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Clotrimazole, bis-phenyl-(2-chlorophenyl)-1-imidazolyl methane, is a uniquely antifungal compound. In vitro, its spectrum includes dematiaceous, dermatophytes, dimorphic fungi and yeasts species. Its inhibitory concentrations in vitro were ≤ 4μg/mL for most susceptible fungi and ≤1 μg/mL for many species, particularly Trichophyton and Candida. Concentrations >20 μg/mL were fungicidal only [1]. It is also a specific Ca2+ activated K+ channel (Gardos channel) inhibitor [2]. Its IC50 to whole-cell currents in epithelial cells is 9 μmol/l [3].

Gardos channel contributes to pathologic water loss from erythrocytes and results in abnormal hemoglobin and promotes sickling in vitro. To avoid K+ and water loss via this channel was suggested as a potential therapy in vivo [2].

At concentrations ≤0.39 μg/mL, clotrimazole inhibited most isolates of C. neoformans, H. capsulatum and C. immitis. At concentrations < 0.78 μg/mL, clotrimazole did not inhibit one of C. neoformans. At 0.78 μg/mL, clotrimazole was fungicidal for all isolates, except a less susceptible isolate of H. capsulatum [1].

Subjects who had sickle cell anemia were treated with oral clotrimazole (10mg clotrimazole/kg/d for one week, and then daily dose was escalated by 10mg/kg each week). At a dosage of 20mg clotrimazole/kg/d, it was found that the Gardos channel was inhibited, cell K+ content was increased, erythrocyte dehydration was reduced, and hemoglobin levels was somewhat increased in all subjects. There are only three types of adverse effects, i.e. mild/moderate dysuria in all subjects and a reversible increase in plasma aspartic transaminase and alanine transaminase levels in two subjects treated with 30mg clotrimazole/kg/d [2].

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