Ketoconazole and Midazolam interaction

Ketoconazole and Midazolam: both prescribing labels flag this combination with the strongest language, such as a contraindication, a boxed warning, or an instruction to avoid it.

Major

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

Major

…contraindicated with ketoconazole tablets: methadone, disopyramide, dronedarone, ergot alkaloids such as dihydroergotamine, ergometrine, ergotamine, methylergometrine, irinotecan, lurasidone, oral midazolam, alprazolam, triazolam, felodipine, nisoldipine, ranolazine, tolvaptan, eplerenone, lovastatin, simvastatin and colchicine (see PRECAUTIONS: Drug Interactions ).

Contraindicationsnames MidazolamView label on DailyMed
Major

Enhanced Sedation Coadministration of ketoconazole tablets with oral midazolam, oral triazolam or alprazolam has resulted in elevated plasma concentrations of these drugs.

Contraindicationsnames MidazolamView label on DailyMed
Major

Concomitant administration of ketoconazole tablets with oral triazolam, oral midazolam or alprazolam is contraindicated (see PRECAUTIONS: Drug Interactions ).

Contraindicationsnames MidazolamView label on DailyMed
Major

This may potentiate and prolong hypnotic and sedative effects, especially with repeated dosing or chronic administration of these agents.

Contraindicationsby drug classView label on DailyMed
Major

…methadone when coadministered with ketoconazole tablets may increase the risk of serious cardiovascular events including QT prolongation and torsade de pointes, or respiratory or CNS depression [See CONTRAINDICATIONS .] Fentanyl: The potential increase in plasma concentrations of fentanyl when coadministered with ketoconazole tablets may increase the risk of…

Drug interactionsby drug classView label on DailyMed

From the Midazolam (Midazolam in Sodium Chloride) label · effective 2025-07-31

Moderate

Cytochrome P450-3A4 Inhibitors : May result in prolonged sedation due to decreased plasma clearance of midazolam.

Drug interactionsby drug classView label on DailyMed
Moderate

Cytochrome P450-3A4 Inhibitors Concomitant administration with drugs that are known to inhibit the P450-3A4 enzyme system, such as cimetidine (not ranitidine), erythromycin, diltiazem, verapamil, ketoconazole and itraconazole, may result in prolonged sedation due to a decrease in plasma clearance of midazolam.

Drug interactionsby drug classView label on DailyMed

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Not 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.