ABSTRACT
Ketoconazole, the first oral systemically acting azole, was introduced in 1981 and at the time it represented an advance in antifungal therapy. Prior to this, choices of systemic antifungal therapy were limited to intravenous (IV) amphotericin B or miconazole, oral flucytosine. All these agents were associated with significant toxicity, and flucytosine had a narrow spectrum of activity. The use of ketoconazole was limited over time as a result of the subsequent introductions of fluconazole in 1990, and itraconazole in 1992, These azoles were designed to be more specific for fungal cells, and to be associated with less human toxicity. Consequently ketoconazole is now relegated to second-line status for the treatment of many systemic mycoses. Voriconazole, the most recent addition to this class, possesses a broad spectrum of activity and thus, it represents yet another advance in this growing class of antimycotics. The safety and efficacy of fluconazole, itraconazole, and voriconazole, make them significant additions to the antifungal arsenal. These azoles represent relatively safe and effective alternatives to other systemically acting antifungal agents. This chapter will review the pharmacology of the azole class of antifungal agents.
