Metabolism

Question 1

Where within hepatic cells are CYP enzymes located?

Answer 1

Endoplasmic reticulum
Nucleus
Mitochondria
Cytoplasm

Question 2

How is ibuprofen metabolized?

Answer 2

Aliphatic hydroxylation by CYP2C9

Question 3

How is pentobarbital metabolized?

Answer 3

Aliphatic hydroxylation by CYP

Question 4

How is cyclosporine metabolized?

Answer 4

Aliphatic hydroxylation by CYP

Question 5

How is phenytoin metabolized?

Answer 5

Aromatic hydroxylation by CYP2C9

Question 6

How is propanolol metabolized?

Answer 6

Aromatic hydroxylation by CYP2C19

Question 7

How are steroid hormones metabolized?

Answer 7

Aromatic hydroxylation by CYP

Question 8

How is imipramine metabolized?

Answer 8

N-Dealkylation by CYP

Question 9

How is diazepam metabolized?

Answer 9

N-Dealkylation by CYP2C19, CYP3A4

Question 10

How is codeine metabolized?

Answer 10

N-Dealkylation by CYP2D6

Question 11

How is morphine metabolized?

Answer 11

N-Dealkylation by CYP

Question 12

How is tamoxifen metabolized?

Answer 12

N-Dealkylation by CYP

Question 13

How is caffeine metabolized?

Answer 13

N-Dealkylation by CYP1A2

Question 14

How is chlorpromazine metabolized?

Answer 14

S-Oxidation by CYP

Question 15

How is cimetidine metabolized?

Answer 15

S-Oxidation by CYP

Question 16

How is chlorpheniramine metabolized?

Answer 16

N-Oxidation by CYP

Question 17

How is trimethylamine metabolized?

Answer 17

N-Oxidation by CYP

Question 18

In which tissues are CYP active?

Answer 18

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

Question 19

Which enzyme metabolizes acetaminophen?

Answer 19

CYP1A2, CYP2E1

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

Question 20

Which enzyme metabolizes theophylline?

Answer 20

CYP1A2

Question 21

Which enzyme metabolizes warfarin (Coumadin, Coumarin)?

Answer 21

CYP1A2, CYP2A6, CYP2C9 (S-warfarin)

Question 22

Which enzyme metabolizes zidovudine (azidothymidine, AZT)?

Answer 22

CYP2A6

Question 23

Which enzyme metabolizes hexobarbital?

Answer 23

CYP2C9

Question 24

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

Answer 24

CYP2C19

Question 25

Which enzyme metabolizes amitriptyline (and other tricyclic antidepressants)?

Answer 25

CYP2D6

Question 26

Which enzyme metabolizes fluoxetine (Prozac and other SSRIs)?

Answer 26

CYP2D6

Question 27

Which enzyme metabolizes timolol?

Answer 27

CYP2D6

Question 28

Which enzyme metabolizes hydrocodone?

Answer 28

CYP2D6

Question 29

Which enzyme metabolizes ethanol?

Answer 29

CYP2E1, alcohol dehydrogenase | ethanol upregulates CYP2E1

Question 30

Which enzyme metabolizes testosterone?

Answer 30

CYP3A4

Question 31

Which enzyme metabolizes progesterone?

Answer 31

CYP3A4

Question 32

Which enzyme metabolizes cortisol?

Answer 32

CYP3A4

Question 33

Which enzyme metabolizes nifedipine?

Answer 33

CYP3A4

Question 34

Which enzyme metabolizes diltiazem?

Answer 34

CYP3A4

Question 35

Which enzyme metabolizes verapamil?

Answer 35

CYP3A4

Question 36

Which enzyme metabolizes triazolam?

Answer 36

CYP3A4

Question 37

Which enzyme metabolizes amiodarone?

Answer 37

CYP3A4

Question 38

Which enzyme metabolizes erythromycin?

Answer 38

CYP3A4

Question 39

How is aspirin metabolized?

Answer 39

Hydrolysis of ester group

Question 40

What major classes of drugs are metabolized by CYP3A4?

Answer 40

``` Steroids Calcium channel blockers Benzodiazepines Amiodarone Erythromycin ```

Question 41

Which drugs are activated by synthetic reactions?

Answer 41

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

Question 42

What factors modify drug metabolism?

Answer 42

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