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pharm > lec7 pharmacodynamics > Flashcards

lec7 pharmacodynamics Flashcards

1
Q

categories of drug effects

A

therapeutic
nontherapeutic
placebo

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2
Q

dose intensity curves measures

A

how much effect

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3
Q

dose frequency curves measures

A

hoe many affected

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4
Q

application of the law of mass action to the kinetics of the binding of drug and receptor creates the equation

A

drug + receptor bound-receptor –> effect

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5
Q

dissociation constant (Kd) for the drug from the receptor is measured by (2 equations for it)

A

=Kr/Kf
K reverse / K forward
or
= drug + receptor / bound-receptor

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6
Q

the curve for durg conc v fraction of bound receptors (i.e. bound / total receptors) is what shape

A

hyperbolic

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7
Q

the conc at which half of the receptors are bound is the

A

Kd = dissociation constant

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8
Q

Bmax is the

A

totality of the receptors bound by the drug

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9
Q

why are semilogarithmic plots used instead of linear (hyperbola)

A

linear plots at point near zero, the effect changes rapidly
semi log curve has large middle portion close to EC50 which is linear and easier to work with so easier to make accurate determination

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10
Q

Emax =

A

maximum effect

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11
Q

what is used as a measure of Kd

A

EC50

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12
Q

lower EC50 means what to the affinity for binding to the receptor

A

lower EC50 –> lower Kd –> higher affinity for binding to the receptor

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13
Q

drug conc producing an effect that’s 50% of the max effect

A

EC50

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14
Q

EC50 provides what important characteristic of drugs

A

potency

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15
Q

Emax provides what important characteristic of drugs

A

efficacy

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16
Q

define efficacy

A

max effect of a drug achieveable at a high dose

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17
Q

lower EC50 = ____ potency

A

higher

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18
Q

lower Emax = ____ efficacy

A

lower

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19
Q

when comparing 2 drugs you want the one with the lower or higher Emax

A

higher

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20
Q

how well the drug binds the receptor

A

potency

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21
Q

how well the drug produces the effect

A

efficacy

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22
Q

t/f potency and efficacy are related

A

f: unrelated

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23
Q

potency is ___ related to EC50

A

inversely

lower potency = higher EC50

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24
Q

ability of a drug to affect one tissue or receptor in prefereance to another

A

selectivity

25
Q

a highly selective drug is one which

A

affects only a receptor or tissue without affecting others

26
Q

what curve is needed to measure selectivity

A

concentration - response

27
Q

what type of agonist:

drug that has efficacy greater than zero but less than a full agonist

A

partial agonist

28
Q

what type of agonist:

drug that binds to a receptor and produces max bio response

A

full agonist

29
Q

what type of agonist:

drug that induces pharm response opposite of agonist

A

inverse agonist

30
Q

what is a neutral antagonist

A

drug that does NOT induce a bio response and reduces/blocks response induced by agonist

31
Q

order the 3 agonists from highest emax to lowest

A

full > partial > inverse

32
Q

process where a drug decr or opposes action of another drug or endogenous ligand

A

antagonism

33
Q

what are the 4 types of antagonisms

A

chemical
pharmacokinetic
physiological
pharmacological

34
Q

type of antagonism where antagonist accelerates the metabolism or the elimination of the agonist

A

pharmacokinetic

35
Q

type of antagonism where antagonist binds directly to agonistto make it inactive

A

chemical

36
Q

type of antagonism where theres 3 types

reversible competitive, noncompetitive, irreversible

A

pharmacological

37
Q

type of antagonismwhere antagonist activates a diff mechanism that opposes the effects of the agonist

A

physiological

38
Q

what happens to potency and efficacy in reversible competitive

A

right shift of dose-response curve
higher EC50 –> lower potency
no change in efficacy

39
Q

competitive antagonism can be overcome by

A

incr the conc of agonist to achieve the same effect as before

40
Q

can a noncompetitive antagonism be overcome

A

no cant restory to original response by incr conc of agonist

41
Q

what happens to potency and efficacy in noncompetitive

A

lower emax –> decr efficacy

unchanged potency

42
Q

what happens to potency and efficacy in irreversible competitive

A

lower emax –> decr effcacy

no change potency

43
Q

joint effect of 2 drugs is the sum of their individual effects

A

summation

44
Q

joint effect of 2 drugs is greater than sum of their effects

A

synergism

45
Q

inert drug enhances the effect of another drug

A

potentiation

46
Q

drug effect loss over time

A

tolerance

47
Q

mechanism for decreased effect (includes tachyphylaxis)

A

desensitization

48
Q

what curve is all or nothing i.e. their effect is scored on whether present or absent

A

quantal dose-response curves

49
Q

diff bn incremental and cumulative quantal curves

A

incremental - as dose incr, number responders incr (bell curve)
cumulative - as dose incr, number responders adds up

50
Q

which curve has more variability?
shallow, wider
taller, narrow

A

shallow, wide

51
Q

dose producing effect in 50% of subject

A

ED50

52
Q

dose making death in 50% of subjects

A

LD 50 = lethal dose

53
Q

what do different slopes in quantal curves imply

A

diff sources of variability, suggesting diff in route or mechanism of action

54
Q

therapeutic index equation

A

LD50 / ED50

55
Q

the higher the therapeutic index

A

the safer the drug

56
Q

why is pop variability important in quantal curves

A

bc can have same therapeutic index but different risk

57
Q

standardized safety margin equation

A

(LD1-ED99) / ED99 * 100

58
Q

the more positive the ED99 or the greater the diff bn LD1 and ED99 , the ___ the drug

A

safer

pharm (6 decks)

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