Theoretical
aspects of drug action: Introduction,
brief account on various forces involved in drug-receptor complex, types of
receptors. Theories of drug-receptor interactions: 1) occupancy theory, 2) rate
theory, 3) induced fit theory, 4) macro molecular perturbation theory, 5)
topographical and stereo chemical considerations, 6) Ion channel blockers. Case
history of drug development – cimetidine.
Design
and application of prodrugs: Prodrug
concept, choice and function of pro-moiety, bioreversible derivatives for
various functional groups, applications of the pro-drug approach.
Targets
for the development of following chemotherapeutic agents: antiulcer, analgesic, anti-inflammatory, antifungal,
antiangiogenesis and antihypertensive agents.
Biotransformation
of drugs: Enzymes responsible for
biotransformation, microsomal and non-microsomal mechanisms. Phase-I and
phase-II transformations with suitable examples. Factors influencing enzyme
induction and inhibition.
Genesis
of new drugs: Serendipity, random
screening, extraction of active principles from natural sources, molecular
modification of known drugs, selection or synthesis of soft and hard drugs, and
rational drug design.