pharm exam 1 Flashcards
EC50
conc. of drug to get 50% of max response
Kd
conc. of free drug when 50% is bound to receptors
low Kd
high binding, slow dissociation
high Kd
low binding, fast dissociation
rightward shift on dose/response curve
lower affinity for same receptor, same maximal response
lower magnitude on dose/response curve
lower efficacy, lower maximal response
affinity
desire to bind
potency
amount to produce a response. lower EC50 lower potency.
efficacy
maximum possible response, also called intrinsic activity
intrinsic activity
also called efficacy, maximum response possible
quantal dose response
determines therapeutic ratio, all or none, ED50 and LD50
graded dose response curve
determines potency, maximal efficacy etc.
ED50
dose producing desired effect in 50% of population
LD50
dose produces lethal effect in 50% of population
TD50
dose that is toxic to 50% of population
calculate therapeutic index for humans
TD50/ED50
calculate margin of safety for humans
TD1/ED99
higher margin of safety correlates to:
safer drug
allosteric activator
binds to a different site than and increases response to agonist
competitive antagonist
binds to same site as agonist, decrease Kd or EC50
noncompetitive antagonist
bind to different site from agonist, decrease Emax
physiological antagonist
works through completely different mechanism
chemical antagonism
inactivates drug by chemically neutralizing, like antacids
partial agonist
less maximal response than agonist, lower efficacy
ligand regulated transmembrane enzyme examples (tyrosine kinases)
insulin, epidermal growth factor, nerve growth facter
cytokine receptor examples (utilize JAKs and STATs)
growth hormone, erythropoietin, interferons
ligand gated, voltage gated channel examples
nicotinic/Ach, GABA, benzodiazepines, barbiturates
Gs coupled receptors examples
beta 1 & 2 drugs, epinephrine, norepi (beta), dopamine, histamine
Gi coupled receptor examples
alpha 2 drugs, norepi (alpha), morphine
Gq/IP3/DAG coupled receptor examples
alpha 1 drugs
pharmacokinetic tolerance
drug induces enzymes for its own metabolism, warfarin with phenytoin
pharmacodynamic tolerance/cellular tolerance
change in receptor number or function
physiologic tolerance
two drugs with oppposing effects administered together (norepi, histamine)