Pharmacokinetics Flashcards

1
Q

Absorption

A

Process by which unchanged drug proceeds from the site of administration to the site of measurement

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2
Q

Bioavailability

A

Fraction of unchanged drug reaching the systemic circulation following administration by any route

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3
Q

Bioequivalence

A

90% confidence interval of the ratios of the population average estimates of AUC, Cmax and Tmax for the test and reference formulations lie within a pre established bioequivalence limit, usually 80-125%

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4
Q

Therapeutic equivalence

A

Comparable clinical effectiveness and safety between related products

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5
Q

First pass effect

A

To reach general circulation, a drug given orally must pass through the liver via the portal system

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6
Q

Distribution

A

Reversible transfer of drug from one location to another within the body

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7
Q

Volume of Distribution

A

Fluid volume that would be required to contain all of the drug in the body at the same concentration in the blood or plasma.

Vd = amt. of drug in body/plasma drug conc. = X/Cp

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8
Q

Phase I Reactions

A

Convert the parent drug to a more polar metabolite by introducing or unmasking a functional group

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9
Q

Inducer

A

Decrease the conc. Of drug, decrease efficacy and increase metabolism

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10
Q

Inhibitor

A

Increase conc. Of drug, increase toxicity and decrease metabolism

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11
Q

Phase II Biotransformation

A

Conjugation reaction
Metabolized by covalent addition of an endogenous species such as sugar or amino acid
Converts a lipophilic drug into a more polar product

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12
Q

Conjugation reactions

A

Glucoronidation by UDP glucuronosyltransferases
Sulfation/sulfonation by STs
Acetylation by acetyltransferases

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13
Q

Clearance

A

Volume of blood from which all drug would appear to be removed per unit time

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14
Q

Half-Life

A

Time required for the drug concentration to fall by half

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15
Q

First order kinetics

A

Constant fraction of a drug is eliminated per unit time

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16
Q

Zero order kinetics

A

Constant amount of drug eliminated per unit time

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17
Q

ER:F

A

Inverse

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18
Q

Cl:t1/2

A

Inverse

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19
Q

fu(p):Vd

A

Direct

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20
Q

fu(t):Vd

A

Inverse

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21
Q

t1/2:Vd

A

Direct

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22
Q

ER:First pass

A

Direct

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23
Q

Css:t1/2

A

No relationship

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24
Q

Time to Css:t1/2

A

Direct

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25
Q

Absorption

A

Process by which unchanged drug proceeds from the site of administration to the site of measurement

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26
Q

Bioavailability

A

Fraction of unchanged drug reaching the systemic circulation following administration by any route

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27
Q

Bioequivalence

A

90% confidence interval of the ratios of the population average estimates of AUC, Cmax and Tmax for the test and reference formulations lie within a pre established bioequivalence limit, usually 80-125%

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28
Q

Therapeutic equivalence

A

Comparable clinical effectiveness and safety between related products

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29
Q

First pass effect

A

To reach general circulation, a drug given orally must pass through the liver via the portal system

30
Q

Distribution

A

Reversible transfer of drug from one location to another within the body

31
Q

Volume of Distribution

A

Fluid volume that would be required to contain all of the drug in the body at the same concentration in the blood or plasma.

Vd = amt. of drug in body/plasma drug conc. = X/Cp

32
Q

Phase I Reactions

A

Convert the parent drug to a more polar metabolite by introducing or unmasking a functional group

33
Q

Inducer

A

Decrease the conc. Of drug, decrease efficacy and increase metabolism

34
Q

Inhibitor

A

Increase conc. Of drug, increase toxicity

35
Q

Phase II Biotransformation

A

Conjugation reaction
Metabolized by covalent addition of an endogenous species such as sugar or amino acid
Converts a lipophilic drug into a more polar product

36
Q

Conjugation reactions

A

Glucoronidation by UDP glucuronosyltransferases
Sulfation/sulfonation by STs
Acetylation by acetyltransferases

37
Q

Clearance

A

Volume of blood from which all drug would appear to be removed per unit time

38
Q

Half-Life

A

Time required for the drug concentration to fall by half

39
Q

First order kinetics

A

Constant fraction of a drug is eliminated per unit time

40
Q

Zero order kinetics

A

Constant amount of drug eliminated per unit time

41
Q

ER:F

A

Inverse

42
Q

Cl:t1/2

A

Inverse

43
Q

fu(p):Vd

A

Direct

44
Q

fu(t):Vd

A

Inverse

45
Q

t1/2:Vd

A

Direct

46
Q

ER:First pass

A

Direct

47
Q

Css:t1/2

A

No relationship

48
Q

Time to Css:t1/2

A

Direct

49
Q

Absorption

A

Process by which unchanged drug proceeds from the site of administration to the site of measurement

50
Q

Bioavailability

A

Fraction of unchanged drug reaching the systemic circulation following administration by any route

51
Q

Bioequivalence

A

90% confidence interval of the ratios of the population average estimates of AUC, Cmax and Tmax for the test and reference formulations lie within a pre established bioequivalence limit, usually 80-125%

52
Q

Therapeutic equivalence

A

Comparable clinical effectiveness and safety between related products

53
Q

First pass effect

A

To reach general circulation, a drug given orally must pass through the liver via the portal system

54
Q

Distribution

A

Reversible transfer of drug from one location to another within the body

55
Q

Volume of Distribution

A

Fluid volume that would be required to contain all of the drug in the body at the same concentration in the blood or plasma.

Vd = amt. of drug in body/plasma drug conc. = X/Cp

56
Q

Phase I Reactions

A

Convert the parent drug to a more polar metabolite by introducing or unmasking a functional group

57
Q

Inducer

A

Decrease the conc. Of drug, decrease efficacy and increase metabolism

58
Q

Inhibitor

A

Increase conc. Of drug, increase toxicity

59
Q

Phase II Biotransformation

A

Conjugation reaction
Metabolized by covalent addition of an endogenous species such as sugar or amino acid
Converts a lipophilic drug into a more polar product

60
Q

Conjugation reactions

A

Glucoronidation by UDP glucuronosyltransferases
Sulfation/sulfonation by STs
Acetylation by acetyltransferases

61
Q

Clearance

A

Volume of blood from which all drug would appear to be removed per unit time

62
Q

Half-Life

A

Time required for the drug concentration to fall by half

63
Q

First order kinetics

A

Constant fraction of a drug is eliminated per unit time

64
Q

Zero order kinetics

A

Constant amount of drug eliminated per unit time

65
Q

ER:F

A

Inverse

66
Q

Cl:t1/2

A

Inverse

67
Q

fu(p):Vd

A

Direct

68
Q

fu(t):Vd

A

Inverse

69
Q

t1/2:Vd

A

Direct

70
Q

ER:First pass

A

Direct

71
Q

Css:t1/2

A

No relationship

72
Q

Time to Css:t1/2

A

Direct