Part 3: Pharmacodynamics
What the Drug Does to the Body
Pharmacodynamics (PD) describes the relationship between drug concentration and pharmacological effect. It encompasses drug-receptor interactions, signal transduction, and the dose-response relationship that determines therapeutic outcomes.
$$E = \frac{E_{max} \cdot [D]}{EC_{50} + [D]}$$
Emax model: Effect as a function of drug concentration
Topics in This Part
3.1 Drug-Receptor Interactions
Binding kinetics, affinity, selectivity, specificity
3.2 Dose-Response Relationships
Graded vs quantal, potency, efficacy, therapeutic index
3.3 Agonists & Antagonists
Full/partial agonists, competitive/noncompetitive antagonists, inverse agonists
3.4 Receptor Theory
Occupancy theory, two-state model, spare receptors, constitutive activity
3.5 Signal Transduction
Second messengers, kinase cascades, amplification, crosstalk
3.6 Tolerance & Desensitization
Receptor downregulation, tachyphylaxis, dependence, withdrawal
Agonist Types
Full Agonist
Produces maximal response (efficacy = 1)
Partial Agonist
Submaximal response even at full occupancy
Inverse Agonist
Reduces constitutive receptor activity
Neutral Antagonist
Blocks receptor without affecting basal activity