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Drug interactions

Ketoconazole + Riociguat

Severity: Major

Ketoconazole and Riociguat: 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

Ketoconazole inhibits both CYP-mediated metabolism and BCRP-mediated efflux of riociguat, raising its exposure. This may cause symptomatic hypotension.

What this interaction means in plain words

Ketoconazole and Riociguat 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.

Ketoconazole belongs to Anti Fungals; Riociguat belongs to Cardiovascular.

Evidence level: High

Why it happens

Inhibition of multiple CYP enzymes (including CYP3A) and BCRP reduces riociguat clearance.

What to do

Consider a starting dose of 0.5 mg three times daily and monitor for hypotension, reducing the dose if symptoms occur.

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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Frequently asked questions

Can I take Ketoconazole with Riociguat?

MediHelp rates the interaction as major. Ketoconazole and Riociguat 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. Ketoconazole inhibits both CYP-mediated metabolism and BCRP-mediated efflux of riociguat, raising its exposure. This may cause symptomatic hypotension.

How serious is the interaction between Ketoconazole and Riociguat?

MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Consider a starting dose of 0.5 mg three times daily and monitor for hypotension, reducing the dose if symptoms occur.

What other medicines interact with Ketoconazole?

MediHelp also lists interactions of Ketoconazole with, for example, Alfuzosin, Alprazolam, Avanafil. The full list is on the Ketoconazole page.

Full monographs, dosing and an interaction checker in the MediHelp app

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