5 Pharmacology Lecture, Targets For Drug Action

Faculty of
Medicine
Medical Education-
Damietta
University
Level 1
Semester 1
Module 2A
Fundamental Principles of
Pharmacology (PD1)
Targets for drug actions
Mohamad-Hesham Daba
• Contact: Pharmacology Department.
• Official email: [email protected]
• Mobile: 01119950988
• Academic hours:
➢ Sunday: 10:00-12:00 AM
➢ Tuseday: 10:00-12:00 AM
Lecture Outline
• Drug receptors interaction

• Dose response relationship curves and their importance
Learning Outcomes
By the end of the lecture, the students will be able to:
1. Define the Pharmacodynamics versus pharmacokinetics
2. Define Drug receptors versus ligands
3. Define Potency versus efficacy
4. Identify quantal versus graded dose response curve
Case scenario, Clinical Correlate, Practice points
• A 23-year-old male college graduate
student with a history of asthma presents to
the ambulatory care clinic for follow-up.
• He uses a B2-agonist via inhaler when he
has an attack.
• Give a comment
Drug-body interactions
PHARMACODYNAMICS
• Mechanisms of drug
action (main targets for
drug action):
• Receptors
• Ion channels
• Enzymes
Receptors
• Receptors are protein macromolecules

• on the surface or within the cell
• that combine chemically with small molecules (ligands)
and
• produces physiological regulatory functions.
Chemistry of drug receptor binding
• The ionic bonds
• The hydrogen bonds
• The covalent bonds

Biological responses to drug receptor binding
A. Agonist effect:
the drug has both affinity and …………….efficacy
Affinity versus Efficacy
➢Affinity:
• It determines the number of receptors occupied by
the drug.
➢Efficacy
• It is the ability of a drug to produce response (effect)
after binding to the receptor.
B. Antagonist effect:
the drug has affinity but ………………………..no efficacy
C. Partial agonist:
is that agonist gives submaximal response
even at full concentration i.e. never gives Emax
Dose-response relationship studies: Agonist effect
• Graded response • Quantal response

• The response is increased • The response is all-or-none
proportionally to the dose of the response e.g. prevention of
agonist e.g. the response of the convulsions by antiepileptic
heart to adrenaline. drugs
Dose response relationship curves and their importance
1. Determine potency
o ED50 is the dose of the drug that gives 50% of the Emax, or
it is the dose that gives the desired effect in 50% of a test population of subjects.
o A drug that gives ED50 by smaller doses is described as “potent”.
2. Determine efficacy
o Is the maximal response that a drug can elicit at full concentration
Case Discussion/reflection
• A 23-year-old male college graduate
student with a history of asthma presents to
the ambulatory care clinic for follow-up.
• He uses a B2-agonist via inhaler when he
has an attack.
• Give a comment
Q1. Which branch of pharmacology studies the way drugs work
in living organism?
A. Pharmacotherapeutics
B. Pharmacokinitics
C. Pharmacogenitics
D. Pharmacodynamics
E. Pharmacoeconomics
Q2. Which of the following provides information about
the largest response a drug can produces, regardless of
dose?
A. Drug potency.
B. Maximal efficacy.
C. Mechanism of receptor action.
D. Therapeutic index.
E. Therapeutic window.
Q3. Dose response data was
collected during the preclinical
testing of four drugs for the
treatment of acute heart
failure.
Which drug studied was the
most?
➢Efficacious…………
➢Potent……………….
Q4. In the absence of other drug, pindolol causes an increase in
heart rate by activating beta adrenoceptors. In the presence of
highly effective beta stimulants, however, pindolol causes a dose-
dependent, reversible decrease in heart rate. Therefore pindolol
is probably:
A. An irreversible antagonist.
B. A physiologic antagonist.
C. A chemical antagonist.
D. A partial agonist.
E. A Spare receptor agonist.
Q5. A 55-year-old woman with congestive heart failure is to be
treated with a diuretic drug. Drugs X and Y have the same
mechanism of diuretic action. Drug X in a dose of 5mg produces
the same magnitude of diuresis as 500 mg of drug Y. This
suggests that:
A. Drug Y is less efficacious than drug X.
B. Drug X is about 100 times more potent than drug Y.
C. Toxicity of drug X is less than that of drug Y.
D. Drug X is a safer drug than drug Y.
E. Drug X will have a shorter duration of action than drug Y because less of
drug X is present for a given effect
Summary and wrap up
1.Pharmacokinetics versus pharmacodynamics
2.Affinity versus efficacy
3.Agonist versus antagonist
4.Potency versus efficacy
5.Agonist versus partial agonist
Discussion & Feedback
• A 22-year-old man with seasonal allergic rhinitis takes an antihistamine

for relief of symptoms. It is successful for him over 90% of the time.
• Give the idea behind
References or further readings
1) Kaplan USMLE STEP1, lecture notes

Pharmacology latest edition.
2) Lippincott’s illustrated review:

Pharmacology, latest edition

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Faculty of

• Drug receptors interaction

• Receptors are protein macromolecules

• The ionic bonds

• The hydrogen bonds

• The covalent bonds

• Graded response • Quantal response

• A 22-year-old man with seasonal allergic rhinitis takes an antihistamine

1) Kaplan USMLE STEP1, lecture notes

2) Lippincott’s illustrated review:

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