Test 4 Old Test Questions Flashcards

1
Q

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

A

partial agonist,

intrinsic activity between 0-1

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2
Q

term used to describe the response or effect of a drug can elicit is called

A

efficacy

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3
Q

the _______ the drug concentration needed to produce __________, the _______ the drug

A

the lower the drug concentration needed to produce a desired effect, the more potent the drug

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4
Q

T/F efficacy of agonist is partly dependent on the total number of target receptors on the tissue/organ of interest

A

True

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5
Q

which of the following will promote the greatest effect with the least amount of drug

A

high intrinsic activity, high receptor number, high affinity

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6
Q

T/F partial agonists, by definition, have low affinity

A

True

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7
Q

what type of drug would have 0 maximal effect as there is an increase of receptors bound by this drug

A

antagonist

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8
Q

Kd is to _____ as EC50 is to _____

A

Kd is to affinity as EC50 is to potency

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9
Q

as kd (inc/dec), affinity (inc/dec)

A

increases, decreases

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10
Q

an antagonist is administered to a patient that results in a dose ratio of 4. this means that

A

4 times the concentration of the agonist is now required to produce the same response compared to if the antagonist were absent

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11
Q

kd definition

A

ligand concentration which half of the target receptor population is occupied at equilibrium

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12
Q

fractional receptor occupancy is dependent on _____ of the drug

A

affinity and concentration

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13
Q

which curves have the highest efficacy when looking at a graph

A

the ones with the largest Emax

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14
Q

drug A has a kd of 0.1 microM, drug B has a kd of 30 microM. Why might this be?

A

drug A has a higher affinity for the receptor than drug B

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15
Q

as EC50 increases, Emax _____

A

remains the same

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16
Q

as kd increases, Bmax ______

A

remains the same

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17
Q

equation for finding kd

A

koff/kon

L * R / (LR)

18
Q

EC50 is defined as

A

the ligand concentration at which half of the maximum reaction response is achieved

19
Q

if compound A and compound B have the same Emax and Compound B is more potent than compound A what must be true

A

Compound B has a lower EC50 than compound A

20
Q

the ED50 for a receptor agonist is 40mg. this means that

A

40mg is needed to effectively treat half of the study population

21
Q

T/F partial agonists have a low affinity

A

false

22
Q

what is the primary purpose of a drug-receptor binding curve

A

to describe receptor binding as a function of drug concentration

23
Q

a graded dose response tells us about the _____ and ______ of a drug while a quantal dose response curve tells us about _______

A

a graded dose response tells us about the efficacy and potency of a drug while a quantal dose response curve tells us about safety

24
Q

intrinsic activity is:

A

the relative ability of a ligand-receptor complex to produce a biological response

25
Q

T/F when dosed at high enough concentration a partial agonist can exhibit the same maximal efficacy as a full agonist

A

False

26
Q

more potent drugs have ____ kd and ____ affinity

A

more potent drugs have lower kd and higher affinity

27
Q

the presence of a competitive agonist along with a full agonist has what effect

A

reduces the potency but not the efficacy of the agonist

28
Q

the clinical effectiveness of a drug depends on the drug’s

A

maximal efficacy

29
Q

T/F drug potency is related to the drugs affinity for a receptor while efficacy is related to the proportion of receptors activated

A

True

30
Q

T/F the efficacy of an antagonist is decreased in the presence of a noncompetitive antagonist

A

True

31
Q

T/F a partial agonist can reach 100% max effect of a full agonist only at 100% receptor occupancy

A

False

32
Q

T/F the difference between two different drugs can be obtained from a quantal response curve

A

False

33
Q

what best describes a quantal dose response curve

A

population of subjects increasing doses of drug to determine the dose needed to produce a desired effect

34
Q

down-regulation is:

A

usually prolonged agonist exposure, likely lead to a decrease in maximal attainable response, will require a greater dose of agonist in order to achieve the same response prior to down regulation

35
Q

the graph will shift right when drug A is a full agonist and drug B is added that is _____

A
  1. a partial agonist for the receptor
  2. an antagonist for the drug for the receptor
  3. a full agonist for the receptor
36
Q

T/F drug x and drug y have the same affinities for the receptor so they will have the same effect

A

False

37
Q

T/F drug x and drug y both require the same dose for a specific response, therefore they have equivalent potencies for this response

A

True

38
Q

T/F drug X has a lower EC50 than Drug y, therefore Drug Y has a greater efficacy than Drug X

A

False

39
Q

the graph will shift right when drug A is a full agonist and drug B that is added is____

A

enhances the ability of the initial drug to activate the receptor

40
Q

T/F a partial agonist can be more potent than a full agonist in producing a specific response

A

True

41
Q

If compound A and compound B have the same Emax, compound B is more potent than compound B, which must be true?

A

compound B must have a lower EC50 than compound A

42
Q

what is true if two drugs have equal affinities for the same target receptor

A

both drugs will occupy the same percentage of receptors at identical concentration