Drug interactions

ketoconazole + rifampin

For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.

Overview

Severity: Major · Evidence level: High

Rifampin markedly reduces ketoconazole exposure via enzyme induction, risking antifungal failure; both agents can injure the liver.

Mechanism of action

Rifampin is a strong inducer of CYP3A and P-gp → ↓ ketoconazole plasma concentrations; additive hepatotoxicity risk.

Clinical management

Avoid coadministration. Use an alternative antifungal not highly dependent on CYP3A or a non-rifampin regimen. If unavoidable, monitor for clinical failure and liver function tests closely.

Drug reference

References

  • Ketoconazole Tablets (Nizoral) Prescribing Information – Drug Interactions — FDA Label
  • Rifampin (Rifadin) Prescribing Information – Drug Interactions — FDA Label
  • Ketoconazole: Drug interactions — Lexicomp

Frequently asked questions

Can I take ketoconazole with rifampin?

The interaction is rated: Major. Rifampin markedly reduces ketoconazole exposure via enzyme induction, risking antifungal failure; both agents can injure the liver.

How serious is the interaction between ketoconazole and rifampin?

The interaction is rated: Major. Evidence level: High.

How is the interaction between ketoconazole and rifampin managed?

Avoid coadministration. Use an alternative antifungal not highly dependent on CYP3A or a non-rifampin regimen. If unavoidable, monitor for clinical failure and liver function tests closely.

Why do ketoconazole and rifampin interact?

Rifampin is a strong inducer of CYP3A and P-gp → ↓ ketoconazole plasma concentrations; additive hepatotoxicity risk.

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