Pharmacology Exam 2nd Edition
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ED50 - ANSWER dose which produces 50% of maximum effect, used to compare
drugs in terms of potency
drug efficacy - ANSWER maximal effect achievable for a drug, related to number of
receptor/complexes formed, intrinsic activity of drug in activating receptor
full agonist - ANSWER 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 - ANSWER 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 - ANSWER affinity to receptor but only partially activates a receptor,
produces less than the ceiling effect of a full agonist
pure antagonist - ANSWER 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 - ANSWER has no activity in the absence of an agonist or inverse
agonist but can block either's activity
competitive antagonist - ANSWER 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 - ANSWER
pharmacokinetics - ANSWER relationship between drug dosage and concentration in
plasma over time, determines onset, duration, and intensity of drug
pharmacodynamics - ANSWER relationship between drug concentration over time and
therapeutic response
chemical specificity for receptors - ANSWER specificity between receptors and bonds,
EX strict structural requirements for binding
receptor saturability - ANSWER only a finite number of receptors that can be occupied
receptor affinity - ANSWER measure of attraction between drug and receptor
drug potency - ANSWER dose required to have certain effect, related to affinity of
receptor
know the second slide on page 10 of principles of drugs - ANSWER which drugs is
most potent, least potenet, most efficient and least efficient
physiological antagonism - ANSWER 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 - ANSWER
therapeutic index - ANSWER 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 - ANSWER the therapeutic index of 10 is safer, there is a larger
range of dosages we can give without toxicity
therapeutic window - ANSWER 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 - ANSWER drug will be ineffective due to cigarette
smoke impeding the metabolism of theophylline, need 4x the normal dose
first pass metabolism - ANSWER 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 - ANSWER topical cream or ointments, nasal spray,
inhaler
parenteral route of drug delivery - ANSWER administration bypassing the GI tract
examples of parenteral administration - ANSWER IV, IM, transdermal (patches)
IV administration - ANSWER 100% bioavailability (not subject to absorption or 1st pass
metabolism), titratable (can give more or less depending on situation)
IM administration - ANSWER 100% bioavailability but slower onset than IV, useful for
long acting drug delivery due to "depot" injection
transdermal administration - ANSWER convenient and slow absorption at a constant
rate
non-titratable routes - ANSWER oral-slow, subject to absorption
sublingual-more rapid, mostly avoids 1st pass and variable absorption, but not easily
titratable
titratable routes - ANSWER inhalational (N2O2), IV, rapid onset and offset
bioavailability - ANSWER compares amount of drug that reaches the blood by non IV
routes vs amount of drug that reaches blood by IV (IV (bottom number) is always 100)
(conc. of nonIV/conc. of IV)
bioavailability formula question will be on exam
factors affecting absorption - ANSWER properties of drug (smaller size faster
absorption, vehicle, solubility/ionization), envt properties (pH, organ surface area, food
presence)
example of pH and its affect on absorption - ANSWER PenG - susceptible to stomach
acid
Save
ED50 - ANSWER dose which produces 50% of maximum effect, used to compare
drugs in terms of potency
drug efficacy - ANSWER maximal effect achievable for a drug, related to number of
receptor/complexes formed, intrinsic activity of drug in activating receptor
full agonist - ANSWER 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 - ANSWER 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 - ANSWER affinity to receptor but only partially activates a receptor,
produces less than the ceiling effect of a full agonist
pure antagonist - ANSWER 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 - ANSWER has no activity in the absence of an agonist or inverse
agonist but can block either's activity
competitive antagonist - ANSWER 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 - ANSWER
pharmacokinetics - ANSWER relationship between drug dosage and concentration in
plasma over time, determines onset, duration, and intensity of drug
pharmacodynamics - ANSWER relationship between drug concentration over time and
therapeutic response
chemical specificity for receptors - ANSWER specificity between receptors and bonds,
EX strict structural requirements for binding
receptor saturability - ANSWER only a finite number of receptors that can be occupied
receptor affinity - ANSWER measure of attraction between drug and receptor
drug potency - ANSWER dose required to have certain effect, related to affinity of
receptor
know the second slide on page 10 of principles of drugs - ANSWER which drugs is
most potent, least potenet, most efficient and least efficient
physiological antagonism - ANSWER 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 - ANSWER
therapeutic index - ANSWER 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 - ANSWER the therapeutic index of 10 is safer, there is a larger
range of dosages we can give without toxicity
therapeutic window - ANSWER 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 - ANSWER drug will be ineffective due to cigarette
smoke impeding the metabolism of theophylline, need 4x the normal dose
first pass metabolism - ANSWER 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 - ANSWER topical cream or ointments, nasal spray,
inhaler
parenteral route of drug delivery - ANSWER administration bypassing the GI tract
examples of parenteral administration - ANSWER IV, IM, transdermal (patches)
IV administration - ANSWER 100% bioavailability (not subject to absorption or 1st pass
metabolism), titratable (can give more or less depending on situation)
IM administration - ANSWER 100% bioavailability but slower onset than IV, useful for
long acting drug delivery due to "depot" injection
transdermal administration - ANSWER convenient and slow absorption at a constant
rate
non-titratable routes - ANSWER oral-slow, subject to absorption
sublingual-more rapid, mostly avoids 1st pass and variable absorption, but not easily
titratable
titratable routes - ANSWER inhalational (N2O2), IV, rapid onset and offset
bioavailability - ANSWER compares amount of drug that reaches the blood by non IV
routes vs amount of drug that reaches blood by IV (IV (bottom number) is always 100)
(conc. of nonIV/conc. of IV)
bioavailability formula question will be on exam
factors affecting absorption - ANSWER properties of drug (smaller size faster
absorption, vehicle, solubility/ionization), envt properties (pH, organ surface area, food
presence)
example of pH and its affect on absorption - ANSWER PenG - susceptible to stomach
acid
