Metabolism Flashcards

1
Q

Where within hepatic cells are CYP enzymes located?

A

Endoplasmic reticulum
Nucleus
Mitochondria
Cytoplasm

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2
Q

How is ibuprofen metabolized?

A

Aliphatic hydroxylation by CYP2C9

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3
Q

How is pentobarbital metabolized?

A

Aliphatic hydroxylation by CYP

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4
Q

How is cyclosporine metabolized?

A

Aliphatic hydroxylation by CYP

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5
Q

How is phenytoin metabolized?

A

Aromatic hydroxylation by CYP2C9

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6
Q

How is propanolol metabolized?

A

Aromatic hydroxylation by CYP2C19

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7
Q

How are steroid hormones metabolized?

A

Aromatic hydroxylation by CYP

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8
Q

How is imipramine metabolized?

A

N-Dealkylation by CYP

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9
Q

How is diazepam metabolized?

A

N-Dealkylation by CYP2C19, CYP3A4

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10
Q

How is codeine metabolized?

A

N-Dealkylation by CYP2D6

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11
Q

How is morphine metabolized?

A

N-Dealkylation by CYP

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12
Q

How is tamoxifen metabolized?

A

N-Dealkylation by CYP

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13
Q

How is caffeine metabolized?

A

N-Dealkylation by CYP1A2

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14
Q

How is chlorpromazine metabolized?

A

S-Oxidation by CYP

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15
Q

How is cimetidine metabolized?

A

S-Oxidation by CYP

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16
Q

How is chlorpheniramine metabolized?

A

N-Oxidation by CYP

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17
Q

How is trimethylamine metabolized?

A

N-Oxidation by CYP

18
Q

In which tissues are CYP active?

A
Liver (smooth ER)
Gut (intestinal wall)
Brain
Lung
Placenta
Skin
19
Q

Which enzyme metabolizes acetaminophen?

A

CYP1A2, CYP2E1

CYP2E1 is upregulated by ethanol; the metabolite is toxic and can cause liver damage, necrosis, hepatic failure

20
Q

Which enzyme metabolizes theophylline?

A

CYP1A2

21
Q

Which enzyme metabolizes warfarin (Coumadin, Coumarin)?

A

CYP1A2, CYP2A6, CYP2C9 (S-warfarin)

22
Q

Which enzyme metabolizes zidovudine (azidothymidine, AZT)?

A

CYP2A6

23
Q

Which enzyme metabolizes hexobarbital?

A

CYP2C9

24
Q

Which enzyme metabolizes omeprazole (and other proton pump inhibitors)?

A

CYP2C19

25
Q

Which enzyme metabolizes amitriptyline (and other tricyclic antidepressants)?

A

CYP2D6

26
Q

Which enzyme metabolizes fluoxetine (Prozac and other SSRIs)?

A

CYP2D6

27
Q

Which enzyme metabolizes timolol?

A

CYP2D6

28
Q

Which enzyme metabolizes hydrocodone?

A

CYP2D6

29
Q

Which enzyme metabolizes ethanol?

A

CYP2E1, alcohol dehydrogenase

ethanol upregulates CYP2E1

30
Q

Which enzyme metabolizes testosterone?

A

CYP3A4

31
Q

Which enzyme metabolizes progesterone?

A

CYP3A4

32
Q

Which enzyme metabolizes cortisol?

A

CYP3A4

33
Q

Which enzyme metabolizes nifedipine?

A

CYP3A4

34
Q

Which enzyme metabolizes diltiazem?

A

CYP3A4

35
Q

Which enzyme metabolizes verapamil?

A

CYP3A4

36
Q

Which enzyme metabolizes triazolam?

A

CYP3A4

37
Q

Which enzyme metabolizes amiodarone?

A

CYP3A4

38
Q

Which enzyme metabolizes erythromycin?

A

CYP3A4

39
Q

How is aspirin metabolized?

A

Hydrolysis of ester group

40
Q

What major classes of drugs are metabolized by CYP3A4?

A
Steroids
Calcium channel blockers
Benzodiazepines
Amiodarone
Erythromycin
41
Q

Which drugs are activated by synthetic reactions?

A

morphine –> morphine-6-glucuronide (morphine-3-glucuronide is not active)
minoxidil –> minoxidil sulfate

42
Q

What factors modify drug metabolism?

A
Enzyme saturation
Enzyme co-factor availability
Drug-drug interactions
Age
Nutrition
Concurrent disease
Genetic variability (pharmacogenetics)