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, 4/24/26, 7:18 PM Pharmacology Exam 1 Flashcards | Quizlet
chemical specificity for receptors specificity between receptors and bonds, EX strict structural requirements for
binding
receptor saturability only a finite number of receptors that can be occupied
receptor affinity measure of attraction between drug and receptor
drug potency dose required to have certain effect, related to affinity of receptor
ED50 dose which produces 50% of maximum effect, used to compare drugs in terms of
potency
drug efficacy maximal effect achievable for a drug, related to number of receptor/complexes
formed, intrinsic activity of drug in activating receptor
full agonist affinity to, and full activator, of receptor (high intrinsic activity/efficacy), increases
activity above basal level of receptor where receptor has a constitutive (intrinsic
basal) level of activity in the absence of a ligand
inverse agonist affinity to, and full activator of receptor (high intrinsic activity/efficacy), but has
exact opposite effect of full agonist (metoprolol), decreases activity below basal
level of receptor where receptor has a constitutive (intrinsic basal) level of activity
in the absence of a ligand
partial agonist affinity to receptor but only partially activates a receptor, produces less than the
ceiling effect of a full agonist
pure antagonist affinity to receptor but produces no activation, dose curve is a straight line across
the bottom of an XY graph (EX oraverse vasodilates, overcoming the
vasocontriction of the LA)
neutral antgonist has no activity in the absence of an agonist or inverse agonist but can block
either's activity
competitive antagonist lacks efficacy, competes with agonists for binding sites, inhibitory effect can be
overcome by increasing concentration of competing agonist
every drug produces a variety of effects, we hope we
can get separation from things we want and adverse side
effects, this is different for every patient
know the second slide on page 10 of principles of drugs which drugs is most potent, least potenet, most efficient and least efficient
physiological antagonism stimulates competing/opposite physiological responses which counteract the
effects of a therapeutic drug, the inhibitory effect can NOT be overcome by
increasing the agonist dosage (EX epi is used during anaphylaxis to produce
physiological responses instead of an antihistamine which is only a competing
antagonist)
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