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Neuropharmacology of Addiction > Dose Curves > Flashcards

Dose Curves Flashcards

1
Q

What is the dose response function

A

expresses the relationship between the dose administered and the response observed

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2
Q

How are does response functions determined

A

groups of individuals are administered a different amount of a drug in question and the response is measured; the test groups are compared to a control group given a placebo

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3
Q

what is a placebo

A

an inactive drug looks like a medication but is not

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4
Q

what is the placebo effect

A

attributed to psychological factors; expectations of drug effects and prior experiences

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5
Q

what is a double blind procedure

A

control measure for bias; neither the subject or researcher knows whether the substance given is the medication or placebo

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6
Q

What is a dose response curve

A

graph comparing the size of response to the amount of drug
x-axis: dose of drug
y-axis: effect of the drug

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7
Q

what is the difference between dose and concentration

A

concentration is the amount of molecule of interest in its vehicle
Dose refers to the amount of drug administered to a person

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8
Q

what are the components of a dose response

A

1) Dose-plasma concentration relationship
2) Plasma concentration-response relationship

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9
Q

what are the advantages of plotting a dose response curve on a log scale

A

1) full range of doses can be observed
2) easier to illustrate the effects/interactions of agonists and antagonists

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10
Q

What is Kd?

A

ratio of drug receptor dissociation

[drug][receptor] / [drug-receptor complex]

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11
Q

What does it mean if a drug has a high Kd

A

weak interaction, low receptor affinity

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12
Q

what does it mean if a drug has a low Kd

A

strong interaction, high receptor affinity

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13
Q

What happens as the concentration of a free drug increases in terms of Kd

A

the percentage of bound receptors increases

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14
Q

What is Emax

A

maximal observed effect of a dose of a drug

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15
Q

how do you calculate E?

A

E= Emax * [D} / Kd + [D}

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16
Q

what is a graded dose response curve

A

measured in a single biologic unit
continuous scale (increased dose = increased effect)
relates dose to intensity of effect

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17
Q

what is a quantal dose curve

A

population studies
all or none pharmacologic effect (did drug work? yes or no)
relates dose to frequency of effect

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18
Q

what is the slope factor of a dose response curve

A

increase of slope illustrates how much change in effect a little increase of dosage will have

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19
Q

what is a curvilinear or biphasic function of a dose curve

A

increasing doses are associated with increasing responses and then the effect decreases

20
Q

what is the therapeutic window

A

the drug doses in which a therapeutic response is obtained

21
Q

what are the characteristics of drugs that can be derived from dose response curves

A

threshold dose
maximal response

22
Q

what is the threshold dose

A

the smallest dose that produces a measurable response

23
Q

what is the maximal response

A

greatest degree of a given response that can be achieved with that drug

24
Q

what is the ED50 of a drug

A

effective dose for half of the subjects tested /
the dose that produces 50% of max effect

25
Q

what is the LD50

A

lethal dose for half of the subjects tested

26
Q

what is a side effect

A

unintended effects that accompany therapeutic effects

27
Q

what is the therapeutic index

A

a measurement of a drugs relative safety

28
Q

how is therapeutic index calculated

A

ratio of LD50 to the ED50

29
Q

What therapeutic index of a drug is considered safe

A

100+

30
Q

what therapeutic index of a drug is considered unsafe

A

less than 10

31
Q

what is efficacy of a drug

A

refers to how well a drug can produce a given effect

32
Q

what is the potency of a drug

A

refers to how much of a drug is needed to produce a given effect
i.e. the less of a drug required to produce an effect = greater potency

33
Q

what is antagonism

A

potency or efficacy of a drug is reduced in the presence of another drug

34
Q

what is synergism

A

two drugs together are more potent and/or efficacious than either drug alone

35
Q

what are the two different kinds of synergism

A

additive and potentiation

36
Q

what is additive synergism

A

when two drugs are given together and it increases the potency and efficacy of both

37
Q

what is potentiation

A

Drug that has no effect increases potency of another drug when given in combination

38
Q

what is competitive antagonism

A

antagonist binds to the same binding site on receptor as drug

39
Q

how can competitive antagonism be overcome

A

can overcome by increasing the concentration of the drug

40
Q

what does competitive antagonism do to the dose response curve

A

shifts curve to the right

41
Q

what is a partial agonist

A

a drug that binds to a receptor at its active site but produces only a partial response

42
Q

what is an inverse agonist

A

produce a response below the baseline

43
Q

what is the difference between an inverse agonist and a competitive agonist

A

competitive agonist has no effect in the absence of agonist, whereas an inverse agonist deactivates receptors that are constitutively active in the absence of agonist

44
Q

What is orthostatic binding

A

ligand binds to the agonist binding site

45
Q

what is allosteric binding

A

ligand binds to alternative binding site

46
Q

what is positive modulation (PAMS)

A

increase the effect of agonist binding

47
Q

what is negative modulation (NAMS)

A

decrease effect of agonist binding

Neuropharmacology of Addiction (15 decks)

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