Drug interactions
Buspirone + Ketoconazole
Severity: Major
Buspirone 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
Buspirone undergoes extensive CYP3A4 first-pass metabolism, and strong inhibitors like ketoconazole can increase its levels many-fold. This can cause dizziness, drowsiness, nausea and headache.
What this interaction means in plain words
Buspirone 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.
Buspirone belongs to Central Nervous System; Ketoconazole belongs to Anti Fungals.
Why it happens
Ketoconazole inhibits intestinal and hepatic CYP3A4, reducing buspirone first-pass metabolism.
What to do
Start buspirone at a low dose, such as 2.5 mg daily, and titrate based on response and tolerability. Monitor for excess sedation and dizziness.
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 Ketoconazole
- Alfuzosin + Ketoconazole Contraindicated
- Alprazolam + Ketoconazole Contraindicated
- Avanafil + Ketoconazole Contraindicated
- Conivaptan + Ketoconazole Contraindicated
- Dihydroergotamine intranasal + Ketoconazole Contraindicated
- Dihydroergotamine + Ketoconazole Contraindicated
Other interactions of Buspirone
- Buspirone + Isocarboxazid Contraindicated
- Buspirone + Linezolid Contraindicated
- Buspirone + Phenelzine Contraindicated
- Buspirone + Procarbazine Contraindicated
- Buspirone + Selegiline Contraindicated
- Buspirone + Selegiline transdermal Contraindicated
Frequently asked questions
Can I take Buspirone with Ketoconazole?
MediHelp rates the interaction as major. Buspirone 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. Buspirone undergoes extensive CYP3A4 first-pass metabolism, and strong inhibitors like ketoconazole can increase its levels many-fold. This can cause dizziness, drowsiness, nausea and headache.
How serious is the interaction between Buspirone 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: Start buspirone at a low dose, such as 2.5 mg daily, and titrate based on response and tolerability. Monitor for excess sedation and dizziness.
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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