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Disease and Defense- Pharm > Drug Metabolism Reactions > Flashcards

Drug Metabolism Reactions Flashcards

1
Q

Drug-metabolizing enzymes have _____ substrates and play role in normal metabolism.

A

endogenous

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1
Q

Nonresponse to antidepressants has been reported in ______ UMs.

A

CYP2D6

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2
Q

______ is a detoxifying process involving formation of readily excreted metabolites that are pharmacologically inactive.

A

Drug metabolism

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2
Q

Individual patients can vary in enzyme activity and can be classified at the extremes as ______ or ______ with total absence of enzyme.

A

ultra-rapid (UM) metabolizers; poor metabolizers (PM)

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2
Q

______ has been reported in CYP2D6 UMs.

A

Nonresponse to antidepressants

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3
Q

_____ are generally converted to more water-soluble (more polar) compounds that are then more readily excreted.

A

Lipid-soluble compounds

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4
Q

Insufficient analgesia with codeine is seen in CYP2D6 _____ due to failure to metabolize to the active metabolite, morphine.

A

PMs

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5
Q

Drug metabolism is a ______ involving formation of readily excreted metabolites that are pharmacologically inactive.

A

detoxifying process

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5
Q

Hydrolysis of some _______ by intestinal bacterial enzymes (β-glucuronidase) results in the formation of _____.

A

glucuronides; free drug

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5
Q

What is N-Acetylation?

A

amide bond formation via N-acetyltransferases

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6
Q

_____ enzymes are present in plasma, liver, and other tissues.

A

Esterases

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7
Q

______ are microsomal enzymes present in liver, kidney, GI tract.

A

Glucuronyl transferases

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7
Q

Glucuronyl transferases are microsomal enzymes present in the ____, _____, and _____.

A

liver, kidney, GI tract

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7
Q

Glutathione-S-transferases have a limited role in drug metabolism but are extremely important in detoxification of _____, ______, and _______.

A

carcinogens; pollutants; toxic metabolites

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8
Q

Oxidation is a _____ metabolic reaction.

A

phase I

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9
Q

Sulfate conjugation results in formation of strong acids with a pKa of _____.

A

1

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10
Q

What is the product of a conjugation reaction?

A

a highly water-soluble, readily excreted product

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10
Q

In N-acetylation, the acetyl group is donated by _____.

A

acetyl CoA

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11
Q

______ of PPIs for peptic ulcers is seen in CYP2C19 PMs.

A

Decreased efficacy

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12
Q

Where are amidases found?

A

liver and gut flora

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13
Q

Name a drug that, when metabolized, can create a toxic metabolite.

A

acetaminophen (to N-Acetyl-benzoquinoneimine)

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13
Q

Increased ______ is seen in patients with CYP2D6 activity PMs.

A

antipsychotic drug toxicity

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13
Q

_____ hydrolyze esters to corresponding alcohol and acid.

A

Esterases

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13
Q

In _____, an amide bond is formed via N-acetyltransferases.

A

N-acetylation

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15
Q

______ have endogenous substrates and play role in normal metabolism.

A

Drug-metabolizing enzymes

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15
Q

What 2 isozymes account for 25% of drug metabolism?

A

CYP2D6 and CYP2C19

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16
Q

______ of some glucuronides by ______ (β-glucuronidase) results in the formation of free drug.

A

Hydrolysis; intestinal bacterial enzymes

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17
Q

Which phase I reduction can produce toxic intermediates?

A

nitro reduction

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19
Q

Give 2 examples of drugs that, when metabolized, are more active.

A

1) codeine (to morphine) 2) hydrocodone (to hydromorphone)

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19
Q

Codeine intoxication is seen in _____ UMs due to rapid metabolism to morphine.

A

CYP2D6

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20
Q

What is the postnatal development of the cytochrome P-450-dependent oxidation?

A

variable; usu neonates are 50-75% of adult levels, but some drugs are metabolized faster

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22
Q

Most drugs undergo ______ after administration to the patient.

A

enzyme-catalyzed chemical structure transformation

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23
Q

Increased antipsychotic drug toxicity in patients with CYP2D6 activity ______.

A

PMs

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23
Q

Increased antipsychotic drug toxicity is seen in patients with _____ activity PMs.

A

CYP2D6

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24
Q

What is Enterohepatic recirculation?

