Adams Chapter 52013

PHARMACOLOGY
CONNECTIONS TO NURSING PRACTICE

Second Edition
Pharmacology: Connections to Nursing Practice, Second Edition
Michael Patrick Adams Carol Quam Urban
CHAPTER
Pharmacodynamics
5
Pharmacodynamics
Pharmaco = medicines
Dynamics = change
What the drug does to the body
Involves drug mechanism of action
Involves effect of drug concentration on
body responses
Interpatient Variability
Individuals have different responses to
drugs
Responses are related to:
Doseresponse relationships
Therapeutic index
Drug receptor interactions
Clinical Implications of
Interpatient Variability
Average dose predicts therapeutic
response in 50%
Client may need less or more of a drug
Need to monitor drug effect on client
Dosage adjustment may be indicated
Therapeutic Index
Identifies safety index of drugs
A common drug with a narrow therapeutic index
= Lanoxin dose range is 0.125 0.250 mg
A common drug with a wide therapuetic range is
metoprolol 12.5 mg 100 mg
Median lethal dose (LD
50
)
Lethal to 50% of test subjects
Effective dose (ED
50
)
Desired drug response in 50% of subjects

Median Toxicity Dose
Produces toxicity in 50% of subjects
Extrapolated from clinical trials
Provides practical clinical information
5.3 The doseresponse relationship
describes how the actions of a drug
change with increasing dose.
DoseResponse Relationship
Drug dose correlates to degree of
response
Three phases
Phase 1: lowest phase
Phase 2: most desirable range
Phase 3: plateau reached

Graded dose-responsive curve
Smooth and continuous
Adjust dose changes in small
increments
Plateau of phase 3
Increasing dose will not increase
therapeutic effect
Increasing dose could cause toxicity
Reaches a ceiling
Figure 5.3 Dose-response relationship.
5.4 Potency and efficacy are
fundamental concepts of
pharmacodynamics that describe a
drugs activity.
Potency and Efficacy
Figure 5.4 Potency and efficacy: (a) Drug A has a higher potency than drug B. (b) Drug A has a higher efficacy
than drug B.
Potency and Efficacy
Not all drugs have equal efficacy
Drugs in same class can differ in
potency and efficacy
Potency compares doses of two
different drugs
Most common application is
equianalgesic dose chart
Figure 5.4 (continued) Potency and efficacy: (a) Drug A has a higher potency than drug B. (b) Drug A has a
higher efficacy than drug B.
Efficacy
Greatest maximal response produced
by drug
Compares desired therapeutic effect of
two drugs
5.5 Most drugs produce their actions
by activating or inhibiting specific
cellular receptors.
Receptor Theory
Receptor Theory
Most drugs enhance or inhibit a
physiological process
Medications bind to receptors
Drug receptor binding is like lock and
key
Once occupied, receptor triggers
second messenger
Biochemical events occur
Drug stimulates or inhibits activity
Figure 5.5 Types of cellular receptors: (a) Drug binds to the receptor opening channel. (b) Drug binds to the
receptor, causing a G proteinmediated reaction in the cell. (c) Drug binds to the transmembrane receptor to
signal a change inside the cell. (d) Drug enters the cell nucleus to increase synthesis of specific proteins.
5.6 Agonists, partial agonists, and
antagonists compete for cellular
receptors and can modify drug action.
Agonists and Antagonists
Agonists
Mimic the action of endogenous
substances
Response may be greater than
endogenous activity
Opioid agonists
Partial agonists
Produce weaker action than endogenous
substances
Antagonists
Prevent action of endogenous
substances
May compete with agonists
Useful in blocking excess endogenous
activity
May reverse adverse effects of
overdoses
Most common is an opioid antagonist
Narcan (naloxone)
Figure 5.6 Agonists, partial agonists, and antagonists: (a) An agonist results in maximum response. (b) A
partial agonist results in less than maximum response. (c) An antagonist results in little or no response. (d) An
agonist plus antagonist results in diminished response.
5.7 In the future, pharmacogenetics
may allow customization of drug
therapy.
Pharmacogenetics
Pharmacogenetics
Drug therapy not effective for everyone
Human genome project
Genetic differences in drug-
metabolizing enzymes

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PHARMACOLOGY

CONNECTIONS TO NURSING PRACTICE

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