PHARMACODYNAMICS

PHARMACODYNAMICS
 What drugs do to the body
 Biological activity of the drug

Concerned with:

Principles of Drug action

Mode of Drug action
Targets of Drug action
Mechanisms of Drug action
 PRINCIPLES OF DRUG ACTION
 Stimulation
Increase the physiological activity
Adrenaline- Heart, Glycogenolysis
 Depression

Depress CNS-Anaesthetics
 Replacement

Endogenous/Exogenous Substances
(Insulin/Vitamin)
 Chemotherapy

Target of invading Microorganisms without affecting host

cell.(Cancer Chemotherapy)
 MODE OF DRUG ACTION
 Physical action
Adsorption, osmotic activity
 Chemical reaction

 Action through enzymes

Induction
Inhibition
 Action through Ion channels

 Action through Receptors

 Action by Replacement

 Chemotherapy
 TARGETS OF DRUG ACTION
 Receptors
 Ion channels

 Enzymes

 Carrier Molecules
 RECEPTORS
 Receptors and Receptor binding (Specificity and affinity)
 Signaling mechanism(Transducer Mechanism)

G Protein coupled Receptors

Tyrosine Kinase Linked Receptors
Second messengers(Cyclic AMP)
 Response of Drug-Receptor Interaction

Affinity
Drug occupancy
Various Response:
Agonist (Affinity-Intrinsic Activity)
Antagonist (Affinity-No Intrinsic Activity)
Partial Antagonist (Affinity-Low Intrinsic Activity)
Inverse Agonist (Affinity-Opposite Intrinsic Activity)
 RECEPTORS

 Quantitative aspects of drug action

Dose-response relationship of Agonists
1. Graded Response (Blood Pressure)
2. Quantal Response (Log Conc.,/Dose response)
Curve- Sigmoidal (25-75% Response- Linear at middle)
LC50, ED50, ED0
Flatter – Large increase in conc.,-Slight change in response
Steepness- small increase in conc.,-Marked change
Biological Activity-
 RECEPTORS
 Dose-response relationship of Antagonists
 Competitive Antagonist
 Irreversible Antagonist
 Non competitive Antagonist
 Physiological Antagonist (pharmacological action-opposite)

 Partial Agonists
Low Efficacy
 Receptor Occupancy and Response

Agonist 1% Occupancy- Maximal Response

Antagonist 100% Occupancy-No Response
 RECEPTORS
 Potency and Efficacy
Ability to produce response – Potency
(Low ED50- High Potency)
Quantification (How much/How fast) of response-
Efficacy
 COMBINED USE OF DRUG
 Synergism
Additive
Potentiation (One drug increases other)
 MECHANISM OF DRUG ACTION
 On cell membrane
 On intracellular constituents

 Outside the cell

 Antimicrobial action