MAJOR — Use With Caution
FDA-documented interaction. Tacrolimus dose reduction typically needed. Frequent tacrolimus level and renal function monitoring required.
Evidence level: STRONG
Fluconazole (Diflucan) can dramatically increase tacrolimus (Prograf) levels in your blood. Since tacrolimus has a very narrow safety margin and can damage kidneys, this is a dangerous combination that requires close monitoring.
Fluconazole inhibits CYP3A4 and CYP2C9. Tacrolimus is primarily metabolized by CYP3A4. Fluconazole significantly increases tacrolimus levels, risking nephrotoxicity. FDA tacrolimus label warns about azole antifungals.
If you take tacrolimus (an anti-rejection medication) and need fluconazole, your doctor should reduce your tacrolimus dose and check blood levels frequently. Report any changes in urination or kidney pain.
Take Fluconazole as directed (some require food for absorption, others an empty stomach — check the label). Azole antifungals are potent CYP enzyme inhibitors that can dramatically increase blood levels of many medications. Tacrolimus levels should be monitored during antifungal treatment.
Higher risk for: those with liver impairment (azole antifungals are hepatotoxic), concurrent CYP3A4 substrate use, elderly, renal impairment, or those on multiple QT-prolonging medications.
Decreased urination, swelling in hands/feet, tremor, headache, nausea, confusion, high blood pressure, elevated creatinine (found on blood tests)
Request tacrolimus level monitoring within 3-5 days of starting fluconazole. Plan preemptive dose reduction. Monitor renal function (creatinine, BUN).
Azole antifungals are potent CYP enzyme inhibitors. Ask your doctor about topical antifungal options to avoid systemic interactions, or about terbinafine which has fewer drug interactions than azoles.
Fluconazole (Diflucan) can dramatically increase tacrolimus (Prograf) levels in your blood. Since tacrolimus has a very narrow safety margin and can damage kidneys, this is a dangerous combination that requires close monitoring.
Take Fluconazole as directed (some require food for absorption, others an empty stomach — check the label). Azole antifungals are potent CYP enzyme inhibitors that can dramatically increase blood levels of many medications. Tacrolimus levels should be monitored during antifungal treatment.
Decreased urination, swelling in hands/feet, tremor, headache, nausea, confusion, high blood pressure, elevated creatinine (found on blood tests)
Azole antifungals are potent CYP enzyme inhibitors. Ask your doctor about topical antifungal options to avoid systemic interactions, or about terbinafine which has fewer drug interactions than azoles.
Request tacrolimus level monitoring within 3-5 days of starting fluconazole. Plan preemptive dose reduction. Monitor renal function (creatinine, BUN).
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