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PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) > PRELIM 02 - Drug Metabolism > Flashcards

PRELIM 02 - Drug Metabolism Flashcards

1
Q

Drug metabolism is also known as __________

A

Biotransformation

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2
Q

Process that plays a central role in the elimination of drugs and other foreign compounds (xenobiotics) from the body

A

Drug metabolism/Biotransformation

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3
Q

The most important organ in drug metabolism

A

Liver

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4
Q

Most drugs absorbed by the body are __________

A

Lipophilic

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5
Q

2 categories of drug metabolism reactions (FC)

A

Phase I (Functionalization reactions), Phase II (Conjugation reactions)

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6
Q

Phase I reactions are also known as __________ reactions

A

Functionalization

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7
Q

Phase II reactions are also known as __________

A

Conjugation reaction

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8
Q

Most common reaction under Phase I reaction

A

Oxidation

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9
Q

Most common reaction under Phase II reaction

A

Glucuronidation

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10
Q

Oxidation (Phase of drug metabolism)

A

Phase I (Functionalization)

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11
Q

Reduction (Phase of drug metabolism)

A

Phase I (Functionalization)

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12
Q

Hydrolysis (Phase of drug metabolism)

A

Phase I (Functionalization)

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13
Q

Glucuronidation (Phase of drug metabolism)

A

Phase II (Conjugation)

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14
Q

Sulfation (Phase of drug metabolism)

A

Phase II (Conjugation)

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15
Q

Glycine conjugation (Phase of drug metabolism)

A

Phase II (Conjugation)

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16
Q

Glutathione conjugation (Phase of drug metabolism)

A

Phase II (Conjugation)

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17
Q

Acetylation (Phase of drug metabolism)

A

Phase II (Conjugation)

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18
Q

Methylation (Phase of drug metabolism)

A

Phase II (Conjugation)

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19
Q

Involves the introduction of a functional polar group (ex. OH, COOH, NH2, SH) into the xenobiotic molecule to produce a more water-soluble compound (Phase of drug metabolism)

A

Phase I (Functionalization)

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20
Q

Involves direct introduction of the functional group or by modifying or “unmasking” existing functionalities (Phase of drug metabolism)

A

Phase I (Functionalization)

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21
Q

Involves the attachment of endogenous compounds to the functional handles of parent compounds to form water-soluble conjugated products (Phase of drug metabolism)

A

Phase II (Conjugation)

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22
Q

2 processes that terminate or attenuate biological activity (Exceptions in Phase II reactions) (MA)

A

Methylation, Acetylation

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23
Q

Process that protects the body against chemically reactive compounds or metabolites (Exceptions in Phase II reactions)

