannulae

*Side effects –
→ Bleeding due to activation of circulating plasminogen.
→ Hpersensitivity – rashes, fever

2. Urokinase →
→ It is an enzyme produced by the kidney, and found in the urine.
→ It is mainly used in the low molecular nt. Form of urokinase obtained from human
neonatal kidney cells growth in tissue culture.

*Mechanism of Action:- It acts on the endogenous fibrinolytic system converting


plasminogen to the enzyme plasmin that degrades fibrin clots as well as fibrinogen and
some other plasma proteins (Non fibrin selective)
→ Urokinase administered by intravenous infusion is rapidly cleared by the liver an
elimination hay life for biologic activity of 12-20 min.
* Clinical use –
→ For the lyses of acute massive pulmonary emboli.
→ Coronary occlusion
→ MI, Thromboembolism, Pulmonary embolism.

* Dose – 2.5 lac. IV over 10 min for MI


Pt ½ → 10-15 min.

* Side effects –
→ Bleeding gums
→ Epistaxis
→ Coughing up blood
→ se Menstural flow
→ Intra cerebral haemorrhage
Plasma Expandius:-
→ These are high molecular wt. substances c execute colloidal
osmotic (oncotic) pressure and when injured IV retain fluid in
vascular compartment this make then useful in conditions of
blood or plasma loss.
→ Desirable properties of plasma expandius →
→ Should exert oncotic pressure comparable to plasma.
→ Should remain in circulations and not leak out in tissues are
be too rapidly disposed.
→ Should not be pyrogenic or Antigenic.
→ Should not interfere grouping and cross matching of blood.
→ Should be stable, easily sterlizable and cheap.

*Substances of plasma expanders


→ Human Albumin
→ Dextron
→ Polygeline
→ Physiological saline or normal saline
→ Heptastich.
1. Human Albumin:-
→ It is obtained from pooled human plasma 100 of 20% human
albumin solution is osmotic equivalent of about 400 ml of fresh
frozen plasma or 800 ml of whole blood.
→ it can be used out regarded to pt’s blood group and does
not interfere coagulation.
→ it is free of risk of transmitting serum hepatitis because the
preparation is heat treated.

*Drugs –
→ Albudac (Inj. 10ml, Inj. Some, Inj. 100ml)
→ Human Albumin (50ml, 250)
→ Albumin (100 ml vial) 20%

*Dose →
→ Burn – Adult – 30 to 50 g/lt., use 5% initially then 25% 1 day
after.
→ Shock – Adult – 500 ml of 5% in 30 min.
→ Hypotrotrinemia – Adult 1000 – 2000 ml of 5% or 25-100g of
25% solution.
→ Hyporbilirubinemia/Erythromblastosis Fetalis 1g of 25%
solution/kg.

*Mechanism of Action
→ Exerts colloidal oncotic pressure when injured IV c pulls fluid
from extra vascular to Intra vascular spaces thus expands
volume of circulating blood thus maintain cardiac output.

*Indications
→ Restores plasma volume in Burns.
→ Hyperbilirubinemia
→ Hypoproteinemia
→ Hypovolemic shock
→ Cerebral edema
→ Cordiopulmonary bypass procedures
→ Nephrotic syndrome
→ Hepatic failures

*Contraindications –
→ severe Anemia
→ CHF Altered respiration
→ Pulmonary edema, Renal insufficiency Hypersensitivity.
*Side effects-
→ Allergic or Pyrogenic reactions
→ Fever, chills, urticarial, rashes, nousea, vomiting, tachycardia,
hypotension.

2. Dextron →
→ it is a polysaccharide obtained from sugar beat. It is available
in two forms dextrin to Dextrin – 40
→ Dextran is a complex, branched glucan (Polysaccharide made
of many glucose molecules) composed of chains of varying
lengths.
→ It is used medicinally as an antithrombotic to reduce blood
viscosity and as a volume expander in anemia.
*Drugs –
→ Nacrodex
→ Rheomacrodex
→ Gentron – 40, 75

*Mechanism of Action –
→ Exerts osmotic pressure on circulating blood.
→ Fluid shifts from extra vascular space Intravascular.
→ sed blood volume
→ Produces Plasma volume expansion of its highly colloidal
starch structure similar to albumin.
→ Dextron is slowly exerted by glomerular filtration as well as
oxidized in body over weeks.

*Dose –
Adult – Max 20ml/kg 24 hours
Children – not recommended

*Indications
→ Hypovolemic and endotoxin shock
→ CVA
→ Peritoneal adhesions after abdominal surgeries.
* Contraindications –
→ Severe Anemia, cardiac failure.
→ Pulmonary edema, Renal insufficiency.
→ Thecombocytopenia, Hypofibrinogemia
→ Bleeding, Hypersensitivity.

* Adverse effects –
→ Nasal congestion, Nausea, vomiting
→ sed urine viscosity, oliguria, Anuria.
→ sed specific Gravity of urine.
→ sed bleeding time.
→ Fever
→ Hypersensitivity.

Unit - 11
Supplementation Contradiction & Medical Treatment of
Pregnancy
Introduction –
Hormones are organic compound synthesize & release by
the endocrine gland. They act as chemical messanger which
performed either action directly on with the help of second
messenger on the largest cell.
These second messenger include cyclic adenosine
monophosphate, inositol phosphate, calcium ion etc.
They either stimulate or inhibit the activity of body cell to
performe desired action.
i) Protein nature Hormone –
These type of hormone are composed of poly peptide chain
or protein such as hormone of anterior pituitary gland.

ii) Peptide of amine nature hormone –


They are composed of amino acid such as thyroxin &
Adrenaline.
- Both protein & amine nature hormone mainly act through
receptor on the cell membranes.

iii) Steroid hormone –


- They are water insoluble but soluble lipid or fat solvent.
- They are mainly cholesterol derivatives & consist of a
cyclopentane pechydro phenanthren ring, progestron,
testosterone corticosteroid hormone [Gluco corticoid &
minerals corticoid]
- Hormonal disorder are of two type –
1) Those disorder which occur due to deficiency of a particular
hormone such as deficiency of insulin & thyroxin.
- The disorder of decreased secretion of hormones can be
managed which is prepared in the laboratory.
2) Disorder are caused due to excess secretion or over
production of a particular hormone, such disorder are managed
by inhibiting the production or by decreasing its effect on the
large cell like anti thyroid drug which are used to treat
hyperthyroidism, hypoglycemia drugs are used to treat
hyperglycemia & type 2nd DM.

#Hormone:-
Hormone is a substance of intense biological activity that is
produced by specific cells in the body & is transported through
circulation to act on its largest cell.

#Hormones & their body function –


Body function Major regulator Hormone
1. Availability of fuel Insulin, glucogen, growth hormone
2. Metabolic rate Tri-iodothygronine, thyroxin
3. Somatic growth GH, Insulin like growth factors.
4. Sex & Reproduction Genodotropines, androgens estrogen,
Progestin
5. Circulating volume Aldosteron, ADH.
6. Adaptation to stress Glucocorticoids Adrenaline
7. Calcium balance Parathormone, calcitonin Vid – D.

Types of Hormone –
Hormones are secreted by the endocrine or ductless gland.
There are –
All hormones are done in 1st year, anatomy & physiology.

*Placenta also secretes many hormones –


- Chronic gonadotropin
- Prolactin
- Estrigens
- Progestrone
- Placental lactogen.
- Chronic thyrotropine.

#Sites & Mechanism of Hormone Action –


Receptors Hormone
(1) At cell memb. Receptors
a) Through alternation of Adrenaline, Glucogen, TSH,
Intracellular CAMP. → FSH, LH, PTH, calcitonin
Antirational protein kinase A → ACTH, some hypothalamine
Regulation of cell function releasing hormones,
rd
acting as 3 messenger in vasopressin [ ]
some situations.
b) Through IP3/DAG generation
release of intracellular Ca+2
protein kinase C activation.
c) Direct transmemb activation Insulin, G-GH prolactin.
of tyrosine protein kinase –
Phosphorylation – Cascade –
regulating of various enzymes
(2) At cytoplasmic receptor Steroidal hormones
Penetrating cell memb. Glucocorticoids
Hormone combines with a Meneralo corticoid
cytoplasmic Androgens
Receptor – Exposes its DNA Estrogens
bindings domain – Migrates to Progestins
nucleus & binds to specific Calcitriol
genes – DNA mediated – m
RNA synthesis – Synthesis of
functional proteins.
(3) At Nuclear Receptor Thyroid hormones:
The hormone penetrates the Thyroxin
nucleus – combines with its Triodothyronine.
receptors – alters DNA – RNA
mediated protein synthesis.

