Pharmacodynamics
1 year MBBS
st
By Prof Dr Maryam Rashid
MBBS, MPhil, PhD (Pharmacology)
CMT, CME
(Certification in Medical Teaching and Editing)
Learning Objectives (LOs)
• Define Pharmacodynamics
• Define affinity & efficacy
• Define receptor, agonist, antagonist, partial agonist,
inverse agonist in terms of AFFINITY & EFFICACY
• One problem solving
Pharmacodynamics
WHAT THE DRUG DOES TO THE BODY
Physiological and biochemical effects of drugs and
their mechanism of action at organ/
subcellular/macromolecular level
How do drugs know where to
go?
Drugs circulate throughout body in blood/plasma
↓
Encounter receptors for which they have affinity
↓
Bind
⇓
• Pharmacological response
Principles of drug action
1.Stimulation: ↑ activity
e.g. adrenaline →stimulates heart
2.Depression: ↓activity
e.g. barbiturates → ↓CNS
3.Irritation: non-selective, noxious effect
applied to less specialized cells (epithelium,
connective tissue)
e.g. bisacodyl (dulcolax) →irritates colonic
epithelium →relieves constipation
5
4.Replacement: Natural metabolites,
hormones or their congeners in deficient
states.
e.g. Insulin in Diabetes
5.Cytotoxic actions: Selective for invading
parasites or cancer cells
e.g. chloroquine →Malaria
6
Mechanism of drug action
• Receptor mediated
• Non-receptor mediated
7
Macromolecular nature of drug
receptors
• Regulatory proteins
• Enzymes
• Transport proteins
• Structural proteins
Receptor
Macromolecule or binding site
Located on surface or inside effector cell
Serves to recognize signal molecule/drug
and initiate the response
It itself has no other function
Types of receptors
Affinity: Ability to bind with receptor
Intrinsic activity (Efficacy): Capacity to induce
functional/conformational change in receptor
e.g. Adrenaline, Histamine, Morphine
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Affinity: Ability to bind with receptor
Intrinsic activity (Efficacy): Capacity to
induce functional/conformational change in
receptor
e.g. Adrenaline, Histamine, Morphine
Agonist
An agent which activates a receptor to produce an
effect similar to that of physiological signal molecule.
It has both Affinity & Intrinsic activity
Partial agonist
Agent which activates a receptor to produce
SUBMAXIMAL effect i.e. response < 100%
It has both Affinity & Intrinsic activity (less than 1)
e.g. Buprenorphine→ Partial µ-agonist
Pindolol Beta blocker
Antagonist
A drug is said to be an antagonist when it binds to a
receptor and prevents (blocks or inhibits) a natural
compound or a drug to have an effect on the
receptor. An antagonist has NO activity.
Its intrinsic activity is = 0
Inverse agonist
An agent which activates a receptor to produce effects
OPPOSITE to that of agonist
It has Affinity .
Its intrinsic activity is = -1
e.g. β- Carboline →at Benzodiazepine site
Diazepam (BZD) is anxiolytic
β- Carboline is anxiogenic
ANTAGONIST
• Antagonist:
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A 55-year-old man is seen in the clinic with
hypertension of 150/95 mm Hg (millimeters of
mercury). His personal medical history and physical
examination are otherwise unremarkable but his
family history is positive for early deaths due to
cardiovascular disease. A decision is made to treat his
hypertension, starting with a calcium channel blocker.
Blocker A in a dose of 5 mg produces the same
decrease in blood pressure as 500 mg of blocker B.
Which of the following predictions is most accurate?
• Potency (min dose producing maximal response)
5 mg
500 mg
• Efficacy (maximal response of a drug)
decrease in BP
a) Blocker A will be more efficacious than blocker B
b) Blocker A will be about 100 times more potent
than blocker B
c) Toxicity of blocker A will be less than that of
blocker B
d) Blocker A will have a wider therapeutic window
than blocker B
e) Blocker A will have a longer half-life than blocker
B
b) Blocker A will be about 100 times more potent
than blocker B
Quick Recap
• Pharmacodynamics
• Agonist , antagonist, partial agonist, inverse agonist
• Receptor; definition, structure, types
