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Drug interactions

Bosentan + Lopinavir

Severity: Major

Bosentan and Lopinavir: 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

Ritonavir-boosted lopinavir greatly increases bosentan concentrations, raising the risk of hepatotoxicity, hypotension and edema. Bosentan may also modestly lower lopinavir levels.

What this interaction means in plain words

Bosentan and Lopinavir 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; Lopinavir belongs to Anti Virals.

Evidence level: High

Why it happens

Lopinavir/ritonavir inhibits CYP3A4 and OATP transport of bosentan, while bosentan induces CYP3A4.

What to do

If starting bosentan in a patient on the protease inhibitor for at least 10 days, use 62.5 mg once daily or every other day. If starting the protease inhibitor, stop bosentan at least 36 hours earlier and restart after 10 days at the reduced dose, monitoring liver enzymes and viral load.

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?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

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References

Frequently asked questions

Can I take Bosentan with Lopinavir?

MediHelp rates the interaction as major. Bosentan and Lopinavir 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. Ritonavir-boosted lopinavir greatly increases bosentan concentrations, raising the risk of hepatotoxicity, hypotension and edema. Bosentan may also modestly lower lopinavir levels.

How serious is the interaction between Bosentan and Lopinavir?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: If starting bosentan in a patient on the protease inhibitor for at least 10 days, use 62.5 mg once daily or every other day. If starting the protease inhibitor, stop bosentan at least 36 hours earlier and restart after 10 days at the reduced dose, monitoring liver enzymes and viral load.

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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