#Hypoglycemic Agents –
Definition – Hypoglycemics are naturally occurring hormones
such as insulin, & chemical pharmaceutical products which are
aimed at lowering blood glucose levels.

*Classification –
*Insulin
1. Short-acting –
- Regular insulin or crystalline zinc insulin.
2. Intermediate actings –
- Nutral protamine Hagedorn [NPH] or isophane insulin.
- Semilente insulin.

3. Long acting –
- Protamine zinc insulin.
- Ultralente insulin.

#Oral Hypoglycemics –
1. Sulfonylurea –
*Generations – 1st
- Tolbutamide
- Acetohexamide
- Chlorpropamide
- Tolazamide

*Generation 2nd –
- Glibenelamide
- Glipizide
- Gliclazide

2. Biguanides:-
- Phenphormine
- Metmorphine
- Buformine

3. glucosydose – inhibitor
- Acarbose
- Voglibose
4. Meglitinides
- Rapeglinide
- Nateglinide

#Insulin & Anti Diabetic Drugs –


Antidiabetic drugs are those group of drugs which are used to
treat or central hyperglycemia in diabetic pt. they are mainly
divided into two group –
1. Insulin
2. Oral hypoglycemic drugs or agent.

#Insulin –
- Insulin is a poly peptide hormone produced by B-cells of is lets
of long erhan’s of pancreas.
- It contain S, amino acid.
- It’s molecute contain two poly peptide chain which are chain A
& chain B.
- Chain A contain 21 amino acid while chain B contain 30 amino
acid, both chains are linked by disulphid bond.
- The molecular wt. of insulin 6808.
- It is only hypoglycemic hormone in our body which decrase
blood sugar level.

MOA:-
Insulin act on specific receptor located almost on the body
cell except brain cells, liver cells, RBC.
- Hypothalamus part of the brain depend on insulin for glucose
uptake.
- These receptor are hetero tetrameric glycoprotein nature.
- They consist of two-extra cellular & two trans memb. & such
unit linked by disulphide bond.

Insulin bind to - sub unit & enzymatic changes occurs on &


sub units which either stimulate or inhibit action of other
enzyme involved in metabolic reaction. Insulin stimulate
glucose transport across the cell memb. & increase glucose
uptake.

#Pharmacological action –
1. Insulin helps in glucose uptake by the peripheral body cells.
2. It help in glucose deposition in the body cell by the converting
glucose into glucose – 6 phosphate by this glucose – 6
phosphate further breakdown of glucose take place.
3. It help in glycogenesis conversion of glucose into glycogen in
the liver & muscle.
4. It decrease glycogenolysis [breakdown of glucose into
glycogen].
5. It decrease the process of gluconeogenesis C formation of
glucose from the substances other than carbohydrate.
6. Insulin inhibit lipolysis in the adepose tissue & fanours by
triglyceride synthesis.
7. It enhances amino acid biosynthesis & inhibit protein
breakdown.
8. It increase transcription of nuclear endothelial lipoprotein
lipase enzyme, so, it increase the clearance of bad cholesterol &
prevent Atheros derosis.
9. It also helps in maintaining integrity of nerve.
Types of insulin –
(A) Depending on duration of action insulin is divided into the
following types –
1. Short – acting insulin –
- These preparation begins their action within 20-40 mins of the
dose intake, their action last for 3-5 hour or up to 6-8 hour.
Ex – Insulin lispro
Regular insulin
2. Intermediate Acting insulin –
Their action starting about 1-2 hour after the dose
administration & it may last for up to 20-24 hour.
Eg. Insulin zinc preparation
Isophane insulin or NPH insulin
NPH – Natural protamine Hegedone.
3. Longer acting insulin – Their action start within 4-6 hour after
the dose & which may last up to 24-36 hours.
Eg. – Protamine zinc insulin.
- Human insulin can also be use for the supplementation or
replacement formed after DNA recombinant technology they
are also costly then the other insulin preparation.
- Human insulin have a rapid subcutaneous action for short
duration of action, they are indicated in following conditions –
* Insulin resistance especially when due to presence of insulin
binding Ab.
* Allergy to conventional insulin preparation.
* Injection side lip dystrophy.
* Short term use of insulin in surgery trauma, infection & keto
acidosis in the diabetic person.
* Use of insulin during pregnancy.

Indication –
- DM [type – I]
- Hyperglycemic Coma
- Type – II DM
- Ketoacidosis

Dose –
Dose depend on severity & duration of type 1st DM.

#Contraindications –
- Hypoglycemia
- HS
- Pregnancy & lactation.

#Side effect –
- Hypoglycemia
- Convulsion
- Coma
- Injection side lipodystrophy
- HS reaction
- Hyper

#Tolbutamide
It is the 1st generation of sulfonylurea group of oral
hypoglycemic drugs.
- It is an odourless, colorless or white crystalline H 2O soluble
compound having bitter taste.
- It is easily absorbed from GIT when given orally.

MOA –
It is an anti-diabetic drug which mainly act on B-cells of islet’s
of Langerhans & increase the release of insulin hormone.
- It is ineffective in pt. with disorder of bull.
- It also improve the functioning of insulin hormone at target
cell.
- It is secreted in the milk so it may cause hypoglycemia in
breast food infant so it should be avoided during lactation.

#Indication –
Type 2nd DM.

#Dose – Orally 1gm before breast feed fast.

#Contraindication –
- After pancreactectomy
- H5 – Pregnancy
- Lactation
- Type – 1st DM
- Diabetic coma
- Ketoacidosis
- Disorder of B-cell.

#Side effects –
- Joint pain
- Hypoglycemia
- Renal impairment
- Nausea & vomiting.

#Glibenelamide –
- It is the 2nd generation sulfonylureas oral hypoglycemic drug.
- It is suitable only those pt. which suffering from type 2 nd Dm
who not respond to other oral hypoglycemia drugs.
- It is used either single or in combination with other oral
hypoglycemic drugs.

#MOA –
It mainly act on & cell of pancreatic islets, it stimulate the
secretion & release of insulin hormone from the B-cell.

Indication –
Type – II [DM]

Dose –
- Orally 2.5mg as a single dose at break fast.
- Maximum dose is 15mg/day orally.
- Dose of glipizide 2.5mg-5mg orally 30 min. before the meal.
- The dose of glipizide 30-300mg orally day.

#Contraindication –
Type – 1st DM
- Diabetic coma.
- HS – Pregnancy, lactation.

#Side effects –
- Nausea & vomiting
- Anorexia
- Restlessness
- Tremors & insomnia.

Metformin –
Metformin is an oral Biguanide group of anti-diabetic drugs.
Intolerance with alcohol may occur easily so, it should not be
consume along with alcohol.
It is a new & commonly used oral hypoglycemic drugs
combination with other drugs for effective control of blood
sugar level.

MOA –
Metformin inhibit hepatic glucose production & increase the
sensitivity of the peri-pheral tissue to the insulin hormone, so it
inhibit glycogenelysis, gluconeogenesis as well as increase
peripheral utilization of glucose so blood sugar level are
effectively controlled.

#Indication –
Type 2nd DM.
When other oral hypoglycemic drugs fails to regulate raised
blood sugar level.

Dose –
500mg orally 2 times in a day & it can be given up to
3gm/day.

#Contraindication –
- Lactation
- Alcoholism
- Hepatic disorder
- Renal disorder
- HS – pregnancy

#Side effect –
- Nausea & vomiting
- Tinnitus
- Vertigo
- Palpitation
- Hypotension
- Weakness
- Loss of consciousness
- It is is taken along with alcohol then adverse effect occur
which are uncontrolled nausea.
- Vomiting
- Palpitation
- Hypotension
- Loss of consciousness

- Other oral hypoglycemic drugs are less commonly used they


include –
- Repeglinide 1.5 – 3mg orally BD.
- Rosiglitazone 4-8mg orally BD.

- A carbose is a new anti-diabetic drug, it mainly act on


intestinal mucosa & inhibit the enzyme - glucose dose [which
increase glucose absorption.]
Inhibition of this enzyme decrease the glucose absorption, so
the level of blood sugar do not raised.
- 50-100mg orally.

