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Med Chem Test 4 > Drug Metabolism and FGs > Flashcards

Drug Metabolism and FGs Flashcards

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1
Q

What are the phase 1 functionallizations?

A

Oxidation
Reduction
Hydrolysis

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2
Q

What are the phase 2 conjugations?

A 
Glucuronidation
Sulfation
AA conjugation
Glutathione conjugation
Acetylation
Methylation
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3
Q

What drug metabolism occurs on alkanes?

A

Nonreactive in vivo and excreted unchanged.

There are exceptions, and when it happens, it usually involves CYP450 oxidation.

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4
Q

What drug metabolism occurs on alkenes?

A

Metabolically stable.

But there are exceptions (epoxides, reduction, hydration, and peroxidation)

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5
Q

What drug metabolism occurs on Aromatic HCs?

A

Prone to aromatic hydroxylation
Some reactive epoxide intermediates (potential carcinogens) have been isolated
In most cases epoxides rearrange to OH products.

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6
Q

What drug metabolism occurs on aromatic HCs that are benzenes?

A

In cases where no-epoxide rearrangement occurs, the epoxide can undergo hydrolysis via EH.

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7
Q

What drug metabolism occurs on aromatic hydrocarbon’s OH metabolite?

A

It can now undergo phase II metabolism. (ex: Glucuronidation & Sulfation)

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8
Q

What drug metabolism occurs on halogenated HCs(HHCs)?

A

Are stable in vivo and not readily metabolized
Are very lipophilic, not readily metabolized to hydrophilic compounds.
They have prolonged half life which increases their potential for toxicity (hepatotoxicity)for some HHCs

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9
Q

What drug metabolism occurs on alcohols?

A

Although, stable in vivo, can undergo phase 1 oxidations and phase II metabolism.

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10
Q

What drug metabolism occurs on phenols?

A

Behave like alcohols in vivo:

Although, stable in vivo, can undergo phase 1 oxidations and phase II metabolism.

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11
Q

What drug metabolism occurs on ethers?

A

Most are excreted unchanged

Althouth, O-dealkylations (methyl and ethyl groups)

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12
Q

What drug metabolism occurs on thioether or sulfide?

A

Undergo oxidative biotransformations.

S-Oxidations & Dealkylations

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13
Q

What drug metabolism occurs on aldehydes & ketones?

A

Undergo non-CYP450 oxidative biotransformations

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14
Q

What drug metabolism occurs on tertiary and secondary amines?

A

secondary and tertiary amines bearing small alkyl groups (M,E,P) undergo N-dealkylations

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15
Q

What drug metabolism occurs on primary amines?

A

deaminations and in some cases N-methylation

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16
Q

What drug metabolism occurs on benzillic amines?

A

Undergo phase II biotransformations

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17
Q

What drug metabolism occurs on carboxylic acids?

A 
Undergo a variety of biotransformations:
B-C-oxidation
Glutamine
Glycine
Glucuronic acid
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18
Q

What types of esters does drug metabolism occur on?

A

carboxylic acid esters
nitrate esters
phosphate esters
sulfate esters

19
Q

What drug metabolism occurs on carboxylic acid esters?

A

They undergo carboxyesterase mediated hydrolytic biotransformations.

20
Q

What drug metabolism occurs on nitrate esters?

A

metabolic biotransformations are still being investigated.

This is a lipophilic FG

21
Q

What drug metabolism occurs on phosphate esters?

A

They undergo phosphatase hydrolytic biotransformations.

22
Q

What are present drugs that undergo phosphatase hydrolytic biotransformations?

A 
Phosphenytoin
Prednisolone phosphate
ATP
DNA
RNA
23
Q

What drug metabolism occurs on sulfate esters?

A

They undergo hydrolytic biotransformations

24
Q

What drug metabolism occurs on amides?

A

Undergo hydrolytic biotransformations, but are more stable in vivo than esters.
Amidases
Beta-lactamase hydrolysis

25
Q

What drug metabolism occurs on carbonates?

A

Carbonates undergo esterase hydrolytic biotransformations to alcohols.

26
Q

What drug metabolism occurs on carbamates?

A

Carbamates are coverted by hydrolytic biotransformations to alcohols and amines.

27
Q

What drug metabolism occurs on heterocycles(epoxide)?

A

Epoxide metabolism can be hydrolyzed by EHs.

28
Q

What drug metabolism occurs on heterocycles(Pyrimidines)?

A

Are deactivated by DPD(Dihydropyrimidine Reductase)

29
Q

What is important about DPD?

A

It exhibits genetic variations that may cause genetic deficiency in patients.

30
Q

What is 5-Fu?

A

It is a cytotoxic uracil pyrimidine derivative.

It relies on Uracil metabolic pathway for activation to inhibit DNA synthesis.

31
Q

What is the rate limiting enzyme for Uracil and 5-Fu activation?

A

Orotate Phosphoribotransferase (OPRT)

32
Q

How much of 5-FU does is deactivated by DPD?

A

80%

33
Q

What functional groups are involved in the phase II drug metabolism of glucuronide?

A

alcohols
carboxylic acids
amides
thiols

34
Q

What enzyme is involved in glucuronide drug metabolism?

A

UDP-glucuronosyl transferases

35
Q

What functional groups are involved in the phase II drug metabolism of sulfate?

A

alcohols

amines

36
Q

What enzyme is involved in sulfate drug metabolism?

A

Sulfotransferases

37
Q

What functional groups are involved in the phase II drug metabolism of amino acid (glycine/glutamine)?

A

carboxylic acids

38
Q

What enzyme is involved in amino acid drug metabolism?

A

Acyl-CoA synthatases/N-acyltransferases

39
Q

What functional groups are involved in the phase II drug metabolism of glutathione?

A

Aromatic Halides
Arene oxide
Epoxide

40
Q

What enzyme is involved in glutathione drug metabolism?

A

Glutathione S-transferases

41
Q

What functional groups are involved in the phase II drug metabolism of acetyl?

A

alcohols

amines

42
Q

What enzyme is involved in acetyl drug metabolism?

A

Acetyltransferases

43
Q

What functional groups are involved in the phase II drug metabolism of methyl?

A

alcohols
amines
thiols
heterocyclic amines

44
Q

What enzyme is involved in acetyl drug metabolism?

A

methyltransferases

Med Chem Test 4 (6 decks)

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