Critical
Itraconazole × Sirolimus
Antifungal, triazole×Selective immunosuppressant, mTOR inhibitor
Mechanism
Itraconazole is the strongest CYP3A4 inhibitor. Sirolimus rises 10+ fold. FDA Rapamune Section 4 contraindication.
Symptoms
Acute nephrotoxicity, hepatotoxicity, cytopenia.
Management
Combination contraindicated.
Check the full regimen, not just this pair
Opens the checker with these two drugs prefilled. Add the rest of the regimen and recompute additive risks.
Sources
- FDA: Sporanox (itraconazole) prescribing information – CYP3A4 inhibition contraindications (2020)– FDA Sporanox label, Contraindications §4 and Drug Interactions §7
- FDA: Rapamune (sirolimus) prescribing information – strong CYP3A4 inhibitor contraindications (2020)– FDA Rapamune label, Drug Interactions §7.2
- FDA: Rapamune (sirolimus) prescribing information (2017)