Drug interactions
Ketoconazole + Sirolimus
Severity: Contraindicated
Ketoconazole and Sirolimus: contraindicated interaction.
Last updated
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.
Summary
Ketoconazole markedly increases sirolimus blood concentrations, causing a risk of immunosuppressant toxicity such as myelosuppression, hyperlipidemia, infection and impaired wound healing. Labeling advises against the combination.
What this interaction means in plain words
Ketoconazole and Sirolimus are not normally used together. Taking them at the same time is expected to cause harm or make one of them unsafe, so a different medicine is usually chosen for one of the two.
Ketoconazole belongs to Anti Fungals; Sirolimus belongs to Miscellaneous.
Why it happens
Ketoconazole inhibits CYP3A4 and P-glycoprotein, reducing sirolimus metabolism and efflux.
What to do
Avoid concurrent use and choose an alternative antifungal, such as an echinocandin. If unavoidable, reduce the sirolimus dose substantially and monitor trough levels closely.
What to ask your pharmacist
- Is there an alternative to one of these two medicines for me?
- If both are essential, who is monitoring me and how often?
- Which symptoms mean I should stop and seek help straight away?
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Other interactions of Ketoconazole
- Alfuzosin + Ketoconazole Contraindicated
- Alprazolam + Ketoconazole Contraindicated
- Avanafil + Ketoconazole Contraindicated
- Conivaptan + Ketoconazole Contraindicated
- Dihydroergotamine intranasal + Ketoconazole Contraindicated
- Dihydroergotamine + Ketoconazole Contraindicated
Other interactions of Sirolimus
- Adenovirus types 4 and 7 live + Sirolimus Contraindicated
- Bcg vaccine live + Sirolimus Contraindicated
- Influenza virus vaccine quadrivalent intranasal + Sirolimus Contraindicated
- Levoketoconazole + Sirolimus Contraindicated
- Measles mumps and rubella vaccine live + Sirolimus Contraindicated
- Measles mumps and rubella vaccine + Sirolimus Contraindicated
Frequently asked questions
Can I take Ketoconazole with Sirolimus?
MediHelp rates the interaction as contraindicated. Ketoconazole and Sirolimus are not normally used together. Taking them at the same time is expected to cause harm or make one of them unsafe, so a different medicine is usually chosen for one of the two. Ketoconazole markedly increases sirolimus blood concentrations, causing a risk of immunosuppressant toxicity such as myelosuppression, hyperlipidemia, infection and impaired wound healing. Labeling advises against the combination.
How serious is the interaction between Ketoconazole and Sirolimus?
MediHelp rates it contraindicated, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid concurrent use and choose an alternative antifungal, such as an echinocandin. If unavoidable, reduce the sirolimus dose substantially and monitor trough levels closely.
What other medicines interact with Ketoconazole?
MediHelp also lists interactions of Ketoconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Ketoconazole page.
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