#Pt. education –
- Develop individualized teaching plan based on client’s previous
knowledge.
- Teach all aspects of drug therapy & advice to take with food.
- Advise to take medication even if feeding well.
- Take any missed dose as soon as possible.
- Teach client & family about s/s of hypoglycemia.
- Teach how to test blood glucose level.
- Advise to avoid smoking & drinking alcohol.

#NSG responsibilities –
- Assess vital signs wt. condition of skin & nails. Serum & urine
glucose level & glycosylated Hb.
- Assess for long term complications r/t accoderate of
atherosterosis, retinopathy, nephropathy, Neuropathy,
impotence & gastro paresis.
- Consult with physician regarding insulin management. When
there is insufficient food intake or when client is NPO for
surgery.

#Thyroid drugs –
The follicular cells secrete two thyroid hormones T4 & T3.
The thyroid hormones are synthesized in the thyroid follicles as
a part of thyroglobulin molecules is a glycoprotein synthesized
by thyroid cells in case of hypothyroidism synthetic
preparations of thyroid hormones are given.

Preparations –
Heretic name Trade Name Dosage [Oral/IM/IV]
Thyroxin sodium Thyronorm 25-100mg
Levothyroxine Levothroid, Oral – 12.5-50 adults
leuoxyl, synthroid child – 2mg/kg/day
IV – up to 500
Liothyronine Cytonel 2.5-25 adult
maintenance-25-50
Liothix Thyrolar, Adult – 12.5 of T4
Euthyroid with 3-10f T3 with
child
Thyroid Thyror adult & children 7.5
– 15mg maintenance
60-120
Protirelin Reflect [TRH] IV adults 0.5mg
children – 7mg/kg
Thyrotropin Thytropar IM SC adult & child
10IV/day 1-7 day

#MOA:-
Both T3 & T4 penetrate cells by active transport & produce
majority of their function, combines with nuclear thyroid
receptors [TR]
- When T3 binds to ligand binding domain of TR, it heterodimer
zed with retinoid ‘X’ receptors & undergo conformation changes
releasing care pressor & binding Co-activator.
- This induces gene transcription production of specific MPNA &
a specific pattern of protein synthesis – various metabolic &
anatomic effects.

*Indications –
- Cretinism
- Adult hypothyroidism
- Myxoedema coma
- Non-toxic goiter
- Thyroid nodule
- Papillary carcinoma of thyroid

#Contraindications –
- Thyrotoxicosis
- Acute MI & CVD.
- Morphologic hypogenadism
- Nephrosis
- Uncorrected hypoadrenalism.
Caustionly use with angina pectoris, HIN, cardiac disease, renal
insufficiency pregnancy, DM, hyperthyroidism & mal absorption
syndromes.

#Side effects –
- Weight gain, vomiting, tachycardia.

#Adverse effects –
- Angina pectoris, coronary occlusion stroke & predisposed
client.
- Hyperthyroidism [over dose] & coma.
- Reaction to thioamides fever, itching & skin rash.

#Drug interactions –
- Thyroid hormone therapy may increase the requirement of
insulin in diabetic pts.
- With thyroid hormone larger dose of digoxin is needed for
digitalization.
- Thyroid hormone with increases the metabolism of Vit – K
dependent clotting factors.

#NSG responsibilities –
- Assess vital signs, BP, wt. & history of wt. change. Normal diet,
energy level, mood, subjective feeling & response to temp.
- In children, check height.
- Monitor thyroid function test, result & blood glucose levels.
- Assess for symptoms of stress that could lead to angina or
stroke.

#Pt. education –
- Teach client how to monitor pulse, wt. & height.
- Instruct to adhere to dosage schedule & intervals, emphasize
that therapy is lifelong.
- Immediately report any chest pain or other signs of aggravated
CVD.
- Explain side effects & related treatment.
- Caution client not to discontinue drug & to wear medical alert
identification.
- With radio active iodine explain that most clients become
hypothyroid & require replacement therapy with thyroid
hormones, urge periodic thyroid evaluation.

#Thyroid inhibitors –
These are the drug’s use to lower functional capacity of
hyperactive thyroid glands, used to treat hyperthyroidism that
is the states of hyperactivity of the thyroid gland with
overproduction of T4 & T3, this state is observed particularly in
grave’s disease.

#Indications –
- Grave’s disease
- Toxic uninodular or multinodular goiter.
- Subacute thyroiditis
- Thyrotoxicosis/Thyroid storm.

#Classification
Mechanism Agent
1. Inhibit hormone synthesis Proplythiuranil, methi-mazole,
carbimazole
2. Inhibit iodide trapping Thio cyanates, perchlorates
nitrates.
3. Inhibit hormone release Iodine, iodides of Na & K,
organic iodide.
4. Destroy thyroid tissue Radio active iodine

#MOA –
*Thioamides derivatives –
Binds to thyroid peroxidase & prevent oxidation of iodine,
therapy
- Inhibit iodination of tyrosine resides in thyroglobulin.
- Inhibit coupling of iodo tyrosine residues to form T3 & T4.

Drugs Dose Remarks


Propylthiouracil 50-150mg TDS. Inhibit peripheral
conserve of T3 or T4.
Methimazole 5-10 mg TDS Active Metabolite
Carbimazole 5-15 mg TDS Acts & largely by
getting converted to
methimazole

#Ionic inhibitors –
They are the competitive inhibitors of thyroidal I –
Transport Via The Na/I symporter.
- Block the reuptake of iodine by the gland.

#Iodine & Iodides –


- At higher Conn iodine limits its own transport & also thyroid
hormone release “thyroid constipation.”
- It also causes reduced thyroid blood flow.
- Thyroid escape occurs; therefore iodides are usually used in
combination with propylthiouracil to inhibit T3 & T4 secretion.

Drugs –
Lugol’s solution *5% iodine in 10% potassium iodide
solution] Iodide [N/K]

Trade Name –
Lugol’s solution, colloid iodine 10% collosal.

Dose – 5-10 drops/day, 8mg iodine/5ml liquid 100-300mg/day


[therapeutic] 5-10mg/day [Prophylactic].

#Radioactive Iodine –
- Iodine of medicinal importance are 1131, 1123, 1125.
- Emits x-rays as well as B-particles.
- Symptoms completely subside within 2-3 months.
- Hypothyroidism can occur as a delayed effect.
- The therapeutic dose is 3-6 micro uric calculated on the basis
of thyroid size.
- Contraindicated in children & pregnant women.
- Metastatic carcinoma is rare with such doses.

#Pharmaco kinetics –
- Absorbed orally well.
- Widely distributed in the body, enter milk & cross placenta.
- Metabolized in liver.
- Excreted in urin.
- is 1-2 hours, action of duration is 4-8 hours.

#Contraindication –
- Previous allergic or reserve reaction to thiomides.
- Impaired hepatic function may require low dose.
- Bronchial asthma.
- Heart blocks & CCF.
- Pregnancy.

#Side effects –
Fever itching, skin rash, joint pain & gI intolerance.

#Adverse effects –
- Hypothyroidism & goiter.
- Agranalocytosis
- Dizziness & alteration in taste.
- Blood dyseraseas & peripheral neuropathy.
- Hypersensitivity to iodides [iodine toxicity causing salivary
glands, stomatitis metallic taste, bleeding disorders &
conjunctiva]

#Nursing responsibilities –
- Assess for tingling of finger & toes.
- Monitor wt. & check for hair loss & skin changes.
- Check CBC, differential count & thyroid & liver function tests.
- Dilute oral iodine solution well in milk, juice or other
beverages.
- Assess for metallic taste in mouth, sneezing, edematous
thyroid, vomiting & bloody diarrhea.

Pt. Education –
- Explain need to wear medical identification tag.
- Explain goals & side effects of medications.
- Advise to report any fever, chills, sore throat & unusual
bleeding.
- Instruct to take medicine at same time of day & with meals or
snacks, space additional daily dose throughout the day.
Oral Contraceptive
Contraceptive are the drug which prevent conception,
these drugs prevent fertility so they are also known as
antifertility drugs.
They are given oral to the female to female of a
reproductive age group has temporary or specific method of
contraception they are mainly aimed at inhibition of ovulation
to prevent fertility.
Most oral contraceptive content progesterone or
testosterone or both in combination.
They are known as estrogen only pills, progesterone only
pills & estrogen progesterone pills.

