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1 Pharmacology

Patho -pharmacodynamics

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0% found this document useful (0 votes)
28 views112 pages

1 Pharmacology

Patho -pharmacodynamics

Uploaded by

schow023
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPTX, PDF, TXT or read online on Scribd

Welcome to: Nurs 2112

Integrated… pathophysiology,
pharmacology & therapeutics

Pathophysiology

Pharmacology Therapeutics
Dr. Mohamed El Hussein NP, PhD

Contact Information
Email: melhussein@[Link]

Office Y456
•[Link]
Weekly Modules
• Posted on BB
• Contain questions to focus required
readings
• Required readings
• Preparation for class and lab
• Use as a study guide
4

How do you learn best?


• Learning strategies
– Interactive activities
– Student participation

• Learning approaches
– Critical questioning
– Student narrative
Tips to be Successful in this
Course
• Complete the modules ahead of time

• Use the lecture slides and notes to help


focus your readings towards key
information

• Form a study group of 3-4 people, practice


teaching difficult concepts to each other

• Plan out your time!


Tips to be successful in this
course
• Think about your work-life balance for
the term.
• Ask questions!
• Book to come and see me if you need
help or do not understand a concept.
Meetings
• Google meet !!
• Send me an invite !!
Pharmacology for Nurses: A Pathophysiological Approach
Third Canadian Edition

Chapter 9
Principles of Drug
Administration

Copyright © 2021 Pearson Canada Inc.


Pharmacology (1 of 2)
• Pharmacology – study of medications
• Drug – substance capable of producing a biologic
response
• Medication – a drug given for the purpose of
producing a therapeutic response
Drug Outcome
Ten Rights of Drug
Administration=assessment
• Right patient / client
• Right history and assessment
• Drug approach and right to refuse
• Right drug
• Right dose
• Right route of administration
• Right time and frequency of delivery
• Right documentation
• Right drug-drug interaction and evaluation
• Right education and information for patient
Three Checks of Drug Administration
• Prior to administering a drug, the nurse should be
checking the drug with the Medication
Administration Record (MAR)===To avoid med
error=under aeesessment
– Check when removing the drug from the storage site of
the drug
– Check when preparing the drug for administration
– Check again just before administering the drug to the
patient
Drug Order Abbreviations
• Common types of orders
– Single order – to be given once
– Continuous order – to be given on an ongoing basis
(IV fluids or medications like insulin being infused
throughout the day.)
– Standing order – routine order, prewritten to be used
in a particular circumstance==only be activated at a
certain time
– PRN order – to be given as required
Drug Order Abbreviations
Table 9.2 Drug Administration Abbreviations
Abbreviation Meaning Abbreviation Meaning
ac before meals qd every day*
ad lib as desired/directed qh every hour
AM morning qhs bedtime (every night)*
bid twice per day qid four times per day
cap capsule qod every other day*
/d per day q2h every 2 hours (even)
Gtt====gyatt drop q4h every 4 hours (even)
h or hr hour q6h every 6 hours (even)
hs hour of sleep/bedtime q8h every 8 hours (even)
Drug Order Abbreviations
[Table 9.2 Continue]
Abbreviation Meaning Abbreviation Meaning
no number q12h every 12 hours
pc after meals; after eating Rx take
PM afternoon STAT immediately; at once
PO by mouth; orally tab tablet
PRN or prn when needed/necessary tid three times per day
q every

*The Institute for Safe Medication Practices recommends the following changes to avoid medication
errors: for qd, use “daily” or “every day”; for qhs, use “nightly”; for qod, use “every other day.”
Routes of Administration – Enteral
• Refers to oral administration of drugs but also
include gastric and nasogastric routes, buccal and
sublingual routes,rectal=GI=Gastrointestinal
• Sublingual (given last)/ Buccal (Against the
cheek)=no first pass effect(only in oral)
– Drug diffuses across mucosal tissues into blood
– Sublingual absorption faster than buccal,because
of increased vascularity

