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Flashcards in Drug Metabolism Deck (30)
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1

CYP1A2 Substrates

TCAs (amitriptyline, clomipramine, desipramine, imipramine)
Duloxetine
Theophylline

2

CYP1A2 Inhibitors

Amiodarone
Ciprofloxacin*
Cimetidine
Estrogens (HRT and OC)

3

CYP1A2 Inducers

Carbamazepine/phenytoin
Rifampin
Smoking
THC

4

CYP2C8 or 9 Substrates

Carvedilol
Phenytoin
Pioglitazone
TCAs (amitriptyline, clomipramine, desipramine, imipramine)
Warfarin*

5

CYP2C8 or 9 Inhibitors

Amiodarone
Gemfibrozil/fenofibrate
Fluconazole
Metronidazole
TMP-SMX
Clopidogrel
Valproate

6

CYP2C8 or 9 Inducers

Carbamazepine/Phenytoin
Rifampin
St John's Wort

7

CYP2C19 Substrates

Phenytoin
Citalopram
Clopidogrel
Most PPIs*
TCAs (normal 4)

8

CYP2C19 Inhibitors

Fluconazole
Fluoxetine
Cimetidine
Gemfibrozil
Omeprazole/esomeprazole

9

CYP2C19 Inducers

Carbamazepine/Phenytoin
Rifampin
St John's Wort

10

CYP2D6 Substrates

Atypical antipsychotics (aripiprazole, risperidone)
Codeine*
SSRI (fluoxetine and paroxetine)
SNRI (duloxetine)
Metoprolol
TCAs

11

CYP2D6 Inhibitors

Amiodarone
Antidepressants (fluoxetine, sertraline, paroxetine, duloxetine, bupropion)
Cimetidine

12

CYP2D6 Inducers

NONE*

13

CYP3A4 Substrates

DOACs (apixaban/rivaroxaban), Amiodarone, Atorvastatin/Simvastatin, BZDs, Carbamazepine, CCBs (amlodipine, verapamil, diltiazem), Clarithromycin,
Cyclosporine/tacrolimus/ sirolimus, Estrogens, Protease inhibitors, PDE5 inhibitors, OCPs, Opioids, SSRIs (citalopram, paroxetine, sertraline), Theophylline

14

CYP3A4 Inhibitors

Amiodarone
Non-DHP CCBs (verapamil, diltiazem)
Cimetidine
Clarithromycin
Fluconazole
Grapefruit juice*
Protease inhibitors

15

CYP3A4 Inducers

Carbamazepine/Phenytoin
Rifampin
St John's Wort

16

Phase I Reactions

Polar groups are added to the lipophilic parent compounds by oxidation, reduction, or hydrolysis to facilitate water-solubility

17

Phase II Reactions

Glucuronic acid (glucuronidation)
Sulfate (sulfation)
Acetate (acetylation)
Methyl group (methylation)

18

Factors affecting Cytochrome P450

Enzyme
Diet (grapefruit inhibits CYP3A, chronic ETOH increases CYP2E1 and decreases glutathione levels)
Other drugs (especially with Narrow TI)
Age
Genetics
Underlying liver disease

19

Drugs with Narrow Therapeutic Windows

Amiodarone
DOACs
Antipsychotics
Carbamazepine
Colchicine
Transplant meds
Statins
Levothyroxine
Oxycodone
Maybe CCBs

20

Drugs and ETOH - Increase Sedation

ETOH + opioids, BZDs, NBRAs, TCAs, 1st gen antihistamines, antipsychotics, and muscle relaxants

21

Drugs and ETOH - Increase intoxication

ETOH + varenicline

22

Drugs and ETOH - Increase GI toxicity

ETOH (3 or more days) + NSAIDs, systemic steroids

23

Drugs and ETOH - Increase hepatotoxicity

ETOH (3 or more days) + INH, MTX, APAP

24

Drugs and ETOH - Disulfuram rxn

ETOH + metronidazole or tinidazole

25

Drugs and ETOH - Increase bleed risk

ETOH + anti-thrombotics (warfarin and DOACs)

26

Drugs and ETOH - Severe hypertension

ETOH + MAOIs

27

Drugs and ETOH - Severe hypotension

ETOH + alpha blockers, beta blockers, and CCBs

28

PGP Subtrates

Amiodarone
Atorvastatin/Simvastatin
Carbamazepine/Phenytoin
Dabigatran/Rivaroxaban
Digoxin
Diltiazem
Estrogen
Omeprazole
Paroxetine/Sertraline
Many chemotherapeutics

29

PGP Inhibitors

Amiodarone
Carvedilol
Clarithromycin
Diltiazem/Verapamil

30

PGP Inducers

Carbamazepine/Phenytoin
Dexamethasone
Rifampin
St. John's Wort