MOA –
The combined estrogen progesterone pills method prevent
FSH & LH rise in the serum level so the follicular growth &
ovulation does not take place.
Estrogen suppress FSH secretion but increase LH-secretion,
this unusual rise in LH suppressed by the FSH so follicular
growth does not occur & ovulation inhibit.
When oral contraceptive pills stop or withdrawal then
bleeding start from the endometrium.
#Pharmacological action –
1. On ovaries –
They decrease functioning of ovaries so the follicular
growth suppress & ovulation does not take place.
2. On endometrium –
In the continue oral contraceptive taking method there is
the no bleeding occur from endometrium but the sudden stop
or withdrawal lead to bleeding occur from endometrium.

#Indication –
- It is mainly used as a contraceptive method.
- These drugs also decreased the chance of ovarian cancer.
- These are the DOC in the metrorrhagea [Excessive bleeding in
the MC]

#Composition of O.C.T –
1. Composition of MALA – N
Nor ethisterone acetate – 1mg
Ethynil estradiol – 30mg
They are available in pack of 28 tablet out of which 21
hormonal pills & iron pills containing iron sulphate & iron
fumrate.
- These MALA – N or MALA – D are supplied by govt. of India
under the health institution free of WST.
Dose –
For 28 days combined pills start from 5th day of menstrual
cycle for 21 day hormonal combined pills should be given
followed by 7 iron containing pills.
- For 21 days pills format start from 5th day M.C till 25th day of
the M.C
- Pills should be taken daily at night before going to bed.
- If the pt. forget to take the pills it should be taken within 12
hours followed by scheduled tablet.
- If there is continue missing of two tablet then extra
contraceptive method or barrier method should be used upto
menstruation.
- The tablet which are missed should not be taken together or
with one another.

#Contraindication –
- Thromboembolism
- DVT
- DM
- Breast adenoma
- Heart disease
- Cancer of cervix
- Migrane
- Pregnancy
- Uterine fibroid
- severe hypertension
- Epilepsy
- Bronchial asthma
- Lactating mother 1st – 6th month or age greater than 35 years.

#Side effects –
- Nausea & vomiting
- Headache
- Leg cramps
- Mactahgia [pain in breast]
- Fluid retention & edema
- Acne
- Thrombopholebitis
- DVT

#Other contraceptive pills –


1. Dost Coitalpills – These are the pills or hormonal
preparations which are used after unprotected sexual
intercourse to prevent conception.
- These pills are used early in the morning so these are also
called morning after pills.
- They contain leuonorgectrol 0.25mg or 0.5mg with ethynil
estradiol drug 50mg.
- They are available in the pack of 4 tablets out of which two
tablet should be taken within 72 hours of the unprotected &
next two tablets within 12 hours after 72 hours.
- It leads to withdrawal bleeding & prevent conception.
- They should not be used without advise of physician & also
should not be repeated too frequently otherwise hormonal
imbalance may occur.
Uterine Stimulants –
Uterine stimulants are those group of drug which stimulate
contraction of uterus increase uterine motility, intensity &
frequency these help in expulsion of uterine content so they are
used to initiate uterine contraction during labor as well as they
are used for contraction & absorption by inhibiting
implementation of fertilized ovum.
The following agent are used as a uterine stimulant:-
- Oxytocin desamino oxytocin
- Erymetrine [Ergonovine], methyl ergemetrine.
- PG or prostaglandins.

#Oxytocin –
Oxytocin is a polypeptide hormone which is secreted from
posterior lobe of pituitary gland.
*Pharmacological action –
i) On uterus –
In small dose oxytocin increase the power & tone of uterine
contraction so it help in evacuation of uterine content.
- In large dose it produce tonic contraction there may be
rupture of uterus foetal asphyxia or O retention.
ii) On cervix – It increase cervical dilation, so helps in early
expulsion of fetus & induce labor.

iii) On Breast – In lactating mother, it act on my epithelial cells


of the breast & increase expulsion of milk from breast.

iv) On kidney – The larger dose of oxytocin decrease urinary


output so increase fluid retention & produce pulmonary edema.

#Indication –
- Induction of labor.
- Augmentation of labor.
- To control post-partum hemorrhage.

Dose –
- For induction of labor IV drip infusion of 5% dextrose solution
containing 10 unit oxytocin per 100 ml followed by 5 IV until
uterine contraction occur.
- For control post-partum haemorrhage 10IV slowly followed by
10IV/IM after delivery of placenta.

#Contraindication –
HS – Early in Pregnancy

#Side effects –
- Pre-mature child birth
- Foetal death
- Jaundice
- Morexia
- Foetal asphyxia
- O retention & pulmonary edema.
- Nausea & vomiting.

#Ergometrine –
Ergometrine is an active alkaloid obtained from ergot.
- It is analog of oxytocin & it increase uterine contraction so it
stimulate labor.
- Pharmacological action same as oxytocin.
Indication – Induction & Augmentation of labor to control post-
partum haemorrhage.

Dose – IM or IV 0.2 mg
Contraindication & side effect same oxytocin.

#Prostaglandin –
Prostaglandin are derivative of essential fatty acid.
They are 20 carbon cyclic structure. They belong to different
group like prostaglandin [PGA], PGF, PGF2, PGG, PGI,

Pharmacological action –
i) On uterus – Prostagledin stimulate myometrium PGF
stimulate one & amplitude of uterine contraction.
ii) On CVS – PGF2 & PGA produce vasodilation & reduce B.P.
PGF causes vasoconstriction & increase B.P.
iii) On GIT – PGA & PGE inhibit gastric secretion.
iv) On Reproductive system –
PG decrease the synthesis of pregnancy maintaining
hormone progesterone secretion in female so it present
implantation of fertilized ovum so it is used as method of
contraception.

Indication –
To induce labor.
- To control post-partum haemorrhage.
- For contraception.

Dose – 25mg/min IV PGF2 < or 0.3mg/min PGE2 infusion.


Contraindications & side effects are same as oxytocin.

#Uterine relaxant –
- Uterine relaxant are the drops which decrease uterine
motality.
- They are used to delay or post-pond labor or threatened
abortion.
- Uterine relaxant are also called tocolytic drugs or uterine
sedatives.
- Isox purine nalothene.
- Rito drine
- These are uterine relaxant drugs these mainly act on my
atrium & inhibit entry of calcium ion into the myometrium cells
so uterine contraction do not occur & uterine relaxants occur.

#Indications –
- To inhibit uterine contraction due to delay or post pond labor.
- To treat threatened abortion.

#Dose –
Initially 100mg in 5% dextrose IV followed by maintenance
dose of 10mg IM every 6 hourly for 24 hour.

#Contradictions –
HS – Hypotension
Labor do not given at the term.

#Side effects –
- Hypotension
- Tachycardia
- Nausea & vomiting
- Atenosity of uterus
- HS reaction
STEROIDS
Corticosteroids are a class of steroid hormones that are
produced in the adrenal cortex. The term'corticosteroids' or
'corticoids' includes natural glucocorticoids and
mineralocorticoids, and their synthetic analogues. Steroids
involved in a wide range of physiologic systems such as
stress response, immune response and regulation of
inflammation, carbohydrate metabolism, protein catabolism,
blood electrolyte levels, and behavior.

Biosynthesis
• Synthesize in the adrenal cortical cells from cholesterol
• The mammalian adrenal cortex is divided into three zones:
- Zona glomerulosa: Produces mineralocorticoids such as
aldosterone, which regulate sodium and water
- Zona fasciculata: Produces glucocorticoids such as
hydrocortisone and corticosterone,
which regulates carbohydrate and protein metabolism, and Na
and water balance
- Zona reticularis Involved in biosynthesis of androgens.
• Cholesterol is usually derived from plasma lipoproteins and
also released by hydrolysis of cholesterol esters
• Cholesterol is then taken to mitochondria, where it is get
converted to Pregnenolone
• Pregnenolone then leaves the mitochondria and involved in
three different routes of corticosteroids biosynthetic pathway
• The rate of secretion of principal corticoid in man is:
- Hydrocortisone – 10-20 mg/day
- Aldosterone-0.125 Mg/day
- Androgens—20 mg/day.
• Corticoids in systemic circulation are reversibly bound to
transcortin (a corticosteroid binding a globulin)
• Transcortin acts as a reservoir from which a constant supply of
free cortisol is provided to target cells.