Not given when patient unconscious,med go to trachea


instead of esophagus(aspiration)
Routes of Administration – Enteral
• Formulations – follow instructions for
administration carefully
– Tablets / Capsules
▪ Enteric coated – protection from stomach acid ( protect from
stomach,to be broken in small intestine slowly)=not in
emergency
▪ Sustained release – dissolve slowly to extend duration of
medication-ER/XR/SR
– Elixirs (Alcohol) / Syrups(Sugar / Suspensions
(shake)
▪ Ensure drugs are shaken before preparing
– Gastric / Nasogastric
▪ Usually liquids
Routes of Administration – Enteral
• Advantages
– Most common route; easy to administer
– Considered to be safest route; drug can be recovered
from stomach in case of an error=vomiting
– Large surface area for absorption
– Subject to first pass metabolism if drug absorbed in
small intestines
– Flexible formulations – enteric coated and sustained
release
Routes of Administration – Enteral
• Disadvantages
– Client must be conscious and able to swallow
– Can be challenging for some pediatric and geriatric
patients with difficulty swallowing
– Drugs can be rendered inactive by stomach acid and
gastric / intestinal enzymes
– Subject to first pass metabolism if drug absorbed in
small intestines
– GI motility (peristaltic movt)can affect
bioavailability=Delayed movement to the small intestine
(the main absorption site) leads to delayed onset of
action.
Routes of Administration – Topical
• Refers to administration of drugs onto the surface
of the skin or of membranous linings of eye, ear,
nose, respiratory tract, urinary tract, vagina and
rectum
• Formulations
– Dermatologic – creams, lotions, gels, powders, sprays
– Inhalations for respiratory tract – inhalers,
nebulizers, positive pressure devices
– Instillations and irrigations=Solutions applied to
mucous membranes, such as eye or ear drops.
Routes of Administration – Topical(patches)
• Local effects – topical administration is often
used to produce an effect at the place it is applied
– Unintended adverse effects usually due to drug being
absorbed into circulation
• Systemic effects – some drugs given topically
are absorbed into blood to produce effects
throughout the body
– Slow release preparations
Routes of Administration – Topical
• Advantages
– Can be formulated and applied to achieve local or
systemic effects
– Application is directly to the site of intended action
– Fewer adverse effects than enteral or parenteral routes
– No first pass metabolism or digestion by enzymes
– For some routes, patient does not have to be
conscious
Routes of Administration – Topical
• Disadvantages
– Can be irritating to site of administration
– Local application can produce systemic adverse effects
Routes of Administration – Parenteral
=blood
• Refers to routes in which a drug is injected
– Subcutaneous, dermal
– Intramuscular
– Intravenous, intraarterial
– Intrathecal
– Intraosseous
– Intraperitoneal
Routes of Administration – Parenteral
• Advantages
– Absorption is often more rapid, depending on blood
supply to site of injection(muscle fast>fat)
▪ Intravenous is the standard for measuring bioavailability
– Alternate route for administration for patients that can’t
take drug enterally
– Effects can be local or systemic depending on
preparation and route=drug acts only at or near the site
of administration without affecting the rest of the
[Link]:Intradermal injection (e.g., tuberculin
test): The effect is limited to the skin [Link]
anesthetics (e.g., lidocaine injections): Used to numb a
specific area before surgery or procedures.
Routes of Administration – Parenteral
• Disadvantages
– Risk of infection
– Irritation at site of injection
– Once drug has been administered, it cannot be
removed if an error has been made
Pharmacokinetics
• Refers to the movement of a drug through the
body
• Describes what the body does to a drug as it
enters the blood, as it moves to target tissues, as
it is metabolized and as it is removed from the
body
– Drugs must pass a series of barriers to reach target
tissue
– Depends on physiologic processes
Pharmacokinetics
• Drug must reach target tissue at high enough
concentration to produce a therapeutic effect
(higher absorption-loading dose)
• Nurse must be aware of how many factors may
impact of drug that reaches target tissue
– Route of administration
– Patient characteristics
Pharmacokinetics
• Four Processes of Pharmacokinetics=ADME
– Absorption
▪ How drug reaches the circulation
– Distribution
▪ How drug reaches target tissue
– Metabolism
▪ How drug is altered by body=LIPID SOUBLE TO WATER
SOLUBLE FOR EXCRETION
– Excretion
▪ How drug is removed from body
Transport Across Membranes
• Diffusion
– Movement of a chemical from an area of higher
concentration to an area of lower concentration (conc
gradient)
– Does not require energy(no carrier/channel)
• Simple diffusion
– Diffusion across a membrane
– Rate of diffusion affected by concentration gradient,
properties of chemical, properties of membrane
Transport Across Membranes
• Properties of drugs that affect diffusion across
plasma membranes
– Concentration gradient
▪ Related to dosage of drug—higher dose-more diffusion
– Size of drug molecule
