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PH 110 - Pharmaceutical & Medicinal Organic Chemistry (Lec) > PRELIM 02 - Metabolic Changes of Drugs > Flashcards

PRELIM 02 - Metabolic Changes of Drugs Flashcards

1
Q

The process by which the drug is chemically converted in the body to a metabolite

A

Drug metabolism

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2
Q

Refers to the formation of inactive and relatively nontoxic compounds

A

Detoxification

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3
Q

Main site of drug metabolism

A

Liver

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4
Q

The first pass effect __________ bioavailability

A

Decreases

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5
Q

Effect wherein drugs are metabolized before they are distributed to the rest of the body

A

First pass effect

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6
Q

Effect that involves the rapid metabolism of an orally administered drug before reaching the general circulation

A

First pass effect

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7
Q

The most important enzyme system affecting drug metabolism

A

CYP450 enzyme system

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8
Q

Cytochrome P450 enzymes are involved in __________

A

Oxidative biotransformation

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9
Q

Cytochrome P450 enzymes are __________

A

Monooxygenases

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10
Q

Caffeine, testosterone, R-warfarin (CYP enzyme)

A

1A1

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11
Q

Acetaminophen, caffeine, phenacetin, R-warfarin (CYP enzyme)

A

1A2

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12
Q

17β-estradiol, testosterone (CYP enzyme)

A

2A6

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13
Q

Cyclophosphamide, erythromycin, testosterone (CYP enzyme)

A

2B6

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14
Q

Acetaminophen, tolbutamide, hexobarbital, S-warfarin, phenytoin, testosterone, R-warfarin, zidovudine (CYP enzyme)

A

2C-family

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15
Q

Acetaminophen, caffeine, chlorzoxazone, halothane (CYP enzyme)

A

2E1

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16
Q

Acetaminophen, codeine, debrisoquine (CYP enzyme)

A

2D6

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17
Q

Acetaminophen, caffeine, carbamazepine, codeine, cortisol, erythromycin, cyclophosphamide, S- and R-warfarin, phenytoin, testosterone, halothane, zidovudine (CYP enzyme)

A

3A4

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18
Q

2 phases of drug metabolism

A

Phase I, Phase II

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19
Q

Phase I is also known as __________

A

Functionalization reactions

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20
Q

Oxidation of aromatic moieties (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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21
Q

Oxidation of olefins (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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22
Q

Oxidation of benzylic, allylic carbon atoms, and carbon atoms to carbonyl and imines (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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23
Q

Oxidation involving carbon-heteroatom systems (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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24
Q

Oxidation of alcohols and aldehydes (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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25
Q

Other miscellaneous oxidative reactions (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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26
Q

Reduction of aldehydes and ketones (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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27
Q

Reduction of nitro and azo compounds (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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28
Q

Miscellaneous reductive reactions (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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29
Q

Hydrolysis of esters and amides (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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30
Q

Hydration of epoxides and arene oxides by epoxide hydrase (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

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31
Q

Phase II reaction is also known as __________

A

Conjugation reactions

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32
Q

Glucuronic acid conjugation (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

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33
Q

Sulfate conjugation (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

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34
Q

Conjugation with glycine, glutamine, and other amino acids (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

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35
Q

Glutathione or mercapturic acid conjugation (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

36
Q

Acetylation (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

37
Q

Methylation (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

38
Q

Involves the introduction of a functional polar group by direct introduction or modification/unmasking (Phase of drug metabolism)

A

Phase I (Functionalization reaction)

39
Q

4 functional polar groups (OCNS)

A

OH, COOH, NH2, SH

40
Q

__________ involves the direct introduction of functional group (Examples of Phase I reactions)

41
Q

__________, __________, and __________ involves modifying or unmasking existing functional groups (Examples of Phase I reactions) (ORH)

A

Oxidation, Reduction, Hydrolysis

42
Q

Involves the conjugation or attachment of small, polar, and ionization endogenous compounds (Phase of drug metabolism)

A

Phase II (Conjugation reaction)

43
Q

Phase II (Conjugation reactions) are catalyzed by __________

A

Transferase enzymes

44
Q

Is the most common conjugative pathway in drug metabolism due to readily available supply of D-glucuronic acid (Examples of Phase II reactions)

