The Sound of Evolution
Ketoconazole
Mechanism of action:
Ketoconazole is an imidazole derivative. It inhibits fungal lanosterol 14α-demethylase (CYP51), the enzyme responsible for converting lanosterol into ergosterol. When this step is blocked, the fungal cell membrane becomes structurally defective, while lanosterol accumulates because it can no longer be converted, producing toxicity and ultimately inhibiting fungal growth or causing fungal death.
Reference(s):
1. Goeders NE et al. (1998). Ketoconazole reduces low dose cocaine self-administration in rats. Drug Alcohol Depend.
2. Berwaerts J et al. (1999). Cushing's syndrome in pregnancy treated by ketoconazole: case report and review of the literature. Gynecol Endocrinol.
3. Kazy Z et al. (2005). Population-based case-control study of oral ketoconazole treatment for birth outcomes. Congenit Anom (Kyoto).