Drug interactions
Itraconazole + Sirolimus
Severity: Major
Itraconazole and Sirolimus: major interaction.
Last updated Sources: US FDA label
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
Itraconazole markedly increases sirolimus blood concentrations, which can cause immunosuppressant toxicity such as myelosuppression, hyperlipidemia, infections and impaired wound healing. The effect persists for some time after itraconazole is stopped.
What this interaction means in plain words
Itraconazole and Sirolimus can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.
Itraconazole belongs to Anti Fungals; Sirolimus belongs to Miscellaneous.
Why it happens
Itraconazole inhibits CYP3A4 and P-glycoprotein, reducing sirolimus metabolism and efflux.
What to do
Avoid the combination where possible. If it is necessary, reduce the sirolimus dose substantially and monitor trough levels closely during and after itraconazole therapy.
What to ask your pharmacist
- Does the benefit of taking both outweigh the risk in my case?
- Do I need any blood test, ECG or other check while on both?
- What early warning signs should I watch for, and what should I do if they appear?
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References
Other interactions of Itraconazole
- Alfuzosin + Itraconazole Contraindicated
- Alprazolam + Itraconazole Contraindicated
- Avanafil + Itraconazole Contraindicated
- Conivaptan + Itraconazole Contraindicated
- Dihydroergotamine intranasal + Itraconazole Contraindicated
- Dihydroergotamine + Itraconazole 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
- Ketoconazole + Sirolimus Contraindicated
- Levoketoconazole + Sirolimus Contraindicated
- Measles mumps and rubella vaccine live + Sirolimus Contraindicated
Frequently asked questions
Can I take Itraconazole with Sirolimus?
MediHelp rates the interaction as major. Itraconazole and Sirolimus can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Itraconazole markedly increases sirolimus blood concentrations, which can cause immunosuppressant toxicity such as myelosuppression, hyperlipidemia, infections and impaired wound healing. The effect persists for some time after itraconazole is stopped.
How serious is the interaction between Itraconazole and Sirolimus?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid the combination where possible. If it is necessary, reduce the sirolimus dose substantially and monitor trough levels closely during and after itraconazole therapy.
What other medicines interact with Itraconazole?
MediHelp also lists interactions of Itraconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Itraconazole page.
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