Nizoral and Roflumilast

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 roflumilast. You may be more likely to experience side effects of roflumilast such as diarrhea, nausea, abdominal pain, weight loss, headache, insomnia, depression, and anxiety. Let your doctor know if side effects become excessive or intolerable. 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 systemic exposure to roflumilast and its pharmacologically active N-oxide metabolite. The proposed mechanism is ketoconazole inhibition of CYP450 3A4, the isoenzyme that partially metabolizes both roflumilast and the metabolite. In 26 healthy volunteers, administration of roflumilast 500 mcg orally once daily for 11 days in combination with a single 200 mg dose of ketoconazole on day 11 resulted in a 34% increase in roflumilast systemic exposure (AUC) and no change in peak plasma concentration (Cmax) compared to administration of roflumilast alone. Single-dose ketoconazole also reduced the Cmax and AUC of roflumilast N-oxide by 20% and 12%, respectively. When a single 500 mcg oral dose of roflumilast was administered in combination with repeated doses of ketoconazole (200 mg twice daily for 13 days) to 16 healthy volunteers, Cmax and AUC of roflumilast increased by 23% and 99%, respectively, while Cmax of roflumilast N-oxide decreased by 38% and AUC increased by 3% (not significant). Total phosphodiesterase 4 inhibitory activity (i.e., combined effect of both roflumilast and roflumilast N-oxide) increased by 9% in association with these changes. No clinically relevant adverse events were observed during the study.

MANAGEMENT: Caution is advised when roflumilast is used in combination with ketoconazole. Treatment with roflumilast should be re-evaluated if an interaction is suspected and persistent intolerability occurs. Patients should be advised to contact their doctor if they experience increased frequency and/or severity of side effects such as diarrhea, nausea, abdominal pain, weight loss, headache, insomnia, depression, and anxiety.

Nizoral

Generic Name: ketoconazole

Brand name: Nizoral

Synonyms: n.a.

What is Nizoral?

Roflumilast

Generic Name: roflumilast

Brand name: Daliresp

Synonyms: n.a.

What is Roflumilast?