Examples of CYP3A4 Inhibitors (Categorized by Strength)
Strong Inhibitors
These cause a ≥5-fold increase in the blood levels of substrate drugs.
- Antiretrovirals: Ritonavir , cobicistat (another booster, found in Stribild, Genvoya).
- Antifungals: Ketoconazole, itraconazole, voriconazole, posaconazole.
- Antibiotics: Clarithromycin, telithromycin.
- Protease Inhibitors (for HCV): Boceprevir, telaprevir.
- Others: Nefazodone, conivaptan.
Moderate Inhibitors
These cause a 2 to <5-fold increase in substrate drug levels.
- Antifungals: Fluconazole, isavuconazole.
- Cardiovascular: Diltiazem, verapamil.
- Antibiotics: Erythromycin.
- Food: Grapefruit juice and Seville oranges (bergamottin is the inhibiting compound).
- Others: Ciprofloxacin, cimetidine, cyclosporine, imatinib.
Weak Inhibitors
These cause a 1.25 to 2-fold increase in substrate drug levels.
- Many common drugs fall here, including amlodipine, ranolazine, and others. While “weak,” they can still be significant when combined with a narrow therapeutic index drug.
From the strong inhibitor list, I am going to have trouble getting a script from a local doctor…