Drug interactions
Fluconazole + Macitentan
Severity: Major
Fluconazole and Macitentan: 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
Fluconazole inhibits both CYP3A4 and CYP2C9, which contribute to macitentan clearance, and is predicted to increase exposure considerably. This raises the risk of adverse effects such as anemia, edema and hepatotoxicity.
What this interaction means in plain words
Fluconazole and Macitentan 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.
Fluconazole belongs to Anti Fungals; Macitentan belongs to Cardiovascular.
Why it happens
Dual CYP3A4 and CYP2C9 inhibition by fluconazole reduces macitentan metabolism.
What to do
Avoid the combination if possible; if unavoidable, monitor hemoglobin, liver tests and fluid status.
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 Macitentan
- Amiodarone + Macitentan Major
- Apalutamide + Macitentan Major
- Bosentan + Macitentan Major
- Carbamazepine + Macitentan Major
- Clarithromycin + Macitentan Major
- Efavirenz + Macitentan Major
Other interactions of Fluconazole
- Dihydroergotamine intranasal + Fluconazole Contraindicated
- Dihydroergotamine + Fluconazole Contraindicated
- Dofetilide + Fluconazole Contraindicated
- Domperidone + Fluconazole Contraindicated
- Dronedarone + Fluconazole Contraindicated
- Erythromycin + Fluconazole Contraindicated
Frequently asked questions
Can I take Fluconazole with Macitentan?
MediHelp rates the interaction as major. Fluconazole and Macitentan 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. Fluconazole inhibits both CYP3A4 and CYP2C9, which contribute to macitentan clearance, and is predicted to increase exposure considerably. This raises the risk of adverse effects such as anemia, edema and hepatotoxicity.
How serious is the interaction between Fluconazole and Macitentan?
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 if possible; if unavoidable, monitor hemoglobin, liver tests and fluid status.
What other medicines interact with Macitentan?
MediHelp also lists interactions of Macitentan with, for example, Amiodarone, Apalutamide, Bosentan. The full list is on the Macitentan page.
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