Ketoconazole and Other Imidazole Derivatives as Inhibitors of Steroidogenesis

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Abstract
Background IMIDAZOLE antifungal drugs are effective therapeutic agents in the treatment of mycotic infections (1). Because ketoconazole can be administered orally and has a broad spectrum of activity against both superficial and deep mycoses, this imidazole derivative has become widely used throughout the world as an antifungal agent (1, 2). In recent years it as become apparent that ketoconazole has additional potent actions to inhibit steroidogenesis. Much of the discussion to follow will be directed at the specific drug ketoconazole and its ability to suppress the synthesis of steroid hormones. However, other structurally related imidazole antifungal agents share in these antihormonal actions. In addition, other categories of drugs contain imidazole or azole structures, and some element of the hormonal effects to be discussed for ketoconazole may also apply to these drugs as well. Prominent examples are cimetidine, thiobendazole, and metronidazole. The ability to inhibit steroidogenesis is especially relevant for the drug etomidate, an imidazole, intravenous sedative-hypnotic agent used for the induction and/or maintenance of anesthesia. Etomidate closely resembles ketoconazole in its effects on steroidogenesis.

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