Pharmacodynamics Flashcards
Pharmacodynamics
receptor binding, postreceptor effects, drug interactions
Drug receptors
protein macromolecules, sp. structure in macromolecule that with drugs forms a complex that triggers a biologic effect; located on cell mpembrane, some use sites acted on by endogenous molecules (chemical mediators, hormones), recognize chemical signals of agonists due to binding site, ionic groups
Types of receptors - from protein w/membrane channel
cholinergic receptors(nicotinic subtype), gamma-aminobutyric acid, takes milliseconds
Membrane receptors w/ enzymatic activity
bind agonist at extracellular and intracellular end, tyrosikinase activity, intracellular effects and phosphorylization of other enzymes, minutes to hours
Receptors w/ enzymatic activity examples
insulin receptors, erythropoietin receptors
Serpentine receptors examples
a&B receptors, cholinergic receptors (muscarinic subtype), dopamine receptors, angiotensin receptors, opioid receptors, acts in seconds to minutes
intracellular receptors
steroid receptors, act in hours
Drugs have
efficiency/intrinsic activity, potency(qty needed for 50%eff); depends on number of receptors and duration of binding
Receptors have
binding site, selectivity, affinity
Parameters characterizing pharmacodynamic activity
type of action, potency of action, latency, selectivity, efficiency
Agonists
total, partial
Antagonists
reversible, pseudo-irreversible, irreversible
Patient related factors
age, nutritional status, alcohol, diseases
Drug related factors
chemical structure, dose (24h, therapeutic, loading, maintaining, children), environmental