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MODULE 5: PHARMACODYNAMICS

LEARNING OUTCOMES:

After reading this module (5), the student should be able to:
1. Explain the applications of pharmacodynamics to nursing practice.
2 Discuss how a drug’s therapeutic index is related to its margin of safety.
3. Explain the significance of the graded dose–response relationship to nursing practice.
4. Compare and contrast the terms potency and efficacy.
5. Distinguish among an agonist, a partial agonist, and an antagonist.
6. Explain the relationship between receptors and drug action.
7. Explain possible future developments in the field of pharmacogenetics

1. Pharmacodynamics and Interpatient Variability

 The term pharmacodynamics comes from the root words pharmaco, which means
“medicine,” and dynamics, which means “change.”

 In simplest terms, pharmacodynamics refers to how a medicine changes the body.

 A more complete definition explains pharmacodynamics as the branch of pharmacology

concerned with the mechanisms of drug action and the relationships between drug
concentration and responses in the body.

 Pharmacodynamics has important nursing applications: Knowledge of therapeutic

indexes, dose–response relationships, and drug–receptor interactions will help nurses
provide safe and effective treatment.

2. Therapeutic Index and Drug Safety

 The therapeutic index is a measure of a drug’s safety margin: The higher the value, the
safer the medication.

 The therapeutic index offers the nurse practical information on the safety of a drug and a
means to compare one drug with another.

3. The Graded dose- Response Relationship and Therapeutic Response

 Increasing the drug dose produces no additional therapeutic response. This may occur
for a number of reasons. One explanation is that all the receptors for the drug are
occupied.

 Although increasing the dose does not result in more therapeutic effect, nurses should
be mindful that increasing the dose may produce toxic effects.

Pharmacodynamics Celia Cruz-Fajardo, M.D.

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4. Potency and Efficacy

 There are two fundamental ways to compare medications within therapeutic and
pharmacologic classes.
› First is the concept of potency.
. A drug that is more potent will produce a therapeutic effect at a lower
dose, compared with another drug in the same class
. Potency is one way to compare the doses of two independently
administered drugs in terms of how much is needed to produce a
particular response.
› The second method used to compare drugs is called efficacy, which is the
magnitude of maximal response that can be produced from a particular drug.

 From a pharmacotherapeutic perspective, efficacy is almost always more important than

potency.

 As another comparison, the patient with cancer is much more concerned about how
many cancer cells have been killed (efficacy) than what dose the nurse administered
(potency).

5. Cellular Receptors and Drug Actions

 Drugs act by modulating or changing existing physiological and biochemical processes.
To exert such changes requires that drugs interact with specific molecules and
chemicals normally found in the body.

 A cellular macromolecule to which a medication binds in order to initiate its effects is

called a receptor.

 The concept that a drug binds to a receptor to cause a change in body chemistry or
physiology is a fundamental theory in pharmacology.

 Receptor theory explains the mechanisms by which most drugs produce their effects. It
is important to understand, however, that these receptors do not exist in the body solely
to bind drugs. Their normal function is to bind endogenous molecules such as
hormones, neurotransmitters, and growth factors.

 Although a drug receptor can be any type of macromolecule, the vast majority are
proteins.

6. Types of Drug-Receptor Interactions

 A drug that produces the same type of response as the endogenous substance is called
an agonist.
› Agonists sometimes produce a greater maximal response than the
endogenous chemical.
. The term partial agonist or agonist-antagonist drug describes a
medication that produces a weaker, or less efficacious, response than
an agonist.

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 A second possibility is that a drug will occupy a receptor and prevent the endogenous
chemical from acting.
› This drug is called an antagonist.
. Antagonists often compete with agonists for the receptor binding sites.

 Not all antagonism is associated with receptors.

› Functional antagonists inhibit the effects of an agonist not by competing for a
receptor but by changing pharmacokinetic factors

 The relationships that occur between agonists and antagonists explain many of the
drug–drug and drug–food interactions that occur in the body

7. Pharmacology of the Future: Customizing Drug Therapy

 In the past, unpredictable and unexplained drug reactions had been labeled as
idiosyncratic responses. It is hoped that performing a DNA test before administering a
drug may someday address idiosyncratic differences.

 Pharmacogenetics is the area of pharmacology that examines the role of heredity in

drug response. The greatest advances in pharmacogenetics have been the identification
of the human genome and subtle genetic differences in drug-metabolizing enzymes
among patients.

 Pharmacogenomics deals with the influence of genetic variation on drug response in

patients by correlating gene expression or actual variants of the human genome

SUMMARY:
1. Pharmacodynamics is the area of pharmacology concerned with how drugs produce change
in patients and the differences in patient responses to medications.
2. The therapeutic index, expressed mathematically as TD50 ÷ ED50, is a value representing
the margin of safety of a drug. The higher the therapeutic index, the safer is the drug.
3. The graded dose–response relationship describes how the therapeutic response to a drug
changes as the medication dose is increased.
4. Potency, the dose of medication required to produce a particular response, and efficacy, the
magnitude of maximal response to a drug, are means of comparing medications.
5. Drug–receptor theory is used to explain the mechanism of action of many medications.
6. Agonists, partial agonists, and antagonists are substances that compete with drugs for
receptor binding and can cause drug–drug and drug–food interactions.
7. In the future, pharmacotherapy will likely be customized to match the genetic makeup of
each patient.

Reference: Pharmacology for Nurses: A pathophysiologic Approach by Adams, Holland and Urban (pp.
69 – 75).

Pharmacodynamics Celia Cruz-Fajardo, M.D.