Saxagliptin and Ketoconazole Topical: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Ketoconazole Topical
Saxagliptin
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 sAXagliptin exposure
Interaction Deep Dive
Caution is advised if ketoconazole (strong CYP3A4 inhibitor) and sAXagliptin (moderate CYP3A4 substrate) are coadministered, as it may increase sAXagliptin exposure. Upon coadministration, closely monitor patients for signs or symptoms of increased or prolonged effects or side effects of sAXagliptin1. Limit the dose of sAXagliptin to 2.5 mg/day when used with ketoconazole 23. SAXagliptin AUC and Cmax increased by 145% and 62%, respectively, when coadministered with ketoconazole, a strong CYP3A4 inhibitor. Limit the dose of sAXagliptin to 2.5 mg/day, if sAXagliptin and a strong CYP3A4 inhibitor are to be coadministered 4.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of sAXagliptin
Literature reports
3 reports — tap to read
a) In a drug interaction study, ketoconazole 200 mg twice daily for 7 days with a single 20 mg sAXagliptin dose resulted in increased sAXagliptin AUC by 3.67-fold and Cmax by 2.44-fold 32.
b) In a drug interaction study, ketoconazole 200 mg twice daily for 9 days with sAXagliptin 100 mg dose resulted in increased sAXagliptin AUC by 2.45-fold and Cmax by 1.62-fold 32.
c) Coadministration of ketoconazole, a strong CYP3A4 inhibitor, and sAXagliptin, a CYP3A4 substrate, increased sAXagliptin exposure in a drug interaction study with 15 healthy participants. In the study, ketoconazole 200 mg was administered twice daily 6 days, after which participants received ketoconazole 200 mg twice daily and sAXagliptin 100 mg (single dose). Results showed that coadministration with ketoconazole increased AUC values of sAXagliptin by 145% and increased Cmax of sAXagliptin by 62% versus sAXagliptin alone 4.
Common questions
Can I take Saxagliptin and Ketoconazole Topical together?
Increased sAXagliptin exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Saxagliptin and Ketoconazole Topical 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 "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Saxagliptin 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 (4)
- Product Information: Ketoconazole oral tablet, ketoconazole oral tablet. Taro Pharmaceuticals U.S.A. Inc. (per DailyMed), Hawthorne, NY, 2024. DailyMed
- Product Information: ONGLYZA(R) oral tablets, saxagliptin oral tablets. AstraZeneca Pharmaceuticals LP (per FDA), Wilmington, DE, 2024. DailyMed
- Product Information: KOMBIGLYZE(R) XR oral extended-release tablets, saxagliptin metformin HCl oral extended-release tablets. AstraZeneca Pharmaceuticals LP (per FDA), Wilmington, DE, 2024.
- Patel CG, Li L, Girgis S, et al: Two-way pharmacokinetic interaction studies between saxagliptin and cytochrome P450 substrates or inhibitors: simvastatin, diltiazem extended-release, and ketoconazole. Clin Pharmacol 2011; 3:13-25. PubMed
Keep reading about Ketoconazole Topical
Keep reading about Saxagliptin
These medications also interact with supplements
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.
Check another combination
Our instant two-drug interaction checker is almost here.
Still have questions about this combination?
Every question gets a real answer from a licensed pharmacist — free, and usually within a day.
Ask the pharmacist