CYP Substrates, Inhibitors, Inducers and Key Transporters

NOT ALL EXAMPLES

NTI (3A4 enzymes)

Name the drugs

• Cyclosporine

• Quinidine

• Tacrolimus

Sensitive Substrate (3A4 enzymes)

Name the Drugs

• Simvastatin

• Lovastatin

• Carbamazepine

Strong Inhibitor (3A4 enzyme)

Name the Drugs

• Clarithromycin

• Itraconazole

• Ketoconazole

Moderate Inhibitor (3A4 enzyme)

Name the Drugs

• Fluconazole

• Verapamil

• Ciprofloxacin

• Grapefruit juice

Strong Inducer (3A4 enzyme)

Name the Drugs

• Carbamazepine

• Phenytoin

• St John’s Wort

Moderate Inducer (3A4 enzyme)

Name the Drugs

• modanifil

• Naficillin

• Bosentan

NTI (2D6 enzyme)

Name the Drugs

• only codeine

• DRUG WARNING FOR CODEINE ON LABEL

Sensitive Substrate (2D6 enzyme)

Name the Drugs

• metoprolol

• nebivolol

• venlafaxine

Strong Inhibitor (2D6 enzyme)

Name the Drugs

• Fluoxetine

• SSRIs

• Bupropion

Moderate Inhibitor (2D6 enzyme)

Name the Drugs

• Duloxetine

• Dronedarone

Weak Inhibitor (3A4 enzyme)

Name the Drugs

• Amiodarone

• Amlodipine (w/ more)

• Cimetidine

Weak Inhibitor (2D6 enzyme)

Name the Drugs

• Amiodarone

• Diltiazem

• Sertraline

NTI (2C9 enzyme)

Name the Drugs

• Warfarin

• Phenytoin

• IMPORTANT S-WARFARIN warning → NTI

Sensitive Substrate (2C9 enzyme)

Name the Drug

• celecoxib

Moderate Inhibitor (2C9 enzyme)

Name the Drugs

• Amiodarone

• Fluconazole

• fluoxetine

Weak Inhibitor (2C9 enzyme)

Name the Drug

• only fluvoxamine

Moderate Inducer (2C9 enzyme)

Name the Drugs

• carbamazepine

• rifampin

Genetic Polymorphs for 2C9

List considerations

• EM (wildtype/ common in pop.)

• PM (truncate protein and WT)

  • truncate protein → poor function hence PM

NTI (2C19 enzyme)

Name the Drug

• mephenytoin ONLY

Sensitive Substrate (2C19 enzyme)

Name the Drugs

• Omeprazole

• Lansoprazole

Strong Inhibitor (2C19 enzyme)

Name the Drugs

• Fluconazole

• Fluoxetine

• Ticlopidine

Moderate Inhibitors (2C19 enzyme)

Name the Drugs

• Felbamate

• Cannabidiol

Strong Inducer (2C19 enzyme)

Name the Drug

• Rifampin

Moderate Inducer (2C19 enzyme)

Name the Drugs

• Phenytoin

• Carbamazepine

Genetic Polymorphism Considerations (2C19 enzyme)

• EM

• PM (truncate protein and similar to WT)

• UM

NTI (2C8 enzyme)

Name the Drug

• Paclitaxel

Sensitive Substrate (2C8 enzyme)

Name the Drug

• Repaglinide

Strong Inhibitor (2C8 enzyme)

Name the Drugs

• Gemfibrozil

• Clopidogrel

Moderate Inducer (2C8 enzyme)

Name the Drug

• rifampin

Strong Inducer (2E1 enzyme)

Name the Drug

• ethanol

• Isoniazide

Sensitive Substrate (2B6 enzyme)

Name the Drug

• Bupropion

Strong Inhibitor (2B6 enzyme)

Name the Drug

• Ticlopidine

Strong Inducer (2B6 enzyme)

Name the Drugs

• Carbamazepine

• phenobarbital

Moderate Inducer (2B6 enzyme)

Name the Drugs

• Rifampin

• Efavirenz

NTI (1A2 enzyme)

Name the Drug

• Theophylline

• Tizanidine

Sensitive Substrate (1A2 enzyme)

Name the Drugs

• Duloxetine

• caffeine

Strong Inhibitor (1A2 enzyme)

Name the Drugs

• Fluvoxamine

• Ciprofloxacin