A

when the drug is secreted by the liver into bile as a drug-conjugate and then reabsorbed via the GI tract as a free drug

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25
Q

Which reactions do phase I transformations include?

A

oxidation, reduction, hydrolysis

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27
Q

What do CYP450 enzymes do?

A

catalyze oxidation in the smooth ER

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27
Q

The coenzyme donor of sulfate is _____.

A

PAPS

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29
Q

Cytochrome P450 is part of an oxidation system that also includes the cofactor NADPH, the flavoprotein NADPH-cytochrome P450 reductase, and ______.

A

molecular O2

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30
Q

Name an important enzyme in neurotransmitter metabolism.

A

monoamine oxidase

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31
Q

What is vitamin K reductase (VKORC1)?

A

the enzyme target of warfarin

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32
Q

Decreased efficacy of PPIs for peptic ulcers is seen in CYP2C19 _____.

A

PMs

34
Q

What other tissues, besides the liver, have enzymes capable of drug metabolism?

A

the intestine, lung, kidney, skin, placenta, and bacteria in the intestine

35
Q

What is a phase II transformation?

A

the endogenous substrate binds with functional group to form highly polar conjugate that is readily excreted

36
Q

Many transformations are catalyzed by membrane-bound enzymes of the ______ and some by soluble enzymes in the _____.

A

smooth endoplasmic reticulum; cytosol

36
Q

What is CYP2C9?

A

the enzyme that metabolizes warfarin

37
Q

______ include esterases and amidases.

A

Phase I hydrolysis reactions

38
Q

What enzyme does warfarin target?

A

vitamin K reductase [VKORC1]

40
Q

Drug-metabolizing enzymes have endogenous substrates and play role in _____.

A

normal metabolism

41
Q

What analyzes blood-derived DNA to detect genetic polymorphisms in the activity of CYP2D6 and CYP2C19?

A

Amplichip® CYP450 Test

42
Q

____ reach adult levels in first few months and are used to design pro-drugs.

A

Esterases

44
Q

Name 4 outcomes of drug metabolism.

A

1) inactivate drug 2) increase drug activation 3) activate previously unactive druge 4) make toxic metabolite

45
Q

In N-acetylation, an _____ bond is formed via N-acetyltransferases.

A

amide

46
Q

In cytochrome P-450-dependent oxidation, the substrate must be ______.

A

lipid soluble

48
Q

What is the most common pathway of chemical transformation in the body?

A

oxidation

49
Q

Phase I hydrolysis reactions include ____ and ____.

A

esterases; amidases

50
Q

What is the Amplichip® CYP450 Test?

A

test that analyzes blood-derived DNA to detect genetic polymorphisms in the activity of CYP2D6 and CYP2C19?

51
Q

_______ results in formation of strong acids with a pKa of 1.

A

Sulfate conjugation

52
Q

Cytochrome P450 is part of an oxidation system that also includes the cofactor NADPH, the flavoprotein _______, and molecular O2.

A

NADPH-cytochrome P450 reductase

53
Q

Where is monoamine oxidase located?

A

in the outer mitochondrial membrane

53
Q

Full adult activity of ____ is not reached for 5 years.

A

alcohol dehydrogenase

53
Q

In N-acetylation, an amide bond is formed via _____.

A

N-acetyltransferases

54
Q

The cytochrome P-450-dependent oxidation has both ____ and _____.

A

inducibility and inhibition

56
Q

Insufficient analgesia with codeine is seen in _____ PMs due to failure to metabolize to the active metabolite, morphine.

A

CYP2D6

58
Q

Recent evidence has suggested that individual differences in response to the anticoagulant effects of warfarin may be based on genetic variations to?

A

1) enzyme that warfarin targets (vitamin K reductase[VKORC1]) 2) enzyme that metabolizes warfarin (CYP2C9)

59
Q

What is the most common outcome of drug metabolism??

A

detoxification- excretion of metabolites that are pharmacologically inactive

61
Q

______ is part of an oxidation system that also includes the cofactor NADPH, the flavoprotein NADPH-cytochrome P450 reductase, and molecular O2.

A

Cytochrome P450

62
Q

What do amidases do?

A

Hydrolyze amides to acids and amines

63
Q

Hydrolysis of some glucuronides by intestinal bacterial enzymes (______) results in the formation of free drug.

