FLUCONAZOLE

Fluconazole

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Manufacturer and trade name: Pfizer and many other companies, therefore several trade names, such as Diflucan^®, Fluconazole CT^®/Stada, or Flucobeta^®.

Indications: Candida infection, cryptococcal meningitis and some rare mycoses.

§  Fluconazole^® capsules, 50 mg, 100 mg, 200 mg.

§  Fluconazole^® suspension, 50 mg per 10 ml.

§  Fluconazole^® IV for injections, 100, 200 and 400 mg.

Dose: for oral candidiasis, 100 mg QD orally; for candida esophagitis 200 mg QD for 7-10 days. Double the dose on the first day. An attempt with a higher dose (up to 800 mg daily) may be made if there is persistent candidiasis after 10 days.

Cryptococcal meningitis: Initially, 400-800 mg daily, combined with flucytosine and amphotericin B if possible. After completion of acute therapy – usually after 6 weeks – maintenance therapy with 200 mg fluconazole daily.

Renal insufficiency: half the dose with creatinine clearance of 10 to 50 ml/min; reduce to 25% below 10 ml/min.

Side effects: overall good tolerability, rarely gastrointestinal complaints and elevated transaminases. Reversible alopecia in approximately 10% of cases with more than 400 mg daily.

Interactions, warnings: long-term treatment may lead to development of candida-resistant strains. Fluconazole is not effective against C. krusei or aspergillus. In cases of C. glabrata infection higher doses are required (sensitivity is dose-dependent). Fluconazole levels are reduced with concurrent administration of rifabutin/rifampin. Fluconazole increases the serum levels of rifabutin, atovaquone, clarithromycin, theophylline, opiates, coumarin derivatives, benzodiazepines, cyclosporine, tacrolimus, phenytoin and anti-convulsive drugs as well as AZT.

Comments: Fluconazole is the first choice for HIV-associated candidiasis and for the secondary prophylaxis of cryptococcosis (also as component of acute therapy). The tablets have good absorption. Infusions (more expensive) are only required in cases of non-adherence, severe mucositis, and/or problems with absorption.

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