Test 4 Old Test Questions Flashcards
in areas where dopamine are low drug increases dopamine by activating the receptors. where dopamine levels are high, it causes a dose-dependent, reversible decrease in dopaminergic activity by blocking the receptors. this drug is best characterized by
partial agonist,
intrinsic activity between 0-1
term used to describe the response or effect of a drug can elicit is called
efficacy
the _______ the drug concentration needed to produce __________, the _______ the drug
the lower the drug concentration needed to produce a desired effect, the more potent the drug
T/F efficacy of agonist is partly dependent on the total number of target receptors on the tissue/organ of interest
True
which of the following will promote the greatest effect with the least amount of drug
high intrinsic activity, high receptor number, high affinity
T/F partial agonists, by definition, have low affinity
True
what type of drug would have 0 maximal effect as there is an increase of receptors bound by this drug
antagonist
Kd is to _____ as EC50 is to _____
Kd is to affinity as EC50 is to potency
as kd (inc/dec), affinity (inc/dec)
increases, decreases
an antagonist is administered to a patient that results in a dose ratio of 4. this means that
4 times the concentration of the agonist is now required to produce the same response compared to if the antagonist were absent
kd definition
ligand concentration which half of the target receptor population is occupied at equilibrium
fractional receptor occupancy is dependent on _____ of the drug
affinity and concentration
which curves have the highest efficacy when looking at a graph
the ones with the largest Emax
drug A has a kd of 0.1 microM, drug B has a kd of 30 microM. Why might this be?
drug A has a higher affinity for the receptor than drug B
as EC50 increases, Emax _____
remains the same
as kd increases, Bmax ______
remains the same
equation for finding kd
koff/kon
L * R / (LR)
EC50 is defined as
the ligand concentration at which half of the maximum reaction response is achieved
if compound A and compound B have the same Emax and Compound B is more potent than compound A what must be true
Compound B has a lower EC50 than compound A
the ED50 for a receptor agonist is 40mg. this means that
40mg is needed to effectively treat half of the study population
T/F partial agonists have a low affinity
false
what is the primary purpose of a drug-receptor binding curve
to describe receptor binding as a function of drug concentration
a graded dose response tells us about the _____ and ______ of a drug while a quantal dose response curve tells us about _______
a graded dose response tells us about the efficacy and potency of a drug while a quantal dose response curve tells us about safety
intrinsic activity is:
the relative ability of a ligand-receptor complex to produce a biological response