Ketoconazole and Rifabutin interaction
Ketoconazole and Rifabutin: both prescribing labels flag this combination with the strongest language, such as a contraindication, a boxed warning, or an instruction to avoid it.
Do not combine without a prescriber's guidance. The label language below is the strongest FDA uses.
What the FDA labels say
From the Ketoconazole label · effective 2026-07-07
Therefore, administration of potent enzyme inducers of CYP3A4 with ketoconazole tablets is not recommended.
Examples include: Antibacterials: isoniazid, rifabutin (see also under 'Drugs that may have their plasma concentrations increased'), rifampicin.
Antibacterials rifabutin telithromycin Rifabutin: see also under Drugs that may decrease ketoconazole plasma concentrations.
Coadministration of ketoconazole tablets with potent enzyme inducers of CYP3A4 may decrease the bioavailability of ketoconazole to such an extent that efficacy may be reduced.
From the Rifabutin label · effective 2026-09-01
Effect of Other Drugs on Rifabutin Pharmacokinetics Some drugs that inhibit CYP3A may significantly increase the plasma concentration of rifabutin.
Therefore, carefully monitor for rifabutin associated adverse events in those patients also receiving CYP3A inhibitors, which include fluconazole and clarithromycin.
In some cases, the dosage of rifabutin may need to be reduced when it is co-administered with CYP3A inhibitors.
ANTIFUNGALS Fluconazole 200 mg once a day for 2 weeks 300 mg once a day for 2 weeks HIV-infected patients (12) ↑ AUC by 82%, ↑ C max by 88% ↔ Monitor for rifabutin associated adverse events.
Antiretroviral and Anti-HCV Drug Interactions Protease inhibitors act as substrates or inhibitors of CYP3A4 mediated metabolism.
Taking more than these two? Interactions stack. Check your whole list at once; it stays in your browser.
Open in the checkerNot medical advice. Interaction Checker quotes FDA label text and NIH fact sheets. Whether an interaction matters for you depends on doses, timing, kidney and liver function, and other conditions. Confirm with a pharmacist or prescriber.