Overview of Pharmacology Principles
Overview of Pharmacology Principles
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.
Pharmacology
Pharmacon + logos
Drugs to study
Drogs
Dry hub
( first medicine)
Definition –
It is scientific study of drug movement (ADME) and its effect (Power) on human body is called as pharmacology.
Pharmacokinetics :-
Pharmacodynamics : -
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.
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
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.
#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
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.
#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.
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.
Phagocytosis Pinocytosis
(solid liquid
self eating) (self drinking)
#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.
#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.
#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.
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.
#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.
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.
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.
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)
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
*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.
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.
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).
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
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
Duration of Contact
Higher the concentration of the antiseptic, greater is its effect.
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.
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.
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.
#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.)
*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.
*Indication of SGAs –
- Allergic rhimtis conjunctivitis the fever.
- Verticaria, Atopic sczima.
- AC allergic to drugs food.
#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.
#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
# 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
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.
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.
*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.
*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
*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.
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.
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
#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.
→ Antagonize receptors
Use – Motion sickness.
8. Steroids – Dexamethasone
Use – Nausea/vomiting
*Indications ul side effects –
1. Ondansteron – Indications
- Radio therapy induced vomiting
- Chemotherapy induced vomiting
- Post op. vomiting
Uses:-
Ulcerative colitis
Travellor’s diarrhea
Acute Secretory Diarrhea
(3) Antimotility:-
(A) Codene
(B) Loperamide
(C) Diphenoxylate astropine
(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.
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)
*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.
*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.
*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.
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.
*Classification –
(1) Bronchodilators:-
(A) Sympathomimetic – Salbutamol, salmeteral Adrenaline,
Terbutaline, Ephedrine.
(B) Methylaxanthines – Theophylline, Aminophylline,
Hydroxyethyl theophylline.
(C) Anticholinergies – Ipratropium bromide Tiotropium Bromide.
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.
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
→ Anxiety
→ Insomnia
→ Restlessness & fatigue
→ Headache
→ Tremor
→ Muscle Cramps
→ Rashes, urticarial
→ Dry mouth, Diarrhea, Dyspepsia, Nausea & vomiting.
*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.
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.
- 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.
*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.
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.
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
*MOA –
Central the rate of protein synthesis & depresses the
migration of polymorphonuclear leukocytes fibroblacts.
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.
*Dosage –
* Sodium Cromoglycate – 20 mg capsule for aerosol.
* Ketotifen – 1-2 mg BD with.
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.
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.
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
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.
*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.
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.
*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.
*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.
*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.
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.
*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.
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
*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.
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.
*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.
*Indications –
Allergic disorders, Allergic rhinitis, common cold, Insect
bites, drug reaction, anaphylactic reaction. Insomnia, allergic
cough, urticaria, pruritis, nausea & vomiting.
#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.
*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
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 :-
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 :-
Acute CHF, acute pulmonary edema, edema associated with CHF, edema renal & liver disease, hypertemion acute,
renal failure, cerebral edema, acute hypoglycemia & hyperkolmia.
Contraindications :-
. anuria
. hepatic
Side effects :-
. hypersensitivity reaction
. Hypotension
. ECH changes
. hypokalenia
. cardiae disturbance.
. metabolic alkalosis
. hyponatremia
. blurred vision
NSh responsibilities :-
Drug :-
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.
Indications
- Edema
- Hypertension
- Diabetes insipidus
- Hypercaleiurea
- Liver ciruhosis
Contraindications :-
- Allergy to thiazides
- Sulfonamides; fluid or electrolyte imbalavie
- Renal disease & liver disease & anuria.
Adverse effect :-
Other :- muscle cramps, muscle spasms, fever gouty attacks, fluching, wt. loss, rhinorrhea, electrolye imbalances,
hyperglycemia.
NSG responsibilities :-
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 :-
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.
- Allergy
- Alyperkolemia
- Renal disease
- Anuria
- Use cautinaly with pregnancy & lactation.
Adverse effect :-
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.
Mark calendars of edema outpatiens as reminders of alteroute day or 3 – 5 day / week therapy.
Pt. education :-
Advise pt. to wt. yourself on a regular basis, at the some time in the some colotting & record the wt. on your calendar.
Advise pt. that if she / he experience any type of side effect & adverse effect should contact with given & physicion
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 :-
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 :-
Hypersenlitivity Hex4
NSG responsibilities :-
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 :-
Anti – diuretics [ inhibit the water excretion without affecting salt excretion ] are drugs that reduces urine volume
particularly in diabetic insipidus.
Classification :-
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 :-
Hemophilia & van willebrond’s disease :- may release factor VIII & prevent bteedi
Contraindications :-
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 :-
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)
Moderate restriction of Na+, Cl- intake has been show to enhance the avtidioetic effect
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 :-
Contraindications :-
hypoglycemia, nausea, vomifing diarrhea, constipation, headache, het, gain, cholestatic jaundice, dilutional
hyponatremia iutolernce to alcohol.
NSG Responsibilities :-
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.
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 :-
Hypersensitivity rexn
Hepatitis
Vaniting, diarrhea.
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.