▪ Smaller molecules absorbed faster-more likely to be diffused
– Lipid solubility
▪ Structure of molecule
▪ Ionization /charged of molecule, influenced by pH=not
absorbed
▪ Lipophilic drugs cross membranes more easily than
hydrophilic drugs
Transport Across Membranes
• Facilitated Diffusion
– Diffusion across a membrane that requires a
transport protein
▪ Ion channels
▪ Cotransporters, antiporters
– Show specificity and saturation kinetics=Each
transport protein is specific to a certain type of
molecule
– Do not require energy though concentration gradient
for diffusion may be maintained through active
transport
Transport Across Membranes
• Osmosis
– Diffusion of water down its concentration gradient (high
to low)
• Active Transport
– Movement of a substance from area of low
concentration to area of high concentration=Against
conc gradient
– Requires a transport protein
– Requires source of energy, usually ATP
– Shows specificity and saturation kinetics
Absorption
• Movement of drug from site of administration
to circulation-moving into the blood
– Primary factor for determining onset of drug action(as
soon as absorbed ,sooner action) (empty stomach-
absorbed better)
– Quantified as bioavailability(once it moves to the blood)
• Factors affecting rate of absorption
– Route of administration
▪ Enteral, parenteral, topical
▪ Increase dose = increases rate of absorption due to
increased concentration gradient
Absorption
• Factors affecting rate of absorption
– GI tract environment
▪ Presence of food may decrease absorption
▪ Presence of certain foods and drugs may alter rate of
absorption =High-fat meals may delay drug absorption.
▪ Motility – influences time during which absorption can occur
– Blood flow and surface area
▪ Increase blood flow = increase rate of absorption
▪ Increase surface area = increase rate
▪ Route of administration
▪ Impact of temperature on blood flow=Warm temperatures
increase blood flow, enhancing absorption.
Absorption
• Factors affecting rate of absorption
– Drug ionization
▪ Depending on pH of surrounding fluid, most drugs in either
charged or uncharged state
▪ Acids are absorbed in acids because they are nonionized.
▪ Bases are absorbed in bases because they are nonionized.
▪ Acid in a basic environment is ionized and therefore less able
to cross membrane
• Can you influence?
• Antacids?
• Increase absorption curve: Antacids can
enhance drug absorption by altering pH,
especially for weak [Link] elimination
curve: Antacids can reduce the rate of elimination
by slowing drug metabolism or absorption
changes.
Clinical Correlate
To Change Urinary pH
• Acidify: NH4Cl, vitamin C, cranberry juice
• Alkalinize: NaHC03, acetazolamide
(historically)
Distribution
• Transportation of drugs throughout body to target
tissue(Albumin take meds to site of action)
• Factors affecting distribution of drug
– Blood flow to target tissue
▪ Increased blood flow = more drug reaching target tissue
– Drug solubility
▪ Hydrophilic drugs transported in solution
▪ Lipophilic drugs – a portion is bound to plasma proteins (ie
albumin); a portion of drug is in solution(to enter blood plasma)
Distribution
• Factors affecting distribution of drug
– Drug-protein binding
▪ Lipophilic drugs in equilibrium between being in solution and
being bound to plasma protein
▪ Only portion of drug in solution is available to diffuse to target
tissue
▪ Properties of drug allow some lipophilics to bind better to
plasma proteins than others – competition for binding sites on
plasma proteins can create drug interactions
Distribution
• Drug must move from circulation to target tissues
to create response
• Special barriers to drug distribution
– Blood–brain barrier
▪ Does not contain pores
▪ Protects brain from pathogens and toxins
▪ Only lipid-soluble drugs able to cross
▪ Not fully developed in neonates
▪ Inflammation can increase permeability.
Distribution
• Special barriers to drug distribution
– Fetal–placental barrier (FPB)
▪ Prevents harmful substances from passing from mother's
blood stream to fetus
▪ Permeability of barrier changes during pregnancy
▪ However, some drugs can cross (alcohol, cocaine, caffeine,
some prescription meds)
▪ Pregnancy categories for drugs=A
▪ Must consider if patient is of childbearing age prior to
prescribing a drug.
Metabolism/biotransformation
• Metabolism is a process that changes the
activity of a drug and makes it more likely to
be excreted.
Metabolism
• Process by which structure (and function) of
drugs, nutrients, vitamins, and minerals is altered
– Liver is primary site for metabolism
– Metabolism usually makes drug more excretable
(hydrophilic)
▪ Drug in solution can be filtered by kidney
▪ Drug bound to plasma protein not filtered=NOT FREE
Metabolism
– Structural changes result in functional changes to drug
▪ Metabolites may be functional (metabolism activates drug);
inactive form is termed “prodrug”
▪ Metabolites many be non-functional (metabolism inactivates
drug)
▪ Metabolites may be toxic
Metabolism
• Drugs and toxins are seen as foreign to patients
bodies
• Drugs can undergo metabolism in the lungs,
blood, and liver
• Body works to convert drugs to less active forms
and increase water solubility to enhance
