Ketoconazole (Systemic) and Rosiglitazone Maleate

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.

Ketoconazole may increase the blood levels and effects of rosiglitazone. This can increase the risk of hypoglycemia (low blood sugar). Symptoms include headache, dizziness, drowsiness, nervousness, weakness, tremor, nausea, hunger, sweating, and fast or pounding heartbeats. You may need a dose adjustment or more frequent monitoring of your blood sugar 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 rosiglitazone. The proposed mechanism is ketoconazole inhibition of the metabolism of rosiglitazone via CYP450 2C8 and 2C9. In ten healthy Korean male volunteers, administration of a single 8 mg dose of rosiglitazone following ketoconazole 200 mg twice daily for 5 days resulted in a 17% increase in the mean rosiglitazone peak plasma concentration (Cmax) and a 47% increase in mean systemic exposure (AUC) compared to administration after placebo. Ketoconazole also prolonged the mean elimination half-life of rosiglitazone from 3.55 to 5.50 hours and reduced its apparent oral clearance (Cl/F) by 28% compared to placebo. No clinical effects attributable to the interaction were reported in the study. However, clinical significance of the interaction in diabetics cannot be precluded due to potentially reduced counter-regulatory response to hypoglycemia in these patients.

MANAGEMENT: Because the antidiabetic effect of rosiglitazone is dose- and concentration-dependent, pharmacologic response to rosiglitazone should be monitored more closely following the addition or discontinuation of ketoconazole. Patients should be advised to regularly monitor their blood sugar and counseled on how to recognize and treat hypoglycemia, which may include symptoms such as headache, dizziness, drowsiness, nervousness, confusion, tremor, hunger, weakness, perspiration, and palpitations. The rosiglitazone dosage may require adjustment if an interaction is suspected.

Ketoconazole (Systemic)

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: Ketoconazole

What is Ketoconazole (Systemic)?

Rosiglitazone Maleate

Generic Name: rosiglitazone

Brand name: Avandia

Synonyms: Rosiglitazone

What is Rosiglitazone Maleate?