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Everolimus Tablets (Afinitor) and Ketoconazole (Systemic)

Determining the interaction of Everolimus Tablets (Afinitor) and Ketoconazole (Systemic) and the possibility of their joint administration.

Check result:
Everolimus Tablets (Afinitor) <> Ketoconazole (Systemic)
Relevance: 03.07.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Using everolimus together with ketoconazole is not recommended. Combining these medications can significantly increase the blood levels of everolimus, which may make you more likely to develop serious side effects such as pneumonitis (inflammation of the lungs), infection, mouth ulcers, anemia, or bleeding. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Professional:

GENERALLY AVOID: Coadministration with potent or moderate inhibitors of CYP450 3A4 and/or P-glycoprotein may significantly increase the plasma concentrations of everolimus following oral administration. Everolimus is a substrate of both the CYP450 3A4 isoenzyme and P-glycoprotein drug efflux transporter, thus their inhibition in the intestine can enhance the absorption of everolimus. The risk of side effects such as pneumonitis, stomatitis, infection, dyspnea, diarrhea, anemia, leucopenia, thrombocytopenia, hyperglycemia, and hyperlipidemia may be increased.

MANAGEMENT: The use of everolimus with potent or moderate inhibitors of CYP450 3A4 and/or P-glycoprotein such as protease inhibitors, macrolide antibiotics, and azole antifungal agents should generally be avoided.

References
  • "Product Information. Nizoral (ketoconazole)." Janssen Pharmaceutica, Titusville, NJ.
  • "Product Information. Afinitor (everolimus)." Novartis Pharmaceuticals, East Hanover, NJ.
Everolimus Tablets (Afinitor)

Generic Name: everolimus

Brand name: Zortress, Afinitor, Afinitor Disperz

Synonyms: Everolimus

Ketoconazole (Systemic)

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: Ketoconazole

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.