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Clinical Pharmacology > Drug Metabolism > Flashcards

Drug Metabolism Flashcards

1
Q

CYP1A2 Substrates

A

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

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2
Q

CYP1A2 Inhibitors

A

Amiodarone
Ciprofloxacin*
Cimetidine
Estrogens (HRT and OC)

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3
Q

CYP1A2 Inducers

A

Carbamazepine/phenytoin
Rifampin
Smoking
THC

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4
Q

CYP2C8 or 9 Substrates

A 
Carvedilol
Phenytoin
Pioglitazone
TCAs (amitriptyline, clomipramine, desipramine, imipramine)
Warfarin*
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5
Q

CYP2C8 or 9 Inhibitors

A 
Amiodarone
Gemfibrozil/fenofibrate
Fluconazole
Metronidazole
TMP-SMX
Clopidogrel
Valproate
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6
Q

CYP2C8 or 9 Inducers

A

Carbamazepine/Phenytoin
Rifampin
St John’s Wort

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7
Q

CYP2C19 Substrates

A 
Phenytoin
Citalopram
Clopidogrel
Most PPIs*
TCAs (normal 4)
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8
Q

CYP2C19 Inhibitors

A 
Fluconazole
Fluoxetine
Cimetidine
Gemfibrozil
Omeprazole/esomeprazole
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9
Q

CYP2C19 Inducers

A

Carbamazepine/Phenytoin
Rifampin
St John’s Wort

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10
Q

CYP2D6 Substrates

A 
Atypical antipsychotics (aripiprazole, risperidone)
Codeine*
SSRI (fluoxetine and paroxetine)
SNRI (duloxetine)
Metoprolol
TCAs
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11
Q

CYP2D6 Inhibitors

A

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

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12
Q

CYP2D6 Inducers

A

NONE*

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13
Q

CYP3A4 Substrates

A

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

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14
Q

CYP3A4 Inhibitors

A 
Amiodarone
Non-DHP CCBs (verapamil, diltiazem)
Cimetidine
Clarithromycin
Fluconazole
Grapefruit juice*
Protease inhibitors
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15
Q

CYP3A4 Inducers

A

Carbamazepine/Phenytoin
Rifampin
St John’s Wort

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16
Q

Phase I Reactions

A

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

17
Q

Phase II Reactions

A

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

18
Q

Factors affecting Cytochrome P450

A 
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
Q

Drugs with Narrow Therapeutic Windows

A 
Amiodarone
DOACs
Antipsychotics
Carbamazepine
Colchicine
Transplant meds
Statins
Levothyroxine
Oxycodone
Maybe CCBs
20
Q

Drugs and ETOH - Increase Sedation

A

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

21
Q

Drugs and ETOH - Increase intoxication

A

ETOH + varenicline

22
Q

Drugs and ETOH - Increase GI toxicity

A

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

23
Q

Drugs and ETOH - Increase hepatotoxicity

A

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

24
Q

Drugs and ETOH - Disulfuram rxn

A

ETOH + metronidazole or tinidazole

25
Q

Drugs and ETOH - Increase bleed risk

A

ETOH + anti-thrombotics (warfarin and DOACs)

26
Q

Drugs and ETOH - Severe hypertension

A

ETOH + MAOIs

27
Q

Drugs and ETOH - Severe hypotension

A

ETOH + alpha blockers, beta blockers, and CCBs

28
Q

PGP Subtrates

A 
Amiodarone
Atorvastatin/Simvastatin
Carbamazepine/Phenytoin
Dabigatran/Rivaroxaban
Digoxin
Diltiazem
Estrogen
Omeprazole
Paroxetine/Sertraline
Many chemotherapeutics
29
Q

PGP Inhibitors

A

Amiodarone
Carvedilol
Clarithromycin
Diltiazem/Verapamil

30
Q

PGP Inducers

A

Carbamazepine/Phenytoin
Dexamethasone
Rifampin
St. John’s Wort

Clinical Pharmacology (54 decks)

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