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
what is the LD50
lethal dose for half of the subjects tested
26
what is a side effect
unintended effects that accompany therapeutic effects
27
what is the therapeutic index
a measurement of a drugs relative safety
28
how is therapeutic index calculated
ratio of LD50 to the ED50
29
What therapeutic index of a drug is considered safe
100+
30
what therapeutic index of a drug is considered unsafe
less than 10
31
what is efficacy of a drug
refers to how well a drug can produce a given effect
32
what is the potency of a drug
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
what is antagonism
potency or efficacy of a drug is reduced in the presence of another drug
34
what is synergism
two drugs together are more potent and/or efficacious than either drug alone
35
what are the two different kinds of synergism
additive and potentiation
36
what is additive synergism
when two drugs are given together and it increases the potency and efficacy of both
37
what is potentiation
Drug that has no effect increases potency of another drug when given in combination
38
what is competitive antagonism
antagonist binds to the same binding site on receptor as drug
39
how can competitive antagonism be overcome
can overcome by increasing the concentration of the drug
40
what does competitive antagonism do to the dose response curve
shifts curve to the right
41
what is a partial agonist
a drug that binds to a receptor at its active site but produces only a partial response
42
what is an inverse agonist
produce a response below the baseline
43
what is the difference between an inverse agonist and a competitive agonist
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
What is orthostatic binding
ligand binds to the agonist binding site
45
what is allosteric binding
ligand binds to alternative binding site
46
what is positive modulation (PAMS)
increase the effect of agonist binding
47
what is negative modulation (NAMS)
decrease effect of agonist binding