elimination=prevents the drug from building up
and causing toxic effects.
Metabolism
• Microsomal enzymes in liver carry out most
metabolic activities
– Cytochrome P450 (CYP)-family of enzymes of
liver(CYP 3A4)
▪ An enzyme that metabolizes many drugs
▪ Many isoenzyme systems within CYP
– Determine speed at which drug is metabolized
Metabolism
• Liver - primary route of drug metabolism
• Liver may be used to convert pro-drugs
(inactive) to an active state
• Types of reactions
– Phase I (Cytochrome P450 system)-easily leave body
– Phase II-conjugate-(linked to another molecule like
glucuronic acid, sulfate, or glutathione) =make more
water soluble-leave by poop=enterohepatic
circulation(liver-gall bladder)
=meds have long duration of action=have a longer half-
life
Phase I reactions types
• Hydrolysis
• Oxidation
• Reduction
• Demethylation
• Methylation
• Alcohol dehydrogenase metabolism
Phase II reactions
• Polar group is conjugated to the drug
• Results in increased polarity of the drug
• Types of reactions
– Glycine conjugation
– Glucuronide conjugation
– Sulfate conjugation
Phase I reactions
• Cytochrome P450 system
• Located within the endoplasmic reticulum of
hepatocytes
• Through electron transport chain, a drug bound
to the CYP450 system undergoes oxidation
or reduction=Conversion of prodrugs (inactive
drugs) to their active forms, such as codeine
being metabolized into morphine.
• Enzyme induction/INHIBITION=Grapefruit
juice inhibits CYP3A4, increasing the levels of
Metabolism
• Contribute to drug‒drug interactions
– Drugs are substrates for CYP
▪ presence of one drug may alter metabolism of another drug by
competing for same isoenzyme
– Drugs can inhibit CYP enzymes=GRAPEFRUIT
▪ Inhibiting isoenzyme could reduce metabolism of another
drug → toxic levels
– Drugs can induce CYP enzymes=SMOKING
▪ Inducing isoenzyme could increase metabolism of another
drug → reduce amount of functional drug
Primary Processes of
Pharmacokinetics
• Metabolism
– Alters structure and function of drugs, nutrients,
vitamins, and minerals
– Primary site is liver.
– Changes to drug structure allow for excretion.
– Functional changes alter pharmacological
activity.
▪ Metabolites may be more toxic.
Metabolism
• Ability of patient to metabolize drugs changes
throughout life cycle
– Infants lack mature microsomal enzyme systems.
– Enzyme activity often reduced in older adults
• Ability of patient to metabolize drugs influenced by
many factors
– Decreased metabolism with liver impairment
– Genetic variations of CYP enzymes-genetic
polymorphism
Excretion
• Removal of drug from the body
– Kidney is primary site for excretion
– Pulmonary, glandular, fecal excretion
– Rate of excretion influences concentration of drug in
blood
• Renal excretion
– Most drugs are filtered into the nephron but not
reabsorbed (drug remains in urine)
– pH of urine can influence reabsorption of drug from
nephron
Excretion
• Renal excretion
– Damage to kidney usually reduces excretion of drug
thus dose reduction may be necessary for renal
patient
• Pulmonary excretion
– Gases and volatile liquids
– Most drugs excreted unmetabolized
– Respiratory rate and blood flow affect excretion.
Excretion
• Glandular secretion
– Drugs can be secreted in saliva, sweat, breast milk
– Consideration for nursing mother
• Fecal and biliary excretion
– Drugs taken via enteral route may not be fully
absorbed and are excreted in feces
– Enterohepatic recirculation
▪ Lipid soluble drugs can be reabsorbed with bile via
enterohepatic recirculation → decreases rate of
excretion=slow onset=half life increased
Time-Response Relationships
• Goal of nurse is to maintain drug at a
concentration (therapeutic range) in blood that
produces a therapeutic response
– Plasma drug levels rise as drug is absorbed and then
decrease as drug is excreted
– If plasma levels exceed the therapeutic range (toxic
range), drug is more likely to produce more adverse
effects
– Therapeutic range can be very narrow
Time-Response Relationships
• Onset – time from point at which drug is
administered until it reaches a therapeutic
range
• Duration – time period in which drug
concentration is in a therapeutic range
• Termination – time period from when drug is
administered until its concentration drops out of
a therapeutic range
Time-Response Relationships
• Drug half-life (t1/2)
– Provides estimate of duration of action
– Time that it takes for the plasma concentration of a
drug to be reduced by 50%
– Drugs with short half-life have to be given more
frequently to maintain drug in therapeutic range(4-5
half lifes to reach therapeutic range and to get out of
body-go below mec)
– Drugs with long half-life can be given less frequentl
Clinical Application
• Patient comes to ER, 5mg drug in body. Said she
dosed 8hours ago
• How much did she ingest? Half life 4 hours
Time-Response Relationships
• Maintaining plasma concentration within
therapeutic range requires careful dosing
– Must consider magnitude and frequency of dose, as
well as drug half-life
▪ More than 90% of drug is excreted after four half-lives
– Repeated dosing required to maintain steady plasma
concentration of drug
▪ Next dose given before plasma concentration dips out of
therapeutic range