Classification of Steroids
• Mineralocorticoids (cortisone, fludrocortisone)
• Glucocorticoids (betamethasone, methylprednisolone)
• Sex steroids (estrogen, progestins)

Mechanism of Action
Glucocorticoid
• The steroid present in the blood is bound to transcortin, but
enters the cell as free molecule
• A glucocorticoid molecule binds to cytoplasmic receptor
protein (active complex is created by dissociation of certain
proteins)
• A structural changes occur in receptor steroid complex that
allows its migration into the nucleus
• Binding to glucocorticoid response elements on the chromatin
• Suppression of genes (prevention of transcription)
• Inhibition of certain genes, which are contributing to their
anti-inflammatory and immunosuppressive action.
• Induction of genes (initiation of transcription): -
- Transcription of specific mRNA leads to production of
desired proteins that brings about final hormonal response. This
may results in metabolic action and anti-inflam matory action.
Effects of corticosteroids are not immediate and once the
appropriate proteins are synthesized effects persist much
longer than steroid itself.

Cellular Actions
Metabolic Actions
• Translocation of glucose transporters from plasma membrane
to deeper sites
• Induction of hepatic gluconeogenetic enzymes
• Induction of hepatic glycogen synthase
• Site specific changes in sensitivity of adipocytes to GH, and,
insulin
• Increased expression of vascular adrenergic and adrenergic
receptors.

Anti-inflammatory and Immunosuppressant Action


• Induction of lipocortins in macrophages, endothelium and
fibroblasts
• Negative regulation of cyclooxygenase 2 (COX-2) and
cytokines in macrophages, endothelial cells and lymphocytes
• Decreased production of collagenase and stromolysin
• Decreased production of the factors involved in localization
and adhesion of leukocytes.

Pharmacologic Action
• Carbohydrate and protein metabolism
• Fat metabolism promotes lipolysis. Free fatty acids raise in the
body. Redistribution of hody fats occur according to their
sensitivity to insulin
• Calcium metabolism and water excretion
• Cardiovascular-permissive effect
• skeletal muscles—weakness occur in both hypo- and hyper-
corticism
• CNS – patients with Addison's disease suffers from apathy,
depression, and occasional psychosis. Precipitates seizures in
epileptic patients
• Stomach-increased secretion of gastric acid and pepsin
• Hemopoitic system-increase in number of RBCs and platelets,
but decrease lymphocytes, eosinophils and basophils. Enhanced
the rate of destruction of lymphoid cells in malignancy; basis of
their use in lymphomas
• Inflammatory response—it is suppressed and the action is
nonspecific and covers all the components and stages of
inflammation. This includes reduction of:
- Increased capillary permeability
- Local exudation
- Cellular infiltration
- Phagocytic activity
- Capillary proliferation, collagen deposition and scar formation
- Limitation of recruitment of inflammatory cells at local site of
inflammation
• Immunologic and allergic responses—suppress all types of
allergic phenomenon and hypersensitization:
- Impairs the ability of inflammatory cells to migrate to site of
immunologic reaction
- Process of antibody is also suppressed
- Phagocytosis and digestion of antigen by macrophages is also
inhibited. The efficacy of glucocorticoids in controlling graft
rejection is due to their ability to:
- Reduce antigen expression from graft cell
- Delay revascularization - Decreased sensitization to T
lymphocytes.

Mineralocorticoid
• Mineralocorticoids receptor (MR) complex also binds to
mineralocorticoid response elements
• Aldosterone exerts its effects on Na and K homeostasis by
acting on MR present in distal renal tubules and collecting ducts
• The MR has equal affinity for both aldosterone and
hydrocortisone
Hydrocortisone on binding to MR in kidney is inactivated by
11-6 hydroxysteroid ydrogenase to receptor inactive cortisone.
Aldosterone escapes degradation.
This explains why specificity of MR for aldosterone action
on kidney is maintained, in the face of much higher levels of
circulating glucocorticoids.

Action in Kidneys
• Transcription of mRNA in renal tubular cells directs synthesis
of proteins aldosterone induced proteins (AIP)
• Promotes Na reabsorption and K excretion by number of
mechanisms
- Activate sodium channels
- Translocate Na channels from cytosolic site to luminal
membrane
- Na+K+, ATPase to basolateral membrane, increases ATP
production by mitochon

Pharmacokinetics
• Absorption-effective by oral route, acts rapidly by IV/IM •
Bioavailability—oral bioavailability of synthetic corticosteroids
are high
• Plasma protein binding-90% bound to plasma proteins •
•Metabolism-primarily by hepatic microsomal enzymes
•Excretion-metabolites conjugated with glucuronic acid or
sulfate are excreted in u
• Distribution-widely distributed—10 L/kg
• Plasma t12-66 minutes.

Preparations and Doses


Synthetic steroids have largely replaced the natural compounds
in therapeutic use becaus are potent, longer acting and more
selective for glucocorticoid/mineralocorticoid actions.
Preparations of steroids
Drug Dose Route
Hydrocortisone 20 mg, 100 mg Oral, IV
(Efcorlin)
Prednisolone 5-60 mg/day, 10-40 Oral,IM
(Wysolone) mg
Methylprednisolone 4-32 mg, 1g Oral,IV
(Solu-medrol) infusion
Triamcinolone 4-32 mg/day, 5-40 Oral,IM
(Kenacort) mg
Dexamethasone 0.5-5 mg/day, 4-20 Oral,IV/IM
(Dexona) mg/day
Betamethasone 0.5-5 mg/day, 4-20 Oral,IV/IM
(Betnesol) mg/day
Desoxycorticosterone 2-5 mg, 10-20 mg Sublingual, IM
(Docabolin) Once or twice
weekly
Fludrocortisone 50-200 Mg Orally
(Floricort)

*Aldosterone not used clinically

Topical Applications
Used in bronchial asthma, allergic/seasonal rhinitis
• Beclomethasonedipropionate: Beclate Inhaler
• Budesonide: Pulmicort, Budecort
• Fluticasone Propionate: Flohale Inhaler
• Flunisolide: Syntaris
• Ciclesonide: Ciclez.

Intranasal Sprays
About 25-250 g sprays in each nostril two to three times a day.
skin preparations: Conjunctivitis:
• Flucinolone: Flucort-H
• Triamcinolone: DesOwen
• Hydrocortisone: Lycortin
• Dexamethasone: Decadron-cream
• Flucortotone: Ultralan
Dose: 0.01%-2.5% formulations

Indications
Replacement Therapy
• Acute adrenal insufficiency, e.g. adrenalectomy
• Chronic adrenal insufficiency, e.g. addison's disease
• Congenital adrenal hyperplasia.

Pharmacotherapy
• Arthritides
• Collagen disease, e.g. systemic lupus erythematosus (SLE),
polyateritis, dermatomyositis
• Severe allergic reactions—urticaria, angioedema, serum
sickness, conjunctivitis
• Autoimmune disease—ITP (medicines decreases the immune
response)
• Bronchial asthma
• Other lung disease used in respiratory distress syndrome
(RDS) in neonates and to accelerate lung maturation in fetus.
Benefits in aspiration pneumonia, pulmonary edema
• Infective diseases-severe form of lepra reactions, bacterial
meningitis and pneumonia in AIDS patient
• Eye diseases—used in large number of inflammatory ocular
diseases.
• Topical instillations-allergic conjunctivitis, iritis, keratitis
• Systemic-optic neuritis, uveitis
• Skin diseases-topical therapy in atopic eczema, allergic
contact dermatitis, varicose eczema. Systemic therapy in
pemphigus vulgaris, exfoliative dermatitis, Stevens Johnsons
syndrome
• Intestinal diseases- In ulcerative colitis, Crohn's disease, celiac
disease. Corticosteroida are indicated during acute phase
• Cerebral edema due to tumors, tubercular meningitis,
responds to corticoids
• Malignancies -used in acute phase lymphatic leukemia,
Hodgkin's and other lymphomas because of their marked
lympholytic action
• Organ transplantation and skin allograft-to prevent rejection
reaction
• Septic shock
• Thyroid storm
• To test adrenal pituitary axis function.

Contraindications
Absolute
• Hypersensitivity
• Cushing syndrome
• Herpes ocular infection.

Relative
• Peptic ulcer
• DM and HTN
• Viral and fungal infections
• Tuberculosis
• Osteoporosis
• Psychosis
• Epilepsy
• CHF
• Renal failure.

