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Med Chem Test 3 > Drug Metabolism Pathways (DM13) > Flashcards

Drug Metabolism Pathways (DM13) Flashcards

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1
Q 
All of the following are correct attributes of DM and DMEs, except:
A.  Xenobiotic inactivation
B. Microsomal activity
C. Hepatocyte inactivity
D. Nuclear receptor activation
A

C. Hepatocyte inactivity

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2
Q

Phase 1 pathways include what enzymes?

A 
CYP450 & Non-CYP450
ADH
ALDH
XO
MAO
FMO
Azo-reductase
Nitro-reductase
cytosolic enzymes
EH
3A4
Carboxyesterases
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3
Q

Phase 1 pathways include what reactions?

A

Oxidations (Use CYP450 & Non-CYP450)
Reductions
Hydrolytic

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4
Q

Phase 1 reactions are functionalization meaning?

A

New FGs are introduced or existing FGs are modified or exposed in readiness for excretion or conjugation.

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5
Q

What are the types of reactions included in CYP450 oxidative reactions?

A

Aliphatic, allylic & benzylic carbons
Aromatic groups
Heteroatom systems (N-dealkylation, N-oxidation, O-dealkylation, S-dealkylation, Oxidative deamination_
Dehalogenation
Epoxidation

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6
Q

What are the types of Non-CYP450 oxidations?

A

ADH, ALDH, Xanthine oxidase, MAO, FMO

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7
Q

What are the types of reductive reactions?

A

Azo, Nitro, Miscellaneous reductive reactions

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8
Q

What are the types of hydrolytic reactions?

A

Esters, Amides, Epxoides

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9
Q 
\_\_\_\_\_\_\_\_ are the only exception to the commonly encountered reactions of the phase I type.
A.  Bond reductions
B. Bond hydrolysis
C.  O-atom additions
D. N-atom additions
A

D. N-atom additions

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10
Q

What does Alcohol Dehydrogenase (ADH) do and what pathway is it part of?

A

It changes primary alcohols to aldehydes in the liver. It is part of the Non-CYP450 Oxidations.

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11
Q

What type of specific enzyme is ADH and ALDH?

A

NAD

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12
Q

What does Aldehyde Dehydrogenase (ALDH) do and what pathway is it part of?

A

It changes aldehydes to Carboxylic acids in the liver (mitochondrial). It is part of the Non-CYP450 Oxidations.

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13
Q

What does Xanthine Oxidase/Dehydrogenase or Xanthine Oxidoreductase do?

A

Purine metabolism in the liver and intestine.

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14
Q

What is the cofactor of Monoamine oxidase (MAO)?

A

Flavin Adenosine Dinucleotide (FAD)

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15
Q

What does MAO do?

A

Neurotransmitter metabolism in the mitochondiral

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16
Q

What does Flavin-containing Monooxygenase (FMO) do?

A

Uses reduced flavin to activate molecular oxygen in microsomal.

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17
Q

What does FMO require?

A

FMN(flavin mononucleotide) reductase

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18
Q

What does FMO oxidate?

A

amines & thiols (3 amines and amides from N-oxides)
1 & 2 amines form hydroxylamines
thiols form sulfoxides and sulfones

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19
Q

Azo-reductase is what type of reaction?

A

Reduction reaction in intestinal microflora

20
Q

What miscellaneous reductions occur by cytosolic enzymes?

A

Disulfirm to Diethyldithiocarbamic Acid

Dimethylsulfoxide to Dimethylsulfide

21
Q

In hydrolytic reactions epoxide hydrolysis occurs by what enzyme?

A

Epoxide hydrolases (EH)

22
Q

In hydrolysis reactions ester hydrolysis and amide hydrolysis occurs by what enzyme?

A

Carboxyesterases

23
Q 
What enzyme is not a member of the phase I family?
A. 3A4
B. NAT
C. FMO
D. EH
E. MAO
A

B. NAT

24
Q

What are the phase 2 pathways?

A

Conjugation or synthesis
utilize existing Functional Groups
Most increase polarity for urinary excretion
Other decrease polarity
Catalyzed by enzymes known as transferases
Require an endogenous cofactor

25
Q

What are the phase 2 reactions?

A 
Glucuronidation 
Sulfation
Glutathione Conjugation
Acetylation
Amino Acid Conjugation
Methylation
26
Q

What is the enzyme for glucuronidation?

A

UGT (Uridine diphosphate glucuronosyl transferase)

27
Q

What is the enzyme for sulfation?

A

SULT (Sulfotransferase)

28
Q

What is the enzyme for Glutathione Conjugation?

A

GST (Glutathione S-transferase)

29
Q

What is the enzyme for Acetylation?

A

NAT (N-ACetyltransferase)

30
Q

What is the enzyme for Amino acid conjugation?

A

Acylsnthatase

31
Q

What is the enzyme for Methylation?

A

Methyltransferase (FG specific COMT, TPMT, PNMT, HMT)

32
Q

What are the substrates of Glucuronidation?

A 
Alcohols & Phenols
Carboxylic Acids
Aromatic Amines
Thiols
Bilirubin
33
Q

What are the substrates of Sulfotransferases?

A

Phenols, Alcohols, and Aromatic amines

34
Q

What is the cofactor of UGT?

A

UDPGA

35
Q

What is the cofactor of ST or SULTs?

A

PAPS

36
Q

What is the cofactor of GST?

A

GSH

37
Q

What are the target FGs of Glutathione S-transferase?

A

Electrophilic centers: Halides, Epoxides, and other electrophiles.

38
Q

What are the target FGs of Acetylation?

A

Amine, Hydrazines, and Sulfonamides.

39
Q

What is the cofactor of NAT?

A

Acetyl-CoA

40
Q

In amino acid conjugation Acyl Synthetase requires what to activate the target FG?

A

Acetyl Coenzyme A

41
Q

What are the target FGs of Acyl Synthetase?

A

Aromatic COOH, Aliphatic COOH, Heterocyclic COOH.

42
Q

What are the target FGs of Methyl transferases?

A

OH, -NH2, Heterocyclic-N, -SH

43
Q

What is the cofactor of methyl transferases?

A

SAM

44
Q

What are the NAD specific enzymes?

A

ADH & ALDH

45
Q

What is the cofactor for MAO reactions?

A

Flavin Adenosine Dinucleotide (FAD)

46
Q

What are the reduction reaction’s enzymes?

A

Azo-reductase
Nitro-reductase
Miscellaneous reductions by cytosolic enzymes

47
Q

What are the hydrolytic reactions?

A

Epoxide hydrolysis
Ester hydrolysis
Amide hydrolysis

Med Chem Test 3 (5 decks)

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