Time-Response Relationships
• Sometimes it is important for a drug to reach a
therapeutic range more quickly
• Loading dose is given
– Larger dose that leads to more rapid absorption and
shorter onset of action
– Maintenance doses are given to maintain drug within
therapeutic range
Pharmacodynamics
• Refers to what the drug does to the body to create
a response
– Related to the mechanism of action of a drug
– Related to how a drug interacts with a target tissue
▪ Altering the activity of a cell through interactions with
receptor
▪ Altering the activity of an enzyme
Pharmacodynamics
• Nursing Process
– Recognizing that there is considerable variation in
client response to a particular dose of a drug
– Recognizing consequences of giving too much or too
little of a drug in terms of therapeutic response, risk of
adverse effects
– Application of pharmacodynamics critical for safe and
responsible administration of medications
Interpatient Variability
• Response to dose of drug is normally distributed
across a population-difference in receptor
– Some people require a very small dose to produce a
therapeutic response (left side of curve in figure 4.1)
– Some people require a very large dose to produce a
therapeutic response (right side of curve)
– Most require a dose in the middle to produce a
therapeutic response
Median Effective Dose (ED50)
Interpatient Variability – ED50
• Dose at which 50% of a population exhibit desired
therapeutic response
• Clinical implications
– predicts dose range to achieve therapeutic response
– ED50 may be toxic for some patients and may not
produce a meaningful response in
others=INTERPATIENT VARIABILITY
– Critical to monitor patient response to assess if dosage
adjustment is indicated
TD50 and LD50
• Normal frequency distributions exist for both the
dose of drug at which it is toxic and at which it is
lethal for test subjects
– TD50 refers to median toxic dose
▪ Dose at which 50% of test subjects exhibit a response
indicative of toxicity
– LD50 refers to median lethal dose
▪ Dose at which 50% of test subjects are killed by drug
Therapeutic Index (TI)
• Measure that compares LD50 to ED50 using a ratio
• TI = LD50 / ED50
• If a drug has a large TI, it is considered to be safer
(upper panel of figure 4.2) than a drug with a
smaller TI (lower panel of figure 4.2)
Therapeutic Index
Margin of Safety (MOS)
• Dose of drug that is lethal to 1% (LD 1; left tail of
orange curve in figure 4.2) of animals divided by
dose of drug that produces a therapeutic effect in
99% (ED99; right tail of green curve in figure 4.2) of
animals
– MOS = LD1 / ED99
– Drugs with a large TI will also have a larger MOS
Graded Dose-Response Relationship
• Describes relationship between dose of drug and
intensity of drug response
– See figure 4.3
• Sinusoidal curve with three distinct phases
– Phase 1: occurs at low doses; very little change in
response as dose increases
– Phase 2: linear phase; sharp increase in response as
dose is increased
– Phase 3: plateau phase; no change in response as
dose increases
Graded Dose-Response Relationship
Graded Dose-Response Relationship
• Phase 2 is best range of doses to achieve a safe,
therapeutic effect
• Response to drug usually due to several
mechanisms
– More receptors being affected by drug
– More enzymes being affected by response
– Patient symptoms affected by drug
▪ ie patient has a headache and feels better after taking
medication
Graded Dose-Response Relationship
• Phase 1
– Few receptors or enzymes affected, therefore response
is minimal
• Phase 2 – linear phase
– As more receptors or enzymes are affected, intensity of
response increases
• Phase 3 – plateau phase
– Drug is bound to all receptors or enzymes, or
symptoms have been alleviated. Increasing dose has
no further effect
Potency and Efficacy
• Even within a pharmacologic class, not all drugs
produce the same intensity of response
• Two measures are commonly used to quantify and
compare elements of graded dose-response
curves
– Potency
– Efficacy
Potency and Efficacy
• Potency=first touch=high affinity
– Amount of drug required to produce a particular
intensity of response
– drug that requires lowest dose to produce particular
intensity of response is most potent (see figure 4.4,
upper panel)
• Efficacy-more important
=EFFECTIVE=continue stimulation
– Maximum intensity of response produced by a
particular dose of drug
– Drug with greatest intensity of response has highest
efficacy (figure 4.4, lower panel)
Potency and Efficacy
Receptor Theory
• Most drugs influence biological response through
interactions with cellular receptors
• Receptor
– Cellular molecule to which a medication binds to
produce its effects
– Intrinsic activity – ability of drug to bind receptor and
produce biological response
– Most drugs enhance or inhibit a physiological
process.
Receptor Theory
• Receptors are only activated or inhibited by
chemicals that bind like lock and key
• When receptor is bound by its ligand, intracellular
response is triggered
– Responses carried out by second messenger systems
within the cell
– Responses can be short term (opening of channels)
– Responses can be long term (transcription and
translation of genes)=LIPID SOLUBE DRUGS
83

