Imatinib and Ketoconazole (Systemic)

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.

Using ketoconazole together with imatinib can cause decreased bone marrow function and blood problems (extreme fatigue, easy bruising or bleeding, black, bloody or tarry stools, fever or chills, or signs of infection), severe nausea, vomiting, diarrhea, and loss of appetite, swelling, and others. Contact your doctor if you experience any of these side effects. You may need a dose adjustment or special test to safely use both medications. 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.

MONITOR: Coadministration with ketoconazole may increase the plasma concentrations of imatinib. The mechanism is ketoconazole inhibition of CYP450 3A4, the isoenzyme responsible for the metabolic clearance of imatinib. In 14 healthy volunteers, coadministration of a single 200 mg oral dose of imatinib with a 400 mg oral dose of ketoconazole resulted in a 26% increase in the mean peak plasma concentration (Cmax) and a 40% increase in the area under the concentration-time curve (AUC) of imatinib compared to administration of imatinib 200 mg alone. Apparent clearance of imatinib was reduced 29% by ketoconazole, although half-life was not significantly altered. The interaction may be greater during multiple-dosing of these agents.

MANAGEMENT: Caution is advised if imatinib is prescribed with ketoconazole. The possibility of prolonged and/or increased pharmacologic effects of imatinib, including serious adverse effects such as edema, hematologic toxicity and immunosuppression, should be considered.

Imatinib

Generic Name: imatinib

Brand name: Gleevec

Synonyms: n.a.

What is Imatinib?

Ketoconazole (Systemic)

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: Ketoconazole

What is Ketoconazole (Systemic)?