Adverse Effects
Occurs Usually with Prolonged Therapy
• Mineralocorticoids—Na and water retention, edema,
hypokalemic alkalosis and progressive rise in BP
• Glucocorticoids
• Cushing habitus-characterized by moon like face,
accumulation of fat in the truncal region
• Hyperglycemia and glycosuria
• Myopathy and muscle wasting
• Susceptibility to infections
• Peptic ulceration
• Ostoeporosis
• Ocular effects -glaucoma can be precipitated
• The CNS side effects-mild psychologic disturbance (euphoria,
insomnia, nervousness) to pronounced psychiatric effects
(psychosis) can occur, but reactions are reversible
• Suppression of hypothalamic pituitary adrenal (HPA) axis
• Growth retardation in children
• Fetal abnormalities-intrauterine growth restriction (IUGR) can
occur after prolonged therapy in pregnant women, increases
the risk of gestational diabetes, PIH, pre-eclampsia
• Miscellaneous-acne, purple striae on thighs and lower
abdomen, hirsutism, weight, gain, pancreatitis, hepatomegaly .
• Topical application may produce skin atrophy
• In patients with AIDS kaposi sarcoma can activated.

Drug Interactions
• Antibiotics, cyclosporine, estrogen and ketoconazole slow
metabolism/clearance
• Aminoglutethemide, carbamazepine, phenobarbitone,
phenytoin and rifampicin may increase the metabolism
• Antianxiety, antipsychotics, anticoagulants, antihypertensives,
hypoglycemics also affect metabolic/clearance.

Nursing Responsibilities
• Check vital signs, BP and lung sounds, weight, nausea and
vomiting, and signs of dependent edema
• Conduct mental status exam and assess for signs of
depression, withdrawal, insomnia and anorexia
• Check skin for striae, thinning, bruising, change in color
• In children on prolonged therapy, monitor height and growth
pattern
• Advise regular ophthalamic examination with long term
therapy
• Check stool for occult blood periodically
• Administer suitable antibiotics as prescribed in proper dosage
along with steroid ir chronic infections.

Patient Education
Mineralocorticoids
• Instruct to report signs of low potassium a/w high sodium
(muscle weakness, paresthesia fatigue, anorexia, nausea)
• May advise to eat food high in potassium
• Advise to weight daily and report consistent weight gain
• Instruct to report any signs of infection, trauma or unexpected
stress.

Glucocorticoids
• Discuss benefits and possible side effects with long term use
• Instruct to take oral doses with food and avoid alcohol
• Suggest weight reduction diet, limiting Na intake and
increasing potassium intake
• If client is diabetic, advise to carefully monitor blood glucose
levels
• Avoid strenuous exercises, if skin is fragile and easily bruises
• Instruct to avoid immunization during therapy and for 3
months after
• Instruct to wear specific medical identification during therapy
• Review drug and teach about specific administration protocol
• Instill measures to minimize HPA axis suppression.
ADRENAL STEROID INHIBITOR
It is available for treating selected cases of Cushingoid
Syndrome (Adrenal hyper function).

Drug of Choice: Aminpalutathimide


Mechanism of Action
It binds to cytochrome

Inhibits conversion of cholesterol

To delta -5-pregnenolone

Thus impairing normal synthesis of adrenal steroids


Mechanism of action of aminoglutethimide

Dosage
Initially 250 mg four times/day, increased to 2 g in 1-2 weeks.

Indications
• Cushing's syndrome
• Investigational uses in advanced mammary carcinoma in
postmenopausal women
• Metastatic prostatic carcinoma.

Contraindications
• Hypersensitivity to glutethimide
• Pregnancy.

Adverse Reactions
•Neutropenia, thrombocytopenia
• Cardiovascular-orthostatic hypotension, tachycardia
• GI: Vomiting
• Dermatologic: pruritus, urticaria
• Other: adrenal insufficiency, hypothyroidism, hirsutism,
altered LFTs.

Nursing Responsibilities
• Monitor client closely as the drug can produce adrenal
insufficiency especially under stress, trauma
• Advise patient that nausea and anorexia can occur during first
few weeks of therapy. Consult physician, if effects prolonged
• Reduce dosage or discontinue, if adverse rxns become too
severe
• Perform thyroid functions at regular intervals
• Perform hematologic studies at regular intervals and LFTs at
regular intervals
• Monitor BP, as there is possibility of orthostatic hypotension.
ANABOLIC STEROIDS
Definition
These are androgens with anabolic properties and are rarely
prescribed, but are commonly abused by athletes in an attempt
to enhance performance. They are developed to replace
androgens.
Mechanism of Action
Testosterone (androgen) is converted to active metabolite
dihydrotestosterone

Increased synthesis of RNA and cellular protein (other


metabolites enhance these directly)

Stimulate growth of muscle, bone, skin and hair, and accelerate


closure of epiphyses at ends of long bones, increase production
of RBCS Large doses can suppress pituitary gonadotropin
secretion and decrease spermatogenesis through feedback
inhibition
Mechanism of Action

Indications
• Retarded growth and development in children
• Debilitating diseases such as severe ulcerative colitis
• Osteoporosis
• Anemia mainly aplastic anemia
• After trauma, surgery
• Prolonged immobilization
• Corticosteroid induced catabolism.

Common Medications
S.N. Drug Dose Route
1. Nandrolone Adults: 25-50 IM
(Durabolin, Deca- mg/mL/week Children:
durabolin) 12.5-25 mg/mL 2-4
week, Breast cancer:
25-100 mg/week
2. Oxandrolone Adults: 1-2 mg/day IM
(Oxandrin, Anavar) Children: 0.25-5
mg/kg/day
3. Stanzolol (Winstrol) Adults and children: 1- Oral
2 mg, 2-3 tablet/ day
4. Oxymetholone (Anrdol- Adults and children:1-
50) 2 mg/kg/day to 5
mg/kg/day

Contraindications
Pregnancy and lactation, CHF, renal failure, liver failure and
enlarged prostrate.
Side Effects
• In Both Genders: Lowered voice, edema and acne, increased
facial hair growth
• In Males: Gynecomastia, oligospermia, impotence and
decreased ejaculatory volume
• In Females: Menstrual irregularities, male pattern baldness a
voice changes.
Adverse Effects
Hepatotoxicity, abusers of anabolic steroids often share
needles, increasing incidence of hepatitis B, C and human
immunodeficiency virus (HIV) transmission.

Nursing Responsibilities
• Do not administer for longer than 90 days without careful
patient reassessment .
• Recognize that these do not significantly enhance the athletics
ability and should not be used to improve performance because
the risk outweighs the potential benefit .
• Asses client for edema, weight gain and skin changes
• Assess client for signs of liver dysfunction
• Evaluate client for signs of depression.
• Administration of injection: Warm and shake vial to dissolve
crystals if present, admin deep into gluteal muscle
• Encourage bedridden patients to perform exercise regularly to
minimize developmer hypercalcemia
• Monitor for adverse effects like precocious puberty in boys,
breast enlargement deep voice, hypercalcemia in women
(nausea, polyuria, weakness).

Patient Education
• Educate client on risks of using anabolic steroids, if they admit
to using medications has been obtained illegally
• Educate client about risk of sharing needles
• Inform client to notify physician of using these medications.

Complementary & alternative system of medicine


Definitions

► Complementary and alternative medicine (CAM) is the term commonly used to describe
a broad range of healing philosophies, approaches and therapies that focus on the whole
person including biopsychosocial and spiritual aspect.

ALTERNATIVE THERAPIES

CAM therapies when used alone referred as alternative therapies.

COMPLEMENTARY THERAPIES

When CAM therapies are used in combination with other conventional therapies referred
as complementary therapies.

Unit - 12

Types of Complementary And Alternative Medicine


Types of Complementary / Alternative Medicine

1. Alternative Medical Systems

2. Mind-Body Interventions

3. Biologically-Based Therapies

4. Manipulative and Body-Based Methods

5. Energy Therapies

1. Alternative Medical Systems

► Alternative medical systems are built upon complete systems of theory and practice.
Often, these systems have evolved apart from and earlier than the conventional medical
approach used.

Types of Alternative Medical Systems

► Acupuncture

► Ayurveda
►Homeopathy

►Naturopathic medicine

Acupuncture

Acupuncture is a component of traditional Chinese medicine that originated in China over


5,000 years ago. It is based on the belief that living beings have a vital energy, called "qi"
that circulates through twelve invisible energy lines known as meridians on the body.