Mechanism of Hormone Action


• Water-soluble hormones circulate in free, unbound
forms
– QUICK,Short-acting response
– Bind to surface receptors
• Lipid-soluble hormones are primarily circulating
bound to a carrier
– Rapid(SLOWER) and long-lasting response
– Diffuse freely across the plasma and nuclear
membranes and bind with cytosolic or nuclear
receptors
Copyright © 2019, Elsevier Canada, a division of Reed Elsevier Canada, Ltd. All rights reserved.
84

Mechanism of
Hormone Action (Cont.)
• Hormone receptors
– Located in the plasma membrane or in the
intracellular compartment of the target cell

Copyright © 2019, Elsevier Canada, a division of Reed Elsevier Canada, Ltd. All rights reserved.
85

Mechanism of
Hormone Action (Cont.)
• Water-soluble • Lipid-soluble
hormones hormones
– High molecular weight – Easily diffuse across the
– Cannot diffuse across plasma membrane and
the plasma membrane bind to cytosolic or
nuclear receptors

Copyright © 2019, Elsevier Canada, a division of Reed Elsevier Canada, Ltd. All rights reserved.
Copyright © 2021 Pearson Canada Inc. 3 - 85
Agonists and Antagonists
• Within a pharmacologic class, some drugs are
better at stimulating intracellular responses than
others
• Agonist
– Mimics the action of endogenous substances;
response may be greater than endogenous activity.
• Partial Agonist
– Produces weaker responses than endogenous
substances
Agonists and Antagonists
• Antagonists=inhibit
– Prevent action of endogenous substances, usually by
competing with endogenous ligand and/or agonist for
receptor binding sites
– Sometimes used to prevent adverse effects of
overdoses
– Antagonists do not usually have intrinsic
activity=Narcan,naloxone,beta blocker(lower blood
pressure)
– =because they bind to the receptor but do not
activate it or produce any effect themselves.
Pharmacogenetics
• Branch of pharmacology that studies the role of
genetic variation in drug responses.
• Considers underlying genetic expression as
reason for why drug therapy not effective for
everyone
• Using data from human genome project, genetic
differences in drug-metabolizing enzymes have
been discovered; opens door to individualized
drug therapy
Source: Davis Drug Guide
Try this thinking
exercise!
Rank these various drug preparations in
order
of the fastest absorption to the
4 slowest
A. Capsules
B. Suspensions 2
C. Powders 3
D. Liquids, elixirs, and 1
syrups 7
E. Enteric-coated tablets 6
F. Coated tablets 5
G. Tablets 8
H. Extended release
Holistic Approach to Pharmacotherapy
• Patients can respond differently to the same
medication
• Response can be influenced by psychological,
cultural and social variables in addition to
biological ones
• Variations can also be due to individual
differences in genes and their expression
Genetic Influences on Pharmacotherapy
• Humans of all races share DNA that is 99.8%
identical
– Remaining 0.2% can result in differences in
responsiveness, often along ethnic lines
• Genetic polymorphism
– Mutation in gene that codes for a protein resulting in
two or more versions of same protein
▪ Mutated form of enzyme has changed structure.
▪ May increase, decrease speed of drug metabolism or may be
non-functional
Genetic Influences on Pharmacotherapy
• Genetic polymorphism (example
– Acetyltransferase metabolizes isoniazid, a drug for
tuberculosis
– Caucasians, African Americans are slow acetylators
thus isoniazid concentration can reach toxic levels
quickly, thus may require lower or less frequent dosing
– Japanese are rapid acetylators thus may require more
frequent dosing
• Genetic Testing for CYP450 Polymorphisms to
Predict Response to Clopidogrel: current evidence
and test availability
• Application: Pharmacogenomics
• [Link]
3252/#:~:text=Genetic%20testing%20to%20deter
mine%20if,high%20risk%20for%20poor%20outco
mes
.
Pharmacogenetics and Pharmacogenomics
• Pharmacogenetics
– Study of specific genetic variations that alter patients'
responses to medications=Genetic polymorphisms
• Pharmacogenomics
– Network of genes that govern a person's response to
drug therapy
Gender Influences
• Current research recognizes gender difference
in drug response
• Factors that influence response
• Body composition (fat to muscle ratios can affect
pharmacokinetics of drug)=Fat-to-Muscle Ratio:Women generally
have a higher body fat percentage compared to men.

