Ketoconazole with Saxagliptin Interaction Details
Brand Names Associated with Ketoconazole
- Ketoconazole
- Nizoral®
Brand Names Associated with Saxagliptin
- Kombiglyze® XR (as a combination product containing Metformin, Saxagliptin)
- Onglyza®
- Qtern® (as a combination product containing Dapagliflozin, Saxagliptin)
- Qternmet® XR (as a combination product containing Dapagliflozin, Metformin, Saxagliptin)
- Saxagliptin
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 02, 2023
Interaction Effect
Increased saxagliptin exposure
Interaction Summary
Concomitant use of saxagliptin, a CYP3A substrate, and strong CYP3A inhibitors may increase saxagliptin exposure. Saxagliptin AUC and Cmax increased by 145% and 62%, respectively, when coadministered with ketoconazole, a strong CYP3A4 inhibitor. If saxagliptin and a strong CYP3A4 inhibitor are to be coadministered, saxagliptin should be limited to 2.5 mg/day ; for saxagliptin/metformin extended-release combination, limit the dose to saxagliptin 2.5 mg/metformin 1000 mg once daily when used with strong CYP3A inhibitors . Monitor for changes in glycemic control or increased adverse effects of saxagliptin, including hypoglycemia.
Severity
Moderate
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Concomitant use of saxagliptin, a CYP3A substrate, and strong CYP3A inhibitors may increase saxagliptin exposure. Limit the dose of saxagliptin to 2.5 mg/day when used with strong CYP3A inhibitors; for saxagliptin/metformin extended-release combination, limit the dose to saxagliptin 2.5 mg/metformin 1000 mg once daily when used with strong CYP3A inhibitors. . Monitor for changes in glycemic control or increased adverse effects of saxagliptin, including hypoglycemia.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated saxagliptin metabolism
Literature Reports
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 .
B) Coadministration of ketoconazole, a strong CYP3A4 inhibitor, and saxagliptin, a CYP3A 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 .
Ketoconazole Overview
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Ketoconazole is used to treat fungal infections when other medications are not available or cannot be tolerated. Ketoconazole should not be used to treat fungal meningitis (infection of the membranes surrounding the brain and spinal cord caused by a fungus) or fungal nail infections. Ketoconazole is in a class of antifungals called imidazoles. It works by slowing the growth of fungi that cause infection.
Saxagliptin Overview
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Saxagliptin is used along with diet and exercise to lower blood sugar levels in patients with type 2 diabetes (condition in which blood sugar is too high because the body does not produce or use insulin normally). Saxagliptin is in a class of medications called dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by increasing the amount of insulin produced by the body after meals when blood sugar is high. Saxagliptin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and, therefore, cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition that may develop if high blood sugar is not treated).
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Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.