Gepirone and Ketoconazole Topical: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Gepirone
Ketoconazole Topical
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased gepirone exposure, an increased risk of gepirone-related adverse effects, an increased risk of QT interval prolongation and cardiac arrhythmias
Interaction Deep Dive
Concomitant use of gepirone with QT prolonging strong CYP3A4 inhibitors is contraindicated as it may increases the exposure of gepirone and may increase the risk of QT prolongation and cardiac arrhythmias. In drug interaction studies, concomitant use of gepirone with a strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily) increases gepirone exposure by approximately 5-fold1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of gepirone; additive QT interval prolongation
Literature reports
1 report — tap to read
a) In drug interaction studies, concomitant use of gepirone with a strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily) increases gepirone exposure by approximately 5-fold 1.
Common questions
Can I take Gepirone and Ketoconazole Topical together?
Increased gepirone exposure, an increased risk of gepirone-related adverse effects, an increased risk of QT interval prolongation and cardiac arrhythmias Always confirm with your pharmacist or prescriber before making any change.
How serious is the Gepirone and Ketoconazole Topical interaction?
It is rated contraindicated. These should generally not be used together.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Gepirone or Ketoconazole Topical need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (1)
- Product Information: EXXUA extended-release oral tablets, gepirone extended-release oral tablets. Mission Pharmaceutical Company (per FDA), San Antonio, TX, 2023. DailyMed
Keep reading about Gepirone
Keep reading about Ketoconazole Topical
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Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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