• Fat-soluble drugs (like diazepam or anesthetics) may accumulate in fat tissues, causing
prolonged effects in women.

• Water-soluble drugs are distributed more quickly in men due to their higher muscle mass and
lower fat.

– Cerebral blood flow variations may affect distribution of


analgesics to CNS
Gender Influences
• Woman tend to pay more attention to changes,
seek health care earlier than men.
• May affect adherence to medication regimen of
drug class
– Antihypertensive drugs
▪ May produce impotence, gynecomastia in men
▪ Abrupt withdrawal may cause strokes
– Estrogen in oral contraceptives
▪ Elevated risk of thromboembolic disorders in women
Nursing Process
• 5 step process
– Assessment
– Nursing Diagnosis=Identifying patient health problems
based on data, To prioritize
– Planning=Setting goals and deciding interventions.
– Implementation
– Evaluation=Determining the effectiveness of the care
plan.
Assessment
Table 5.1 Health History Assessment Questions Pertinent to
Drug Administration
Health History Component Pertinent Questions

Chief complaint • How do you feel? (Describe.)


• Are you having any pain? (Describe.)
• Are you experiencing other symptoms? (Especially pertinent to medications are nausea,
vomiting, headache, itching, dizziness, shortness of breath, nervousness or anxiousness,
palpitations or heart “fluttering,” weakness, and fatigue.)
Allergies • Are you allergic to any medications?
• Are you allergic to any foods, environmental substances (e.g., pollen or “seasonal”
allergies), tape, soaps, or cleansers?
• What specifically happens when you experience an allergy?
Past medical history • Do you have a history of diabetes, heart or vascular conditions, respiratory conditions, or
neurological conditions?
• Do you have any dermatological conditions?
• How have these conditions been treated in the past? How are they being treated
currently?
Family history • Has anyone in your family experienced difficulties with any medications? (Describe.)
• Does anyone in your family have any significant medical problems?
Assessment
[Table 5.1 Continued]
Drug history • What prescription medications are you currently taking? (List drug name, dosage,
frequency of administration.)
• What non-prescription/over-the-counter (OTC) medications are you taking? (List drug
name, dosage, frequency.)
• What drugs, prescription or OTC, have you taken within the past month or two?
• Have you ever experienced any side effects or unusual symptoms with any medications?
(Describe.)
• What do you know, or what have you been taught, about these medications?
• Do you use any herbal or homeopathic remedies? Any nutritional substances or vitamins?
Health management • When was the last time you saw a healthcare provider?
• What is your normal diet?
• Do you have any trouble sleeping?
Reproductive history • Is there any possibility you are pregnant? (Ask every woman of childbearing age.)
• Are you breastfeeding?
Personal and social history • Do you smoke?
• What is your normal alcohol intake?
• What is your normal caffeine intake?
• Do you have any religious or cultural beliefs or practices concerning medications or your
health that we should know about?
• What is your occupation? What hours do you work?
• Do you have any concerns regarding insurance or the ability to afford medications?
Health risk history • Do you have any history of depression or other mental illness?
• Do you use any street drugs or illicit substances?
Patient Education
Table 5.2 Important Areas of Teaching for Clients Receiving Medications
Area of Teaching Important Questions and Observations

