Drug metabolism Flashcards

1
Q

BIoactivation of Valacyclovir –>

A

Valacyclovir to acyclovir by Hydrolysis then acyclovir monophosphate by viral thymidine kinase then to acyclovir triphosphate

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2
Q

Acetaminophen: benzoquinoneimine relation

A

Toxic metabolite

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3
Q

Cyclophosphamide (CP) and ifosfamide (IF) are widely used antineoplastic agents, but their side-effect of hemorrhagic cystitis (HC) is still encountered as an important problem. ________ is the main molecule that binds with bladder mucus and responsible of this side-effect and ______ is the commonly used preventive agent

A

Acrolein

mesna (2-mercaptoethane sulfonate)

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4
Q

Active metabolite of spironolactone

A

Canrenone

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5
Q

How does methanol causes histotoxic hypoxia

A

Metabolism of methanol, give rise to formic acid. This acid is an inhibitor of the mitochondrial cytochrome OXIDASE causing histotoxic hypoxia

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6
Q

methanol TOXICITY ANTIDOT

A

Ethanol and fomepizole can be administered to delay methanol metabolism

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7
Q

Ethylene glycol toxicity: mechanism.

A

oxalic acid formation

ANtidot: Ethanol and fomepizole

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8
Q

The primary location for drug metabolizing enzymes

A

Endoplasmic reticulum

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9
Q

UDPGT catalyze

A

glucuronidation

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10
Q

UDPGT present in

A

Mitochondria & Endoplasmic reticulum

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11
Q

Many water-soluble enzymes presnt in

A

Cytosol

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12
Q

alcohol dehydrogenase present in

A

Endoplasmic reticulum

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13
Q

aldehyde dehydrogenase present in

A

Mitochondria

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14
Q

MAOi presnt in

A

Mitochondria

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15
Q

GSH present in

A

Endoplasmic reticulum

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16
Q

Non microsomal enzyme participating in Phase I reaction

A

reductase, aminase and monoamine oxidase (MAO), alcohol dehydrogenase

17
Q

What are Conjugation reactions

A
Glucuronidation, 
glutathione conjugation, 
sulfonation, 
acetylation, 
glycine conjugation
 methylation
18
Q

Bacteria resident in the GI tract are known to be involved in what type of reduction

A

azo and nitro reductions

19
Q

Phase I reaction in sulfasalazine and olsalazine

A

azoreduction

20
Q

5-aminosalicylic acid (5ASA) and sulfpyridine is the product of

A

reduction sulfasalazine

21
Q

General term of enzyme used in conjugation reactions that transfers a high-energy molecule called the cofactor or cosubstrate to the xenobiotic

A

transferase

22
Q

Glutathione is tripeptide . what are the peptides?

A

glycine-cysteine-glutamate

23
Q

Esters (hydrolysis) produce →

A

acid + alcohol.

24
Q

Acyclovir -→ Acyclovir Monophosphate. enzyme involved is

A

viral thymidine kinase

25
Q

Amide hydrolysis products -→

A

acid + amine.

26
Q

Acetanilide hydroxylation →

A

acetaminophen.

27
Q

Acetamininophen → N-Benzylquinoneimine

A

Glutathione conjugation

N-Benzylquinoneimine ——————— → Mercaptopurine

28
Q

vitamin C deficiency Decreases ______ pathways

A

oxidative

29
Q

Vitamin E deficiency retards ____________

A

dealkylation and hydroxylation.

30
Q

Low protein diet decreases _______ drug metabolism

A

oxidative