A

Glutathione (GSH) conjugation

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24
Q

Meaning of LUNA

A

Lipophilic, Unionized, Nonpolar, Absorbed

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25
Meaning of HIPE
Hydrophilic, Ionized, Polar, Excreted
26
Valence increase (Oxidation or reduction)
Oxidation
27
Loss of electrons (Oxidation or reduction)
Oxidation
28
Presence of reducing agent (Oxidation or reduction)
Oxidation
29
Addition of oxygen (Oxidation or reduction)
Oxidation
30
Removal of hydrogen (Oxidation or reduction)
Oxidation
31
Addition of electronegative element (Oxidation or reduction)
Oxidation
32
Valence decrease (Oxidation or reduction)
Reduction
33
Gain of electrons (Oxidation or reduction)
Reduction
34
Presence of oxidizing agent (Oxidation or reduction)
Reduction
35
Removal of oxygen (Oxidation or reduction)
Reduction
36
Addition of hydrogen (Oxidation or reduction)
Reduction
37
Removal of electronegative element (Oxidation or reduction)
Reduction
38
Major pathway for carboxylic acid derivatives such as amides and esters (Examples of Phase I reactions)
Hydrolysis
39
Cofactor involved in glucuronidation (an example of Phase II reaction)
Uridine diphosphate glucuronic acid (UDPGA)
40
Enzyme involved in glucuronidation (an example of Phase II reaction)
UDP glucuronosyltransferase
41
Cofactor involved in sulfation (an example of Phase II reaction)
Phosphoadenosyl phosphosulfate (PAPS)
42
Enzyme involved in sulfation (an example of Phase II reaction)
Sulfotransferase
43
Cofactor involved in glycine conjugation (an example of Phase II reaction)
Glycine
44
Enzyme involved in glycine conjugation (an example of Phase II reaction)
Acyl-CoA glycinetransferase
45
Was the first mammalian metabolite discovered from glycine conjugation
Hippuric acid
46
Cofactor involved in glutathione conjugation (an example of Phase II reaction)
Glutathione (GSH)
47
Enzyme involved in glutathione conjugation (an example of Phase II reaction)
GSH-S-transferase
48
3 amino acids that comprises glutathione (GCG)
Glutamate, Cysteine, Glycine
49
The __________ group in cysteine is responsible for detoxification in glutathione
Thiol (-SH)
50
Cofactor involved in methylation (an example of Phase II reaction)
S-Adenosylmethionine
51
Enzyme involved in methylation (an example of Phase II reaction)
Transmethylases/Methyltransferases
52
Cofactor involved in acetylation (an example of Phase II reaction)
Acetyl-CoA
53
Enzyme involved in acetylation (an example of Phase II reaction)
N-Acetyltransferase
54
__________ is not yet fully developed in neonates and children
Glucuronidation
55
Condition that results from the inability of infants to conjugate chloramphenicol with glucuronic acid
Grey baby syndrome
56
Grey baby syndrome results from the inability of infants to conjugate __________ with glucuronic acid
Chloramphenicol
57
Condition that results from the inability of newborns to conjugate bilirubin with glucuronic acid
Kernicterus (Neonatal hyperbilirubinemia)
58
__________ is the major metabolism route of acetaminophen in children
Sulfation
59
__________ is the major metabolism route of acetaminophen in adults
Glucuronidation
60
In __________, sulfation is major and there is a lack of glucuronyltransferase enzymes
Cats
61
In __________, glucuronidation is major and there is a lack of sulfotransferase enzymes
Pigs
62
In most animals, conjugation for benzoic acid occurs with __________
Glycine
63
In birds, conjugation for benzoic acid occurs with __________
Ornithine
64
___________ involves variation in acetylating ability caused mainly by differences in N-acetyltransferase activity
Acetylation polymorphism
65
4 drugs that undergo acetylation (HIPS)
Hydralazine, Isoniazid, Procainamide, Sulfonamide
66
Egyptians, African-Americans, and Caucasians are __________; they tend to accumulate higher drug plasma concentrations, which leads to a greater therapeutic response
Slow acetylators
67
Eskimos and Asians are __________; they eliminate the drug more rapidly, which leads to an inadequate therapeutic response
Rapid acetylators
68
__________ accumulate higher blood concentrations of the un-acetylated drug, thus they are more prone to drug-induced toxicities
Slow acetylators
69
In slow acetylators, hydralazine and procainamide increases their risk of __________
Systemic lupus erythematosus (SLE) syndrome
70
In slow acetylators, isoniazid increases their risk of __________
Peripheral nerve damage
71
In slow acetylators, sulfasalazine increases their risk of __________
Hematologic disorders
72
__________ produces toxic metabolites more rapidly; they are more likely to develop isoniazid-associated hepatitis
Rapid acetylators
73
__________ is the hepatotoxic metabolite of isoniazid
Acetylhydrazine
74
Rapid acetylators are more likely to develop __________
Isoniazid-associated hepatitis
75
Reduction of an aldehyde yields a __________
Primary alcohol
76
Reduction of a ketone yields a __________
Secondary alcohol
77
Oxidation of a primary alcohol yields an __________
Aldehyde
78
Oxidation of a secondary alcohol yields a __________
Ketone
79
Hydrolysis of an ester yields 1 __________ and 1 __________ (CA)
Carboxylic acid, Alcohol
80
An __________ is an example of a reducing agent
Antioxidant
81
Ranking of functional groups according to hydrolysis reactivity (Least to most reactive) (AETAA)
Amide, Ester, Thioester, Acid anhydride, Acid chloride

PH 110.1 - Pharmaceutical & Medicinal Organic Chemistry (Lab) (11 decks)

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