Therapeutic use • Can you tell me the name of your medicine and what the medicine is used for?
and outcomes • What will you look for to know that the medication is effective? (How will you know that the
medicine is working?)
Monitoring side • Which side effects can you handle by yourself? (e.g., simple nausea, diarrhea)
and adverse • Which side effects should you report to your healthcare provider? (e.g., extreme cases of nausea
effects or vomiting, extreme dizziness, bleeding)
Medication • Can you tell me how much of the medication you are to take? (mg, number of tablets, mL of liquid,
administration etc.)
• Can you tell me how often you are to take it?
• What special requirements are necessary when you take this medication? (e.g., take with a full
glass of water, take on an empty stomach and remain upright for 30 minutes)
• Is there a specific order in which you are to take your medications? (e.g., bronchodilator before
corticosteroid inhaler)
• Can you show me how you will give yourself the medication? (e.g., eye drops, subcutaneous
injections)
• What special monitoring is required before you take this medication? (e.g., pulse rate) Can you
demonstrate this for me? Based on that monitoring, when should you NOT take the medication?
• Do you know how, or where, to store this medication?
• What should you do if you miss a dose?
Other monitoring • Are there any special tests you should have related to this medication? (e.g., fingerstick glucose
and special levels, therapeutic drug levels)
requirements • How often should these tests be done?
• What other medications should you NOT take with this medication?
• Are there any foods or beverages you must not have while taking this medication?
Characteristics of an Ideal Drug
• Effectively prevents, treats or cures condition of
patient
• Easy to administer
• Produces rapid, predictable response at relatively
low doses
• Rapid onset of action
• Duration of action appropriate to reaching
therapeutic goals
• Rapid elimination of drug
Characteristics of an Ideal Drug
• No adverse effects
• No interactions with food or other drugs
• No contraindications – safe for all patients to take
• Inexpensive and accessible
Classification of Drugs
• Therapeutic classification=USE
FOR/INDICATION
– Describes the condition for which a medication is being
given (ie antihypertensive)
• Pharmacologic classification=MECHANISM OF
ACTION
– Describes the mechanism by which the therapeutic
effect is achieved (ie. Beta blockers=Beta blockers
lower blood pressure by slowing heart rate., diuretics,
ACE inhibitors)
• Medications can have multiple classifications
Classification of Drugs
• Indication
– condition or circumstance for which drug has been
approved
– A particular drug may have multiple indications
• Mechanism of action
– Means by which drug carries out a therapeutic effect
▪ ie a diuretic (pharmacologic class) reduces blood pressure
(therapeutic class) by reducing blood volume (mechanism)
Classification of Drugs
• Both therapeutic and pharmacologic
classifications are useful but limited
– therapeutic class identifies purpose of drug (indication)
but not how it works (mechanism of action)
– Pharmacologic class identifies mechanism but not
indication
▪ Multiple pharmacologic classes can be used for a single
therapeutic class
▪ Multiple therapeutic classes can be addressed with a single
pharmacologic class
Classification of Drugs
• Within a pharmacologic class, there are often
many different but related versions of a drug
• Prototype drug – a representative drug from a
class that is used as a point of comparison for
related versions of that drug=Propranolol is a
prototype beta blocker.

– Learning one drug can allow nurse to extend


knowledge to other similar drugs within that class
Nomenclature of Drugs
• IUPAC – scientific name that describes chemical
structure of a drug
– ie 7-chloro-1,3-dihydro-1-methyl-5-phenyl-1,4-
benzodiazepin-2(3H)-one
• Generic – name adopted by regulatory agencies
to describe active ingredient of a drug
– ie diazepam
• Trade – proprietary name used by the company
that produces a drug
– ie valium
Nomenclature
• generic names are preferred as they are
accepted internationally to represent a particular
drug
– Drug given an international non-proprietary name (INN)
specific for that drug
– Ensures safety as generic name is used by all health
care providers to describe same product; no confusion
as to composition of drug
– Can be multiple trade names for a single generic drug
Nomenclature
• Brand name drugs and generic drugs can
usually be found in same dosages
– Generic drugs are usually less expensive than brand
name
– Differences between brand and generic often present
in formulation of drug
– Best measure to compare is bioavailability (the amount
of drug that reaches systemic circulation and that can
interact with target tissues)
– Formulation can affect bioavailability
Drug Schedules in Canada
• All drugs in Canada are categorized into four
schedules requiring varying levels of oversight
Drug Schedules in Canada
Table 2.4 Schedule System for Drugs Sold in Canada
Schedule Description
Schedule I Available only by prescription and provided by a
pharmacist; includes the following:
• All prescription drugs
• Drugs with less potential for abuse: Schedule F
• Controlled drugs: Schedule G
• Narcotic drugs

Schedule II Available only from a pharmacist; must be retained in an


area with no public access
Schedule III Available via open access in a pharmacy or pharmacy area
(over the counter)
Unscheduled Can be sold in any store without professional supervision

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