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 :-
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 :-
Monitor I / o
Advise pt. to avoid excessive intake of alkalinizing foods as milk or citrus fruits.
2. Nitrofurantion :-
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 :-
Oral adult → 50 – 100 mg 4 times a day, chronic therapy 25- 50 mg four times 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.
Administer oral drug with meals or milk to reduce GI distress & possibly to improve absorption.
Instruct pt. rinse mouth though after use of oral suspension to prevent staining of teeth.
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
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.
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.
Use of sodium ascorbate, injection in its with Na restricted or calcium ascorbate in pt’s receiving drugs.
Doses :-
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.
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 :-
Metabolic acidosis
Contraindications :-
Systemic alkalosis
Sodium overload
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 :-
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.
Cardiae disease
Hypertension
Dose :-
Adult → at first, one to four tablets after meals & at bed time
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.
Antacids should be taken at least 2 hours a part from other drugs as drug interaction may occur.
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 :-
8 – 30 mg / kg day in divide doses, usual range is 100 – 400 mg / day in combination with anticomualsants.
Contraindication :-
Acidosis
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 .
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 –
Isoproterenol(Isuprel ) –
Action –
Route –IV
Metaraminalaramine –
Route–IV
Route –IV
Dopamine (Intecopin ) –
Route – IV drip
Action –
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 –
Adult –1mg in 9ml normal saline (1mg /10 ml) pediatricdosage: 0.01 mg /kg (10 mg/kg) in normal saline (up to 5ml)
Adult -0.5 mg
Dose -1mg/kg
Atropine –Asystole or severe bradycardia
20 iug / kg (child)
Oxygen –
Indication–
Pentozoeine–
Verapamil –
Dose -2ml -5mg ,120-240 mg daily in divided doses or IV 2.5 to 5mg slow IV bolus upto10 mg.
MgSo4 –
Lorazepam–
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 –
Dose – 1-2 mg /kg /h IV infusion needed to maintain urine ph b/w 7.5 &8.5.
Nifedipin–
Normal saline –
Dose – 20 mg/kg
Hydrocortisone –
Salbutamol nebulization –
Ipratropium –
Paediatric- 20ug 1dose inhaler (MDI) w9 spacer ,2-4 puffs every 20 minutes in 1st hour.
Aspirin –
Morphine –
Frusemide–
Dose - 20-40 mg IV
Diazepam –
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–
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 –
Nursing action –
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
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
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
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–
TNF inhibitors –
Mainly used in autoimmune disease
Nursing action-
Useful in acute transplant rejection, steroid resistant cases ,depletion T-cells from the donor bone marrow before
transplantation.
Nursing action –
It is used to suppress acute allograft Rejection episodes among steroid resistant cases.
Nursing action –
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:-
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 :-
Within 1-4 days, I’sed serum transanina Jaundic, liver tenderness & prolonged.
Sing& symptoms –
Dehydration
Hyperpyrexia
Gastrointestinal
Irritation
Vomiting
Acid-base imbalance
Restlessness, tremors, delirious
Hallucination
Metabolic acidosis
Convulsions, coma 4 death.
Management :-
Alkaline divresis with sodium bicarbonate & divretic like frusemide is given along with IV fluids.
Morphine & other opioids poisoning :-
Respiratory depression
Management :-
Maintenance of B.P., Gastric lavage with potassium permanganate or renove unabsorbed drug,
Organophosphorous poisoning :-
Sing& symptoms : -
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 :-
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.
Extracrdiac :- Anorexia, nausea, vomiting & dearrhea, weakness, confusion, Halluition, blurred vision.
Stop digitalis
Hypotension
There are reports of even 15 ml of methnat causing blindness, death is due to respiratory failure.
Management :-
CNS depression , dilated pupils, slured speech, nausea, vomiting, tachycoralie circulatory collapse, hypothermia,
stupor& coma.
Management :-
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 :-
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 –
S/S –
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 –
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
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.
#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.
#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.
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.
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.
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.
(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.
#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.
(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.
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.
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.
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.
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.
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.
#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.
#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.
#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.
#Creams –
Creams are emulsions which are either water dispersed in oil
[oil creams or oil dispersed in water [aqueous cream]]
#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
#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
#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.
#Adverse effects –
- Dizziness cirehonism, skin-eruptions, epigastric, discomfort,
pepticulcer& bleeding hypersensitivity reaction.
#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.
#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.
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.
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.
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.
*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.
*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.
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
- 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.
#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.
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
#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.
#Classification:-
Sedative Hypnotics
[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
#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.
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.
- Long acting –
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
*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.
*Classification –
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.
*Medullary paralysis –
Respiration ceases cardio vascular collapse may occur if
respiration arrest is not corrected by resuscitative measures.
Inhalational Intravenous
I. Inhalation Anesthetic –
MOA –
After inhalation
*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.
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.
(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.
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
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 .
*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.
*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.
*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
*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.
#Mode of Action –
Antidepressants Drugs
*Classification –
1) Tricyclic Antidepressants :-
* Amitriotyline [Endep]
* Desipramine [Norpramin]
* Imipramine [Tofranil]
* Nor-triptyline [Aventyl]
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
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.
