Drug interactions
Bosentan + Rifampin
Severity: Major
Bosentan and Rifampin: major interaction.
Last updated Sources: UK SmPC
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
Rifampin strongly induces CYP3A4 and CYP2C9, which lowers bosentan exposure. Initial doses of rifampin may transiently raise bosentan levels through OATP inhibition, and hepatotoxicity risk is additive.
What this interaction means in plain words
Bosentan and Rifampin 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.
Why it happens
Rifampin induces CYP3A4 and CYP2C9 and transiently inhibits hepatic OATP uptake, altering bosentan exposure.
What to do
Avoid if possible; if combined, monitor liver aminotransferases and clinical response. Avoid or closely monitor with other hepatotoxic drugs.
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 Bosentan
- Bosentan + Cyclosporin Contraindicated
- Bosentan + Glibenclamide Contraindicated
- Bosentan + Glyburide-metformin Contraindicated
- Bosentan + Lonafarnib Contraindicated
- Bosentan + Sparsentan Contraindicated
- Artemether / lumefantrine + Bosentan Major
Frequently asked questions
Can I take Bosentan with Rifampin?
MediHelp rates the interaction as major. Bosentan and Rifampin 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. Rifampin strongly induces CYP3A4 and CYP2C9, which lowers bosentan exposure. Initial doses of rifampin may transiently raise bosentan levels through OATP inhibition, and hepatotoxicity risk is additive.
How serious is the interaction between Bosentan and Rifampin?
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 if possible; if combined, monitor liver aminotransferases and clinical response. Avoid or closely monitor with other hepatotoxic drugs.
What other medicines interact with Bosentan?
MediHelp also lists interactions of Bosentan with, for example, Cyclosporin, Glibenclamide, Glyburide-metformin. The full list is on the Bosentan page.
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