01 Principles Flashcards
Affinity definition
potential for drug-receptor binding
Receptor definition
cellular binding site with a biological effect
Intrinsic activity definition
capacity to produce a beneficial biological effect
Agonist definition
substances that STIMULATE a receptor to produce a physiologic reaction (has intrinsic activity)
Antagonist definition
substances that INTERFERE with activity of a receptor and its endogenous substrate; does not produce a physiologic reaction itself (does not have intrinsic activity)
Allostery definition
bound ligand changes configuration of the molecule to influence specificity at a second site
Efficacy definition
[affinity] x [intrinsic activity]
Efficacy v. Potency
efficacy is dose independent; potency is dose dependent
What is the efficacy of an antagonist?
zero (because there is no intrinsic activity)
EC50 definition
effective concentration in 50% of subjects
ED50 definition
effective dose in 50% of subjects
IC50 definition
inhibitory concentration in 50% of subjects (antagonists)
Hypersensitivity definition
result of chronic antagonism
Maximum Dose definition
the MINIMUM amount of drug to produce the MAX therapeutic effect
Partial Agonist definition
LOW intrinsic activity with a therapeutic potency and affinity
Pharmacodynamics definition
how the drugs affect the body (MOA)
Pharmacokinetics definition
how the body affects the drug (ADME)
ADME definition
absorption, distribution, metabolism, elimination
Pharmacotherapeutics definition
how the drug affects disease processes
Concentration v. Dose
concentration is laboratory; dose is clinical
How is Pharmacodynamics measured?
potency, efficacy, affinity, toxicity
How is Potency related to EC50 and IC50?
potency is INVERSELY related to EC50 for agonists and IC50 for antagonists
Posology definition
science of drug dosing
Potency definition
biological response to a given dose