A

Glucuronidation

45
Q

In infants and young children, the __________ conjugate is the main urinary product

46
Q

Involves the conjugation of xenobiotics with sulfate (Examples of Phase II reactions)

A

Sulfonation/Sulfate conjugation

47
Q

Conjugation of xenobiotics with sulfate occurs primarily with __________

48
Q

The sulfate conjugation process involves the activation of inorganic sulfate to the coenzyme __________

A

3-phosphoadenosine-5-phosphosulfate (PAPS)

49
Q

The amino acids __________ and __________ are used to conjugate carboxylic acids (GG)

A

Glycine, Glutamine

50
Q

The amino acids glycine and glutamine are used to conjugate __________

A

Carboxylic acids

51
Q

__________ conjugation is common to most animals

52
Q

__________ conjugation appears to be confined mainly to humans and other primates

53
Q

Takes place in most cells; important in detoxifying potentially dangerous environmental toxins (Examples of Phase II reactions)

A

Glutathione conjugation

54
Q

Xenobiotics conjugated with GSH undergo further biotransformation to give S-substituted N-acetylcysteine products called __________

A

Mercapturic acids

55
Q

Its main function is to terminate pharmacological activity and detoxification (Examples of Phase II reactions)

A

Acetylation

56
Q

This variation is genetic and is caused mainly by differences in N-acetyltransferase activity

A

Acetylation polymorphism

57
Q

__________ and __________ are rapid acetylators (EA)

A

Eskimos, Asians

58
Q

__________ and some __________ groups are mainly slow acetylators (EW)

A

Egyptians, Western European

59
Q

Is important in the biosynthesis of many endogenous compounds and in the inactivation of numerous physiologically active biogenic amines (Examples of Phase II reactions)

A

Methylation

60
Q

The coenzyme involved in methylation reactions is __________

A

S-Adenosylmethionine (SAM)

61
Q

Women are __________ ethanol metabolizers than men

62
Q

Biotransformation time of phenylbutazone in rabbits

63
Q

Biotransformation time of phenylbutazone in horses

64
Q

Biotransformation time of phenylbutazone in monkeys

65
Q

Biotransformation time of phenylbutazone in mice

66
Q

Biotransformation time of phenylbutazone in man

67
Q

Caucasians are __________ acetylators

68
Q

Meaning of NAPQI (a toxic byproduct of paracetamol metabolism)

A

N-acetyl-para-benzo-quinone imine

69
Q

Antidote for paracetamol overdose

A

N-acetylcysteine

70
Q

In __________, phase II reaction occurs first before phase I

A

Paracetamol

71
Q

Reduction of a nitro group yields an __________

72
Q

Reduction of a disulfide group yields a __________

73
Q

Oxidation of an amine group yields a __________

74
Q

Oxidation of a thiol group yields a __________

75
Q

Digestion of carbohydrates starts in the __________

76
Q

Digestion of proteins starts in the __________

77
Q

Phase I is more likely to cross the __________ than Phase II

A

Cell membrane

78
Q

Glucuronidation involves the attachment of glucuronic acid to functional groups like __________, __________, and __________ (PAC)

A

Phenol, Alcohol, Carboxylic acid

79
Q

The most hepatotoxic anti-TB drug

80
Q

N-acetylcysteine is given instead of glutathione during a paracetamol overdose because of __________

A

Le Chatelier’s principle

81
Q

2 rate limiting steps of drug metabolism (SP)

A

Solubility (↑↓↑↓), Permeability (↑↑↓↓)

82
Q

Approximately __________ to __________% of Caucasians lack CYP2D6 activity

83
Q

Approximately __________ to __________% of Africans lack CYP2D6 activity

84
Q

Approximately __________ to __________% of Asians lack CYP2D56 activity

85
Q

Enzyme responsible for converting methanol to acetaldehyde

A

Alcohol dehydrogenase

86
Q

Enzyme responsible for converting ethylamine to acetaldehyde

A

Monoamine oxidase (MAO)

PH 110 - Pharmaceutical & Medicinal Organic Chemistry (Lec) (8 decks)

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