CONTD...

► Acupuncturists insert needles into specified points along meridian lines to influence the
restore balance to the flow of qi. There are over 1,000 acupuncture points on the body

How Acupuncture Works

►There are numerous theories about how acupuncture works. Some of them are:

► Acupuncture stimulates the release of pain

► Acupuncture influences the release of neurotransmitters, substances that transmit


nerve impulses to the brain

► Acupuncture influences the autonomic nervous system

► Acupuncture stimulates circulation

►Acupuncture influences the electrical currents of the body

Conditions Treated By Acupuncture

► Migraines and tension headaches

► Sinusitis

► Common cold

► Addictions, quit smoking

► Meniere's disease

► Arthritis

► Menstrual cramps

► Asthma
► Weight loss

► Infertility

LIMITATIONS OF ACUPUNCTURE

► Acupuncture is considered a safe therapy when the practitioner has been trained and
uses sterilized needles. The complications includes...

► Infection

► Broken needle puncture of an internal organ

► Bleeding

► Fainting

► Seizure

CONTRAINDICATIONS...

► Person with bleeding disorders

► Thrombocytopenia

► Skin infection

► Semi permanent needles should not b used in a person with vascular heart disease
because of the risk of infection.

►Electro acupuncture should avoid in person with a pacemaker, epilepsy or in pregnancy.

Ayurveda

Ayurveda is the traditional medicine of India, which originated there over 5,000 years ago.

Ayurveda emphasizes re establishing balance in the body through diet, lifestyle, exercise,
and body cleansing, and on the health of the mind, body, and spirit.

CONTD...

► According to Ayurveda. everything is composed of five elements: air, water, fire, earth,
and space. These elements combine to form the three doshas i.e.

► Vata

► kapha
► pitta

1. The vata dosha

► The vata dosha is a combination of space and air.

► It controls movement and is responsible for basic body processes such as breathing, cell
division and circulation.

► Vata body areas are the large intestine, pelvis, bones, skin, ears, and thighs. People with
vata as their main dosha are believed to be quick-thinking, thin, and fast, and are
susceptible to anxiety, dry skin, and constipation.

2. The kapha dosha -

► The kapha dosha represents the elements of water and earth.

► Kapha is believed to be responsible for strength, immunity, and growth.

► Kapha body areas are the chest, lungs, and spinal fluid. People with kapha as their main
dosha are thought to be calm, have a solid body frame, and are susceptible to diabetes,
obesity, sinus congestion, and gallbladder problems.

3. The pitta dosha

► The pitta dosha combines fire and water.

► It is thought to control hormones and the digestive system.

► Pitta body areas are the small intestines, stomach, sweat glands, skin, blood, and eyes.
People with pitta as their primary dosha are thought to have a fiery personality, oily skin,
and are susceptible to heart disease, stomach ulcers, inflammation, heartburn, and
arthritis.

An Ayurvedic treatment plan involve

► Diet

► Cleansing and detoxification:

► Herbal medicine

► Yoga

► Meditation
► Exercise

► Massage:

Ayurvedic Medicines for various ailments

►Anemia

►Arthritis

►Asthma

►Back Ache

►Bleeding Gums

►Blood Dysentery

►Bronchitis

►Cancer

► Chicken Pox

►Cholera

► Cough and Cold

► Dengue

3. Homeopathy

Homeopathic remedies are typically derived from plants, herbs, minerals, or animal
products. After being crushed and dissolved in alcohol and/or water, the selected substance
undergoes a long process of dilution and succession (a process that involves vigorous
shaking of the solution). The solution is then stored.

CLINICAL APPLICATION OF HOMEOPATHY

► Diarrhea

► Migraines

►Motion sickness

► The flu

Side Effects of Homeopathic Remedies


Since they're so diluted, homeopathic remedies don't usually cause adverse effects. In
some cases, however, patients may briefly feel worse after first beginning their
homeopathic treatment.

LIMITATIONS OF HOMEOPAHY

1. A surgical problem which has progressed far beyond its initial stages might not respond
to homoeopathy.

2. Some sudden life threatening situations like heart attacks, paralytic strokes, diabetic
comas etc. might have to be initially treated with allopathy, till the patient is out of danger.

3. It is relatively slow acting as compared to the steroids.

4. The success rate is not 100%.

4. Naturopathy:

► Naturopathy uses body's natural healing abilities in prevention and treatment of disease
through a healthy lifestyle.

► It builds immunity, improves mental health, and enhances body functions.

► Naturopathy mainly focuses on finding the cause of the disease rather than merely
treating the symptoms of disease.

►It uses diet, homeopathy, hydrotherapy, herbal medicine, and other therapies to return
the body to a state where it can heal itself.

CLINICAL APPLICATIONS OF NATUROPATHY

►Weight loss

►Fatigue

►Menstrual cycle disturbances (e.g., cramping, fluid retention, irregular cycles)

►Stress and anxiety

►Mild depression

►Mood swings

►Allergies

►Arthritis
CONTD...

► Menopause related problems (e.g. hot flushes, insomnia, mood changes)

►Sleep problems

►Poor immunity

►Arthritis

►Blood sugar imbalances

►Slow metabolism

►General wellbeing

►Preconception care and fertility

TYPES OF NATUROPATHY

► REBALANCING FOOD

► ESSENTIAL OILS, AND OTHER BACH FLOWERS, HERBS AND PLANTS

►RELAXATION TECHNIQUES

►MASSAGE

2. Mind-Body Interventions

Mind-body medicine uses a variety of techniques designed to enhance the mind's capacity
to affect bodily function and symptoms. Some techniques that were considered alternative
in the past have become main stream (for example, patient support groups and cognitive-
behavioral therapy).

TYPES OF MIND- BODY INTERVEVENTIONS

►Meditation and Breathing

►Relaxation

►Hypnosis

►Biofeedback

1. Meditation and Breathing


► Meditation means sitting or resting quietly, often with the eyes closed, which stills the
mind for greater self-awareness.

► Meditation also helps in reduction of pain and relieving stress.

►It also involves sometimes the repetitive sounding of a mantra, which helps the person to
focus. Meditation promotes relaxation.

Components of meditation

► Quite space

► A comfortable position.

► A respective attitude

► A focus of attention

TECHNIQUES OF MEDITATION

 Meditation and rhythmic breathing


 Progressive relaxation
 Relation by sensory pacing
 Relaxing with music

1. Meditation and rhythmic breathing

► Provide a quite environment.

►Help the client get comfortable while seated or lying on back.

►Instruct the client to close eyes and hold a receptive attitude.

► Instruct the client to breath in and out slowly and deeply using abdominal muscles
keeping the chest still.

Contd...

► At the beginning of every out breath have client to repeat the number 'one' silently in
his or her mind and continue for period of meditation.

►Explain that when the mind wanders, being it back to counting the outbreath without
judgment.

►Have client practice for 5, 10, 15 or20 minutes per session practice daily for at least one
session.
2. Progressive relaxation

► Following steps 1, 2,3 and 4 of meditation and rhythmic breathing.

► Once the client is breathing slowly and comfortably instruct client to tighten and relax
the muscles.

►Instruct the client to tense and relax the calves and knees.

3. Relaxation by sensory pacing

► Following steps 1, 2,3 and 4 of meditation and rhythmic breathing.

►Instruct the client to slowly repeat and finish either in a low voice of the following
sentence

-Now I am aware of seeing

-Now I am aware of feeling

-Now I am aware of hearing

► Instruct the client to repeat and complete each sentence 4 times, the 3 times then twice
and finally once.

4. Relaxing with music

► Provide client with a tape recorder and headset.

►Ask client to select a favorite cassette of slow quiet music.

► Instruct client to get into a comfortable position and to close eyes and listen to music
through the headset.

► Instruct client to imagine floating with music.

CLINICAL APPLICATION:

► Prolonging Life Expectancy

►Stress Control

►Pain Management

►Cancer and Other Chronic Illness

►Heart disease
►High blood pressure

► Infertility

►Psoriasis Respiratory crises Premenstrual Syndrome (PMS), Tension Headaches

►Irritable Bowel Syndrome, Ulcers, and Insomnia

►Fibromyalgia

Limitation of meditation

►It may be contraindicated in people who have a strong fear of losing control.