A

β-glucuronidase

65
Q

What is another name for a phase II transformation?

A

conjugation

66
Q

PM

A

poor metabolizers

67
Q

What is the significance of monoamine oxidase?

A

it’s an important enzyme in neurotransmitter metabolism

68
Q

What may be the source of drug interactions in antibiotics and oral contraceptives?

A

enterohepatic recirculation

70
Q

Which enzymes in the smooth ER catalyze oxidation?

A

CYP450 enzymes

70
Q

______ with codeine is seen in CYP2D6 PMs due to failure to metabolize to the active metabolite, morphine.

A

Insufficient analgesia

71
Q

Cytochrome P450 is part of an oxidation system that also includes the cofactor ____, the flavoprotein NADPH-cytochrome P450 reductase, and molecular O2.

A

NADPH

72
Q

Name 4 conjugations.

A

1) Glucuronidation 2) N-Acetylation 3) Glutathione Conjugation 4) Sulfate Conjugation

74
Q

_____ occur in cytochrome P-450-dependent oxidation, including CYP1, CYP2, and CYP3.

A

Many different isozymes

75
Q

_____ are involved in the activation of certain sulfonamides.

A

Azo reductions

77
Q

______ can include the azo reduction, nitro reduction, or carbonyl reduction.

A

Phase I reductions

78
Q

Why are CYP2D6 and CYP2C19 important?

A

they account for 25% of drug metabolism, including many antidepressants, antipsychotics, and opioid analgesics

80
Q

_____ is seen in CYP2D6 UMs due to rapid metabolism to morphine.

A

Codeine intoxication

82
Q

What is a phase I transformation?

A

an insertion or unmasking of a functional group to make the molecule more soluble

83
Q

_______ have a limited role in drug metabolism but are extremely important in detoxification of carcinogens, pollutants, toxic metabolites.

A

Glutathione-S-transferases

84
Q

Nonresponse to antidepressants has been reported in CYP2D6 ____.

A

UMs

85
Q

The duration of action for most drugs would be extremely prolonged if terminated by ______ only.

A

renal excretion

86
Q

What is the chemical transformation drugs undergo inside the patient called?

A

biotransformation or drug metabolism

87
Q

Many different isozymes occur in cytochrome P-450-dependent oxidation, including ____, _____, and _____.

A

CYP1, CYP2, and CYP3

88
Q

Cytochrome P450-independent oxidations include ______ and _____.

A

dehydrogenases; oxidases

89
Q

Lipid-soluble compounds are generally converted to ______ that are then more readily excreted.

A

more water-soluble (more polar) compounds

90
Q

What is the richest source of CYP450?

A

Liver smooth endoplasmic reticulum

92
Q

Adult levels of _______ activity is reached by age 3-4 years.

A

Glucuronidation

93
Q

Why are conjugations limited by supply and more easily saturable than phase I reactions?

A

the drug or drug metabolite is coupled to an endogenous biochemical unit (highly reactive) provided by a coenzyme

94
Q

Phase I reductions can include _____, _____, and _____.

A

the azo reduction, nitro reduction, or carbonyl reduction

95
Q

What hydrolyzes amides to acids and amines?

A

amidases

96
Q

Drug metabolism is a detoxifying process involving formation of readily excreted metabolites that are _____.

A

pharmacologically inactive

97
Q

Codeine intoxication is seen in CYP2D6 ____ due to rapid metabolism to morphine.

A

UMs

98
Q

What enzyme metabolizes warfarin?

A

CYP2C9

99
Q

Give 3 examples of drugs that begin as inactive compounds and are metabolized to create the active ingredient.

A

1) Omeprazole (to a Sulfenamide) 2) Enalapril (to Enalaprilat) 3) Valacyclovir (to Acyclovir)

100
Q

Name 3 drugs that are metabolized faster in neonates than adults.

A

theophylline, phenytoin, phenobarbital

101
Q

______ include dehydrogenases and oxidases.

A

Cytochrome P450-independent oxidations

102
Q

_____ can vary in enzyme activity and can be classified at the extremes as ultra-rapid (UM) metabolizers or poor metabolizers (PM) with total absence of enzyme.

A

Individual patients

103
Q

Azo reductions are involved in the activation of _____.

A

certain sulfonamides

104
Q

UM

A

ultra-rapid

Disease and Defense- Pharm (12 decks)

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