Ketoconazole Topical and Rimegepant: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Ketoconazole Topical
Rimegepant
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 exposure of rimegepant
Interaction Deep Dive
Concomitant use of rimegepant with drugs that are both strong inhibitors of CYP3A4 and P-gp efflux transport results in a significant increase in rimegepant exposure and should be avoided. At steady state, coadministration of rimegepant with itraconazole, a strong CYP3A4 inhibitor, resulted in increased exposures of rimegepant AUC by 4-fold and Cmax by about 1.5-fold1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism and P-gp efflux transport of rimegepant
Literature reports
2 reports — tap to read
a) At steady state, coadministration of a single dose of rimegepant 75 mg with itraconazole, a strong CYP3A4 inhibitor, resulted in increased exposures of rimegepant AUC by 4-fold and Cmax by about 1.5-fold 1.
b) In a dedicated drug interaction study, concomitant administration of rimegepant orally disintegrating tablet with cyclosporine (a potent P-gp and BCRP inhibitor) and with quinidine (a potent P-gp inhibitor) resulted in an increase of similar magnitude in rimegepant exposure (AUC and Cmax by 1.6- and 1.4-fold with cyclosporine, and by 1.6- and 1.7-fold with quinidine, respectively) 2.
Common questions
Can I take Ketoconazole Topical and Rimegepant together?
Increased exposure of rimegepant Always confirm with your pharmacist or prescriber before making any change.
How serious is the Ketoconazole Topical and Rimegepant interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
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 "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Ketoconazole Topical or Rimegepant 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 (2)
- Product Information: NURTEC(TM) orally disintegrating tablets, rimegepant orally disintegrating tablets. Biohaven Pharmaceuticals Inc (per FDA), New Haven, CT, 2020.
- Product Information: NURTEC(R) ODT orally disintegrating tablets, rimegepant orally disintegrating tablets. Biohaven Pharmaceuticals Inc (per FDA), New Haven, CT, 2021.
Keep reading about Ketoconazole Topical
Keep reading about Rimegepant
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