Ketoconazole

Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections. Label It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus. 5 , 11 Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. 9 At this time it was considered a significant improvement over previous antifungals, miconazole and clotrimazole , due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis. 9 , 10 These effects combined with waning efficacy led to its eventual replacement by triazole agents, fluconazole , itraconazole , [voraconazole], and posaconazole . Ketoconazole and its predecessor clotrimazole continue to be used in topical formulations.