►Hypertensive individual require a much shorter session than average 15-20 minute
session.

2. Relaxation

Relaxation techniques are aimed at relaxing muscles and quieting the mind and are mainly
designed to relieve tension and strain. It is also used as an alternative treatment for
insomnia.

CHARACTERISTICS OF RELAXATION

► Decreased heart rate

►Decreased respiratory rate

►Decreased BP

►Decreased oxygen consumption

CLINICAL APPLICATION OF RELAXATION THERAPY:

►Lowering heart rate

►Lowering BP

►tension

►Improving well being

►Reducing symptoms of distress

►Depression

►Anxiety
LIMITATION OF RELAXATION THERAPY

►Individual undergoing relaxation therapy has report fearing loss of control.

► Feeling they are floating and experiencing relaxation induced anxiety related to
theses feelings.

► Occasional relaxation techniques may result in continued intensification of symptoms.

3. Hypnosis

►Hypnosis is a sort of conscious sleep or trance that can help people deal with addictions,
pain or anxiety disorders.

► In hypnosis, a person is put into an advanced state of relaxation in which he is relatively


unaware of his surroundings but not entirely unconscious about it.

►A hypnotized person follows the instructions given by the hypnotherapist and tends not
to be to psycho logic stress and conflict.

Indications for Hypnosis

►Habit Disorders

► Habit Disorders

►Relaxation

►Anxiety States

►OCD

►Psychotic Disorders

Contraindications for Hypnosis

►In a patient who does not want it.

►Hypertensive individual.

4. Biofeedback: Biofeedback
 Biofeedback is a group of therapeutic procedures that use electronic or
electromechanical instruments to measure the process and information to person
about their neuromuscular and autonomic nervous system.
 The information or feed back is given in physical, physiological activity or visual
feedback signals.
CONTD...

 People are trained to exercise some control over the way their bodies work and
involves measuring a subject's bodily processes such as blood pressure, heart rate,
skin temperature using electronic sensors.
 Biofeedback helps a person to be more aware of what his body is doing, and to bring
reactions under control.

The most common biofeedback techniques are:

►Temperature biofeedback

► EMG biofeedback

►EEG biofeedback

►Galvanic Skin Response

Clinical application of biofeedback

Biofeedback helps the treating

►pain

►stress

►Insomnia

►headache.

Limitations of biofeedback

During relaxation the feeling may be uncovered that client cannot cope with them. For this
reason it's recommended that practitioners should be trained.

3. Biologically-Based Therapies

Biologically based therapies in complementary and alternative medicine use substances


found in nature, such as herbs, foods, and vitamins. There are mainly following types of
biological based therapy:

►Herbal Medicine

►Orthomolecular Medicine

1. Herbal Medicine
• Herbal medicine is a system, which uses various remedies derived from plants and their
extracts to treat disorders and maintain good health.

• Either a whole single herb or a mixture of different herbs can be used. .

 Though herbal medicine exhibits a slower and deeper action they assist the body to
eliminate and detoxify,thus taking care of the problem that's causing the symptoms.

• Herbal medicines are available as extracts, infusions, pills, and powders.

Clinical application of herbal therapy

►Minor burns

►Wound healing

►Hypertension

►Diabetes

►Nausea

►Vomiting

►Motion sickness

[Link] Medicine

Orthomolecular medicine involves the use of proper nutrition or nutritional supplements to


maintain and restore health.

Orthomolecular medicine uses combinations of minerals, vitamins and amino acids


normally found in the body to treat specific conditions.

CLINICAL APPLICATIONS

►Arthritis

►Cardiovascular disease

►Hypertension

►Beriberi

►Night blindness

►Osteomalacia
►Pernicious anemia

►Rickets

►Scurvy

► Xerophtalmia

5. Manipulative and Body-Based Methods –

Manipulative and body-based methods in complementary and alternative medicine are


based on manipulation and/or movement of one or more parts of the body.

Types of Manipulative and Body-Based Methods

 Chiropractic
 Osteopathy
 Massage Therapy
 Reflexology

Chiropractic: -

►Chiropractic is based on the theory that disease conditions result from misalignments of
body structures, especially the spine.

►Due to this misalignment pressure is placed on the nerve roots as they exit the spinal
column resulting in decreased function of the nerve and the organs that they serve.

►The treatment for achieving this balance is spinal manipulation to restore correct
alignment and full working order. Researches have shown chiropractic to be effective in
treating low back pain.

Osteopathy

► Osteopathy is a system of diagnosis and treatment by manipulation that mainly focuses


on musculo skeletal problems.

►It differs from chiropractic in its underlying theory that it is impairment of blood supply
and not nerve supply that leads to problems.

► Doctors of osteopathy use manipulation plus traditional medicine to cure problems.

Massage Therapy

►It is the manipulation of body tissues to promote wellness and reduce pain and stress.
►lt plays an important role in treating illness or chronic ailments, and contributes to a
higher sense of general well being. It involves a variety of techniques such as stroking or
kneading for applying pressure to specific points.

►Massage therapy may cause side effects and should not be used in people who have
infectious or contagious skin diseases.

Reflexology .

►Reflexology is the practice of stimulating points on the feet, hands and ears to improve
health or give a beneficial effect on some other parts of the body.

►lt is commonly performed on the particular areas of foot that are believed to correspond
to different organs or systems of the body.

►This helps to eliminate the blockage of energy responsible for pain or disease in the
corresponding body part.

Energy Therapies -

Biofield therapies are intended to affect energy fields that purportedly surround and
penetrate the human body. The existence of such fields has not yet been scientifically
proven. Some forms of energy therapy manipulate biofields by applying pressure and/or
manipulating the body by placing the hands in, or through, these fields.

Types Energy Therapies -

1. Reiki

2. Therapeutic Touch

3. Bioelectromagnetic-based Therapies

1. Reiki Therapy:

►Reiki is a technique, which uses the channeling and flow of energy through the body to
improve health and promote healing.

► It is very much different from conventional healing therapies. Because in a Reiki therapy,
there are no medicines or tools needed to heal diseases.

►All a practitioner has to do is to direct energy towards the body through the hands and
the power of meditation.

Clinical applications of reiki therapy


►Anxiety

►Stress

►Arthritis

►Endometriosis

►Chronic fatigue syndrome

► Insomnia

►Depression

►Migraines

►Hot flashes

►Cramps

Limitations of Reiki therapy

►Regular sessions are requires.

►Need other treatment in addition to Reiki therapy in case of serious illness.

Therapeutic Touch

►This technique uses the therapist's healing energy to identify and repair imbalances in a
person's biofield.

►They believe that by placing their hands on or near a patient's body they can direct
energy and correct disturbances.

CLINICAL IMPLLICATIONS

►Pain

► Fever

►Swelling,

►Infections

►Wounds

►Ulcers
►Thyroid problems

►Burns

►Nausea

►Premenstrual syndrome

►Diarrhea, and headaches

►TT is useful in treating diseases such as measles, Alzheimer's disease

Limitations of therapeutic touch

►Lack of eye and facial contact during session.

►Person who are sensitive to human interaction and touch.

►Physical abused

►Psychiatric diseases.

3. Bioelectromagnetic-based Therapies

Bioelectromagnetic-based therapies use pulsed energy or magnetic fields to alter the


body's electromagnetic fields and cure illness. Magnets have become a popular treatment
for various musculoskeletal conditions and even to relieve pain.

Clinical applications -

►Osteoporosis

► Arthritis

►Effective in healing non-union fracture hip

►Pain

Contraindications

►Pacemaker or other implanted or external medical devices;

►Pregnancy

►Myasthenia gravis

►Hyperfunctional endocrine glands


►Active TB, acute viral diseases

►Malignancies

►Psychoses

►Organ transplant

Role of nurse in complementary and alternative therapy

►The integrative medicine approach is consistent with the holistic approach nurses are
taught to practice.

► Nurses have the potential for becoming essential participants in this type of health care
philosophy.

►Nurses should be knowledgeable of CAM therapies to make appropriate


recommendation.

►Nurses should also provide advice to client regarding when to seek conventional
therapies or CAM therapies.

Contd...

►Nurses need to be aware of their state nurse practice act with regard to CAM therapies
and practice only with in the scope of these laws.

►Nurses have knowledge regarding current researches being done in this area to provide
accurate information not only to patient but to other health care professionals.

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