Drug interactions
Bosentan + Macitentan
Severity: Major
Bosentan and Macitentan: major 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
Bosentan is a moderate CYP3A4 inducer and macitentan is cleared largely by CYP3A4. Coadministration can lower macitentan and its active metabolite exposure and may reduce its efficacy. Both are endothelin receptor antagonists, so combining them also adds no proven benefit and increases the burden of adverse effects such as hepatotoxicity.
What this interaction means in plain words
Bosentan 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.
Bosentan belongs to Miscellaneous; Macitentan belongs to Cardiovascular.
Why it happens
Bosentan induces CYP3A4, increasing macitentan metabolism, and the two agents share the same pharmacological class.
What to do
Avoid combining two endothelin receptor antagonists; use one agent only. Choose a different drug class if additional pulmonary hypertension therapy is needed.
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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Other interactions of Bosentan
- Bosentan + Cyclosporin Contraindicated
- Bosentan + Cyclosporine Contraindicated
- Bosentan + Glyburide Contraindicated
- Bosentan + Glyburide-metformin Contraindicated
- Bosentan + Lonafarnib Contraindicated
- Bosentan + Sparsentan Contraindicated
Other interactions of Macitentan
Frequently asked questions
Can I take Bosentan with Macitentan?
MediHelp rates the interaction as major. Bosentan 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. Bosentan is a moderate CYP3A4 inducer and macitentan is cleared largely by CYP3A4. Coadministration can lower macitentan and its active metabolite exposure and may reduce its efficacy. Both are endothelin receptor antagonists, so combining them also adds no proven benefit and increases the burden of adverse effects such as hepatotoxicity.
How serious is the interaction between Bosentan 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 combining two endothelin receptor antagonists; use one agent only. Choose a different drug class if additional pulmonary hypertension therapy is needed.
What other medicines interact with Bosentan?
MediHelp also lists interactions of Bosentan with, for example, Cyclosporin, Cyclosporine, Glyburide. The full list is on the Bosentan page.
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