(4) Pharmacodynamics Flashcards
Affinity
Tendenc of a drug to bind receptor
Efficacy
Ability of a drug to initiate cellular effect
Agonist
Drug with both receptor affinity and efficacy
Partial Agonist
Drug with submaximal response that can act as an antagonist
Antagonist
Drug w/ receptor affinity but no efficacy
Potency
concentration of a drug required for a particular effect
Median effective dose (ED50)
Dose producing 50% maximal response
Median Lethal Dose (LD50)
Dose causing death in 50% subjects
Therapeutic index (TI)
LD50/ED50
Higher TI= safer drug
Graded dose-response curve
percent of maximum response vs. dose
Quantal dose-response curve
Percent of subjects with response vs. dose (All or none)
Tachyphylaxis
Acute tolerance
Pharmacodynamic tolerance
Down regulation of receptors
Pharmacokinetic tolerance
Upregulation of metabolic enzymes
Pharmacogenetics
Study of genetic basis for variation in drug response
Pharmacogenomic
Tools to assess multigenetic determinants of drug response
Ideosyncratic drug reaction
unable to predict & usually genetically based
Extensive metabolizer
Homozygous for WT CYP450
Intermediate metabolizer
Heterozygous for WT and variant CYP450
Poor metabolizer
Homozygous for variant
Ultrarapid metabolizer
multiple copies of WT