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Pharmacology 1 > Pharmacodynamic Principles > Flashcards

Pharmacodynamic Principles Flashcards

1
Q

what type of drug posses affinity and intrinsic efficacy

A

agonist

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2
Q

what class of agonist binds to the same site as endogenous ligands

A

primary agonist

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3
Q

what class of agonist binds to a different region of the receptor

A

allosteric agonist

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4
Q

what is an example of an allosteric agonist

A

anaesthetic drug effects on GABA receptors

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5
Q

what type of agonist produces maximal efficacy

A

full agonist

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6
Q

what type of agonist can bind to and activate the receptor but produces a sub-maximal effect

A

partial agonist

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7
Q

what opioid receptor acts a full agonist

A

morphine

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8
Q

what opioid receptor is a partial agonist

A

buprenorphine

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9
Q

what type of drug possess affinity but lacks intrinsic efficacy

A

antagonist

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10
Q

what is the function of antagonistic drugs

A

prevent the action of natural agonists (neurotransmitters & hormones)

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11
Q

what is an example of a drug that can act as an agonist and antagonist

A

butorphanol

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12
Q

how does butorphanol act on mu receptors

A

antagonist

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13
Q

how does butorphanol act on kappa receptors

A

agonist

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14
Q

how does butorphanol act on kappa receptors

A

agonist

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15
Q

what are the two types of antagonism

A

competitive & non-competitive

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16
Q

what type of antagonism is present when the antagonistic drug acts on the SAME RECEPTOR as the agonist

A

competitive antagonism

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17
Q

what type of antagonism is reversible when it can be over come by the agonist concentration

A

competitive antagonism

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18
Q

what are examples of competitive antagonistic drugs

A

atropine
propranolol

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19
Q

how will a competitive antagonist impact the potency of a drug

A

lowers potency

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20
Q

how does competitive antagonism effect efficacy

A

efficacy remains constant

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21
Q

which antagonism type is irreversible

A

non-competitive

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22
Q

what type of bond is used by antagonistic non-competitive drugs?

A

covalent

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23
Q

how does the use of a non-competitive antagonistic drug effect potency

A

decreases potency

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24
Q

how does the use of a non-competitive antagonistic drug affect efficacy

A

decreases efficacy

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25
Q

True or False:

A non-competitive EMax will eventually equal that of the regular drug

A

FALSE
there will always be a decrease in efficacy

26
Q

Besides comparing the efficacy of a drug with different amounts of antagonists, what else can those graphs be used for

A

determine antagonist strength

27
Q

what type of site does the non-competitive drug bind to

A

allosteric site because it causes change to the active site

28
Q

what type of agonist acts at the same receptors as an agonist but produces an opposite pharmacological effect

A

inverse agonist

29
Q

what are examples of inverse agonists

A

H1 receptor antihistaminergic drugs
B-blockers / carvedilol
antipsychotic drugs
antihypertensive drugs

30
Q

which type of agonist would you expect to see to bind to only active receptors

A

full agonist
competitive antagonist

31
Q

what agonist type would you expect to see occupying mostly active state receptors but some resting state

A

partial agonist

32
Q

what is the result of the partial agonist only occupying most but not all of the active state receptors

A

lowered max response / partial response

33
Q

what drug type do you expect to see occupying an equal amount of active and resting state receptors

A

antagonist

34
Q

what agonist type would you expect to see only occupying resting state receptors

A

inverse agonist
competitive antagonist

35
Q

what is the effect of an inverse agonist only occupying resting state receptors

A

produces the opposite effect of the agonist

36
Q

True or False:

Drug response is a linear function of drug occupancy

A

true

37
Q

what occurs when a drug occupies all available receptors

A

maximal response

38
Q

when is a response from a drug terminated

A

when it dissociated from the receptor

39
Q

what is occupancy theory of a drug

A

maximal response is proportional the the drug-receptor complex bindings

40
Q

when does max response of a drug occur

A

when all receptors are occupied at equilibrium

41
Q

when there is no ligand present, how is the equilibrium balanced

A

lies far to the left

42
Q

what state of receptor do agonists have a higher affinity for

A

active state

43
Q

which dose-response relationship describes a drug effect that increases in proportion to an increasing drug dose

A

graded dose-response

44
Q

which dose-response is used to measure the effect of a drug on an individual person

A

graded dose-response

45
Q

what can a graded dose-response be used to determine

A

efficacy of a drug over time

46
Q

which dose-response relationship is used to describe a drug effect as present or absent

A

quantal dose-response

47
Q

which dose-response relationship should be determined with a population of people

A

quantal dose-response

48
Q

what does a quantal dose-response graph plot

A

rate of an outcome occurrence in a population against a drug dose

49
Q

besides drug effects on a population, what else can a quantal dose-response graph determine

A

toxic levels of a drug

50
Q

which dose-response relationship results in a greater magnitude of response as the dose increases

A

graded dose-response

51
Q

True or False:

Using Quantal dose-response, a higher percentage of the population will be affected as the dose is increased

A

true

52
Q

when is a drug considered unsafe/toxic in terms of standard safety margin

A

drug has a low safety margin

53
Q

what is used to determine the standard safety margin

A

ED (effective dose)
LD (lethal dose)

54
Q

what is used to evaluate the safety of a certain drug

A

therapeutic index

55
Q

what kind of receptor regulation is present when there is a loss of receptors present

A

downregulation

56
Q

what kind of regulation is present when there is an increase of receptors present

A

upregulation

57
Q

what is the outcome of upregulation

A

more sensitive to a hormone or neurotransmitter

58
Q

how is upregulation created

A

long term administration of an antagonist

59
Q

explain the process of using prolonged antagonistic drugs on upregulation

A

all represent receptors become blocked forcing the cells to create new receptors for ligands to bind to

60
Q

what causes downregulation

A

long term exposure to agonists

61
Q

what is the result of downregulation

A

decreased responsiveness

Pharmacology 1 (10 decks)

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