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Fluconazole (Diflucan): a review.

M Zervos¹, F Meunier

¹William Beaumont Hospital, Royal Oak, MI, USA.

International Journal of Antimicrobial Agents

|January 1, 1993

Summary

Fluconazole, an antifungal medication, effectively treats various fungal infections by inhibiting ergosterol synthesis. It is well-tolerated and suitable for once-daily dosing in patients.

Area of Science:

Mycology
Pharmacology
Infectious Diseases

Background:

Fluconazole is a triazole antifungal agent used for localized and disseminated mycoses.
It exhibits in vivo activity against Candida spp., Cryptococcus neoformans, and other fungi like Blastomyces dermatitidis, Coccidioides immitis, Histoplasma capsulatum, and dermatophytes in animal models.

Purpose of the Study:

To review the efficacy and safety of fluconazole in treating various fungal infections.
To highlight its pharmacokinetic properties and potential therapeutic applications.

Main Methods:

The study is a review of existing data on fluconazole's activity and clinical use.
Information is drawn from animal models and extensive clinical trials.

Main Results:

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Fluconazole inhibits ergosterol synthesis, crucial for fungal cell membranes.
It demonstrates good absorption, tissue penetration (including cerebrospinal fluid), and a long half-life allowing once-daily dosing.
Clinical trials confirm efficacy in candidiasis (oropharyngeal, esophageal, disseminated) and cryptococcal meningitis, with potential in other fungal infections.

Conclusions:

Fluconazole is an effective and well-tolerated antifungal agent for various mycoses.
Its favorable pharmacokinetic profile supports its use in diverse clinical settings, including prophylaxis and treatment of serious fungal infections.