antibioticsbooks

Fluconazole
The introduction of fluconazole in 1990 was a
breakthrough in antifungal pharmacotherapy.
Fluconazole is highly bioavailable, available in both
oral and IV formulations, and highly active against
many species of Candida. Before this, clinicians
were faced with the toxicity and inconvenience of
amphotericin B for serious forms of candidiasis.
Fluconazole has a low incidence of serious adverse
reactions, and converting from IV to oral therapy
is simple. Though a shift toward non-albicans species
of Candida has affected the use of fluconazole,
it remains an important, frequently utilized agent.
Mechanism of Action
All azoles inhibit fungal cytochrome P450 14-alpha
demethylase, inhibiting the conversion of lanosterol
into ergosterol, which is a component of the
fungal cell membrane.
Spectrum
Good: Candida albicans, Candida tropicalis,
Candida parapsilosis, Candida lusitaniae,
Cryptococcus neoformans, Coccidioides immitis
Moderate: Candida glabrata (can be susceptible
dose-dependent, or resistant)
Poor: molds, many dimorphic fungi, Candida krusei
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