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Biochem > Drug/Alcohol Metabolism > Flashcards

Drug/Alcohol Metabolism Flashcards

1
Q

Heme containing superfamily of enzymes with overlapping specificities and allelic variation resulting in different enzymatic activities in different individuals

A

Cytochrome 450 (CYP) system

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2
Q

Most CYPs are here intracellularly

A

Embedded in smooth ER, facing cytosol

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3
Q

CYP for ethanol oxidation

A

CYP 2E1

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4
Q

Phase of xenobiotic metabolism that involves hydroxylation (generally)

A

1

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5
Q

Phase of xenobiotic metabolism that involves the attachment of hydrophilic/solubilizing group to solubilize the molecule
Conjugation reactions for solubility

A

2

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6
Q

Glycine forms conjugates with aromatic like these 2

A

Benzoic acid and aspirin

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7
Q

Aspirin is excreted as a conjugate with this

A

Glycine
(Salicyluric acid)

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8
Q

Glutamine forms conjugates with this

A

Phenylacetate and related compounds

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9
Q

Used to detoxify acetaminophen, cocaine

A

Glutathione

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10
Q

Compound used in the synthesis of plastics that can cause angiosarcoma in liver of exposed workers if not properly metabolized and excreted via CYP 2E1

A

Vinyl chloride

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11
Q

CYP that oxidizes vinyl chloride

A

CYP 2E1

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12
Q

Compound that detoxifies acetaminophen

A

Glutathione

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13
Q

Used as an antidote to acetaminophen poisoning, partly by stimulating glutathione synthesis and also be scavenging free radicals

A

N-acetyl-cysteine

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14
Q

N-acetyl-cysteine is used as an antidote to this

A

Acetaminophen

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15
Q

Toxin that accumulates when acetaminophen uses an alternate pathway via ethanol induces CYP 2E1

A

NAPQI

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16
Q

Fragments of the ER obtained after breaking open cells and separating various intracellular fractions by size and density

A

Microsomes

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17
Q

Km of CYP 2E1

A

High
Active at higher ethanol concentrations

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18
Q

Metabolic effect where MEOS is inducible and metabolizes certain drugs besides ethanol

A

Drug tolerance
Tolerance = inducible

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19
Q

Metabolic effect where alcohol will compete for enzyme with drugs

A

Drug intolerance
Intolerance = competes

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20
Q

Mold toxin found in wet grain and peanuts
CYP 2A1 metabolizes it to a compound producing liver cancer

A

Aflatoxin

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21
Q

Aflatoxin is metabolized to a compound producing liver cancer via this CYP

A

CYP 2A1

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22
Q

Benzopyrene is metabolized to an epoxide that reacts with these

A

DNA guanine residues
Disrups GC bps –> lung cancer

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23
Q

CYP that comprises over half the P450 isoforms

A

CYP 3A4

24
Q

Removes drugs from cells by activate transport
Frequently induced with CYP 3A4

A

Multi-drug transporter (MDR1 gene)

25
Q

MDR is frequently induced with this

A

CYP 3A4

26
Q

Theophylline is a drug for asthma that is metabolized by this CYP

A

CYP 3A4

27
Q

HIV protease inhibitors are metabolized by this CYP

A

CYP 3A4

28
Q

Warfarin is metabolized by this CYP

A

CYP 3A4

29
Q

SSRIs are metabolized by this CYP

A

CYP 3A4

30
Q

Oral contraceptives are metabolized by this CYP

A

CYP 3A4

31
Q

Natural product that induces CYP 3A4, accelerating metabolism of many drugs and affecting their efficacy

A

St. John’s Wort

32
Q

Chemotherapy drugs may be metabolized by this CYP

A

CYP 3A4

33
Q

Simvastatin and atorvastatin are metabolized by this CYP

A

CYP 3A4

34
Q

CYP that is NOT inducible and metabolizes beta blockers, anti-arrhythmics, certain antidepressants

A

CYP 2D6

35
Q

CYP that converts codeine to more active morphine

A

CYP 2D6

36
Q

Risk of lung cancer is related to genetic ability to induce this CYP

A

CYP 2A6

37
Q

CYP inhibited by components of fresh grapefruit juice, thus prolonging the effects of drugs it metabolized

A

CYP 3A4

38
Q

CYP with 4 phenotypes: Poor metabolizer, intermediate metabolizer, extensive (normal) metabolizer, and ultra-rapid metabolizer

A

CYP 2D6

39
Q

CYP that is responsible for majority of the inter-individual variability in the ability to metabolize about 25% of the drugs currently marketed along with CYP2D6

A

CYP 2C19

40
Q

Neonates lack this CYP, making them susceptible to toxicity from caffeine
Induced by St. John’s Wort

A

CYP 2A6

41
Q

CYP that has a major role in disposing of warfarin along with CYP3A4

A

CYP 2C9

42
Q

Energy (kcal/gm) in carbs, amino acids

A

4

43
Q

Energy (kcal/gm) in fats

A

9

44
Q

Energy (kcal/gm) in alcohol

A

7

45
Q

Subcellular location of ADH

A

cytoplasmic

46
Q

Subcellular location of ALDH

A

mitochondrial

47
Q

Enzyme that converts ethanol to acetaldehyde

A

ADH

48
Q

Enzyme that converts acetaldehyde to acetate

A

ALDH

49
Q

Vasodilator used to relieve the pain of angina due to insufficient oxygen supply to the heart

A

Nitroglycerin

50
Q

Enzyme responsible for the release of NO from nitroglycerin

A

ALDH

51
Q

Enzyme that catalyzes:
Acetate + ATP + CoASH → AcetylCoA + AMP

A

Acetyl CoA synthetase

52
Q

High levels of this in the cytoplasm from ethanol metabolism inhibit gluconeogenesis from lactate or glycerol

A

NADH

53
Q

High NADH in the mitochondria shifts the malate to OAA reaction towards this

A

Malate

54
Q

High levels of this in the mitochondria from ethanol metabolism increases ketogenesis and decreases gluconeogenesis from OAA

A

NADH

55
Q

AST and ALT ratio in alcoholism

A

AST > ALT

56
Q

AST and ALT ratio in viral hepatitis

A

ALT > AST

57
Q

Assay for thiamine in blood

A

Transketolase

Biochem (22 decks)

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