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