Pharmacology Exam 1 with correct
answers provided
pharmacokinetics ✅✅relationship between drug dosage and concentration in plasma
over time, determines onset, duration, and intensity of drug
pharmacodynamics ✅✅relationship between drug concentration over time and
therapeutic response
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)
exam will ask you to explain interactions between drugs in reference to physiological
antagonism that were explained in lectures ✅✅
therapeutic index ✅✅the difference between a dose that produces a therapeutic
effect and a dose that produces a lethal toxicity, this has to do with a population
which drug is a safer drug? a drug with a
therapeutic index of 2
or
therapeutic index of 10 ✅✅the therapeutic index of 10 is safer, there is a larger range
of dosages we can give without toxicity
therapeutic window ✅✅difference between ineffective and effective dose range,
drugs like penicillin has a large window where others have a small one (more
dangerous), some DDIs happen to decrease or increase metabolism/reception of the
drug and therefore increase or decrease plasma conc. causing toxicity or
ineffectiveness depending on the type of DDI
theophylline and cigarette smoker ✅✅drug will be ineffective due to cigarette smoke
impeding the metabolism of theophylline, need 4x the normal dose
first pass metabolism ✅✅drug is absorbed into blood stream and goes to the liver first
before it can get into systemic circulation, very important, could lose a lot of the drug
before it is able to reach target, need to compensate by giving more or give the
medication another way (EX sublingual, but most drugs are not absorbed this way,
rectal, or localized)
localized route of administration ✅✅topical cream or ointments, nasal spray, inhaler
parenteral route of drug delivery ✅✅administration bypassing the GI tract
answers provided
pharmacokinetics ✅✅relationship between drug dosage and concentration in plasma
over time, determines onset, duration, and intensity of drug
pharmacodynamics ✅✅relationship between drug concentration over time and
therapeutic response
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)
exam will ask you to explain interactions between drugs in reference to physiological
antagonism that were explained in lectures ✅✅
therapeutic index ✅✅the difference between a dose that produces a therapeutic
effect and a dose that produces a lethal toxicity, this has to do with a population
which drug is a safer drug? a drug with a
therapeutic index of 2
or
therapeutic index of 10 ✅✅the therapeutic index of 10 is safer, there is a larger range
of dosages we can give without toxicity
therapeutic window ✅✅difference between ineffective and effective dose range,
drugs like penicillin has a large window where others have a small one (more
dangerous), some DDIs happen to decrease or increase metabolism/reception of the
drug and therefore increase or decrease plasma conc. causing toxicity or
ineffectiveness depending on the type of DDI
theophylline and cigarette smoker ✅✅drug will be ineffective due to cigarette smoke
impeding the metabolism of theophylline, need 4x the normal dose
first pass metabolism ✅✅drug is absorbed into blood stream and goes to the liver first
before it can get into systemic circulation, very important, could lose a lot of the drug
before it is able to reach target, need to compensate by giving more or give the
medication another way (EX sublingual, but most drugs are not absorbed this way,
rectal, or localized)
localized route of administration ✅✅topical cream or ointments, nasal spray, inhaler
parenteral route of drug delivery ✅✅administration bypassing the GI tract
