Drug interactions
Buprenorphine long-acting + Ketoconazole
Severity: Major
Buprenorphine long-acting and Ketoconazole: 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
Ketoconazole strongly inhibits CYP3A4 and can raise buprenorphine levels from the long-acting injection. The depot cannot be quickly adjusted, so toxicity may be prolonged.
What this interaction means in plain words
Buprenorphine long-acting and Ketoconazole 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
Strong CYP3A4 inhibition reduces buprenorphine metabolism.
What to do
Monitor for sedation, respiratory depression and signs of overdose; if the inhibitor cannot be reduced or stopped, switch to an adjustable transmucosal buprenorphine.
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
- Ketoconazole Esteve 200 mg Tablets - SmPC sections 4.3/4.5 (names the partner; "Buprenorphine IV and sublingual") — electronic medicines compendium (UK SmPC)
Other interactions of Ketoconazole
- Alfuzosin + Ketoconazole Contraindicated
- Alprazolam + Ketoconazole Contraindicated
- Avanafil + Ketoconazole Contraindicated
- Conivaptan + Ketoconazole Contraindicated
- Dihydroergotamine intranasal + Ketoconazole Contraindicated
- Dihydroergotamine + Ketoconazole Contraindicated
Frequently asked questions
Can I take Buprenorphine long-acting with Ketoconazole?
MediHelp rates the interaction as major. Buprenorphine long-acting and Ketoconazole 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 strongly inhibits CYP3A4 and can raise buprenorphine levels from the long-acting injection. The depot cannot be quickly adjusted, so toxicity may be prolonged.
How serious is the interaction between Buprenorphine long-acting and Ketoconazole?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Monitor for sedation, respiratory depression and signs of overdose; if the inhibitor cannot be reduced or stopped, switch to an adjustable transmucosal buprenorphine.
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.
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