Drug interactions
Buprenorphine + Ketoconazole
Severity: Major
Buprenorphine and Ketoconazole: 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
Ketoconazole is a strong CYP3A4 inhibitor and increases buprenorphine exposure, raising the risk of sedation and respiratory depression. Buprenorphine labeling recommends monitoring and dose reduction with strong CYP3A4 inhibitors.
What this interaction means in plain words
Buprenorphine 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.
Buprenorphine belongs to Musculoskeletal; Ketoconazole belongs to Anti Fungals.
Why it happens
Inhibition of CYP3A4-mediated N-dealkylation of buprenorphine reduces its clearance.
What to do
Monitor for oversedation and respiratory depression, and lower the buprenorphine dose if needed. Reassess when the antifungal is stopped as levels will fall.
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 Buprenorphine
- Alvimopan + Buprenorphine Contraindicated
- Buprenorphine + Calcium / magnesium / potassium / sodium oxybates Contraindicated
- Buprenorphine + Olanzapine / samidorphan Contraindicated
- Buprenorphine + Phenelzine Contraindicated
- Buprenorphine + Pimozide Contraindicated
- Buprenorphine + Thioridazine Contraindicated
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 with Ketoconazole?
MediHelp rates the interaction as major. Buprenorphine 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 is a strong CYP3A4 inhibitor and increases buprenorphine exposure, raising the risk of sedation and respiratory depression. Buprenorphine labeling recommends monitoring and dose reduction with strong CYP3A4 inhibitors.
How serious is the interaction between Buprenorphine 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 oversedation and respiratory depression, and lower the buprenorphine dose if needed. Reassess when the antifungal is stopped as levels will fall.
What other medicines interact with Buprenorphine?
MediHelp also lists interactions of Buprenorphine with, for example, Alvimopan, Calcium / magnesium / potassium / sodium oxybates, Olanzapine / samidorphan. The full list is on the Buprenorphine page.
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