MOA –
Increase amount of nor-epinephrine.
Release Catecholamine
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.
*MOA –
SSRIs
*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.
*Side effects –
- Dry mouth, Constipation, sedation, light headaches.
-Tetracyclic drugs are less likely to cause sexual dysfunction,
significant long term. gain, sleep disturbances.
*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
CT flow in neuron
#Pharmacatherapeutic –
Generalized Anxiety, sedative & hyponotic effects.
- Seizures disorder, major depression.
- Skeletal muscle spasm, insomnia, panic attack, preoperative
anxiety.
#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.
#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.
*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.
#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
Antiparkinsonian Drug
#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.
*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.
#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.
#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.
*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.
*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.
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.
*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.
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
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 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]
*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.
Unit – 10
Drugs used in Cardiovascular System
*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.
* 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.
*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.
#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.
Types of Hormone –
Hormones are secreted by the endocrine or ductless gland.
There are –
All hormones are done in 1st year, anatomy & physiology.
#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 –
- 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.
#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.
#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
#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.
#Ionic inhibitors –
They are the competitive inhibitors of thyroidal I –
Transport Via The Na/I symporter.
- Block the reuptake of iodine by the gland.
Drugs –
Lugol’s solution *5% iodine in 10% potassium iodide
solution] Iodide [N/K]
Trade Name –
Lugol’s solution, colloid iodine 10% collosal.
#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
#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.
#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.
#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.
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.
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).
To delta -5-pregnenolone
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
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 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
COMPLEMENTARY THERAPIES
When CAM therapies are used in combination with other conventional therapies referred
as complementary therapies.
Unit - 12
2. Mind-Body Interventions
3. Biologically-Based Therapies
5. Energy Therapies
► 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.
► Acupuncture
► Ayurveda
►Homeopathy
►Naturopathic medicine
Acupuncture
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
►There are numerous theories about how acupuncture works. Some of them are:
► Sinusitis
► Common cold
► 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
► Bleeding
► Fainting
► Seizure
CONTRAINDICATIONS...
► Thrombocytopenia
► Skin infection
► Semi permanent needles should not b used in a person with vascular heart disease
because of the risk of infection.
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
► 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.
► 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.
► 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.
► Diet
► Herbal medicine
► Yoga
► Meditation
► Exercise
► Massage:
►Anemia
►Arthritis
►Asthma
►Back Ache
►Bleeding Gums
►Blood Dysentery
►Bronchitis
►Cancer
► Chicken Pox
►Cholera
► 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.
► Diarrhea
► Migraines
►Motion sickness
► The flu
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.
4. Naturopathy:
► Naturopathy uses body's natural healing abilities in prevention and treatment of disease
through a healthy lifestyle.
► 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.
►Weight loss
►Fatigue
►Mild depression
►Mood swings
►Allergies
►Arthritis
CONTD...
►Sleep problems
►Poor immunity
►Arthritis
►Slow metabolism
►General wellbeing
TYPES OF NATUROPATHY
► REBALANCING FOOD
►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).
►Relaxation
►Hypnosis
►Biofeedback
►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
► 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
► 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.
►Instruct the client to slowly repeat and finish either in a low voice of the following
sentence
► Instruct the client to repeat and complete each sentence 4 times, the 3 times then twice
and finally once.
► Instruct client to get into a comfortable position and to close eyes and listen to music
through the headset.
CLINICAL APPLICATION:
►Stress Control
►Pain Management
►Heart disease
►High blood pressure
► Infertility
►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 BP
►Lowering BP
►tension
►Depression
►Anxiety
LIMITATION OF RELAXATION THERAPY
► Feeling they are floating and experiencing relaxation induced anxiety related to
theses feelings.
3. Hypnosis
►Hypnosis is a sort of conscious sleep or trance that can help people deal with addictions,
pain or anxiety disorders.
►A hypnotized person follows the instructions given by the hypnotherapist and tends not
to be to psycho logic stress and conflict.
►Habit Disorders
► Habit Disorders
►Relaxation
►Anxiety States
►OCD
►Psychotic Disorders
►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.
►Temperature biofeedback
► EMG biofeedback
►EEG biofeedback
►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
►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.
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.
►Minor burns
►Wound healing
►Hypertension
►Diabetes
►Nausea
►Vomiting
►Motion sickness
[Link] Medicine
CLINICAL APPLICATIONS
►Arthritis
►Cardiovascular disease
►Hypertension
►Beriberi
►Night blindness
►Osteomalacia
►Pernicious anemia
►Rickets
►Scurvy
► Xerophtalmia
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
►It differs from chiropractic in its underlying theory that it is impairment of blood supply
and not nerve supply that leads to 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.
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.
►Stress
►Arthritis
►Endometriosis
► Insomnia
►Depression
►Migraines
►Hot flashes
►Cramps
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
►Physical abused
►Psychiatric diseases.
3. Bioelectromagnetic-based Therapies
Clinical applications -
►Osteoporosis
► Arthritis
►Pain
Contraindications
►Pregnancy
►Myasthenia gravis
►Malignancies
►Psychoses
►Organ transplant
►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 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.