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Azole Antifungals

  • Azole Antifungals are a structurally-related class of antifungals often used to treat systemic mycoses.
Mechanism of Action
  • The Azole Antifungals share a common mechanism of action which involves inhibition of fungal cytochrome P450 enzymes. These enzymes are required for successful synthesis of ergosterol, a critical component of the fungal cell wall.
Adverse Effects
  • The azole antifungals do not have substantial adverse effects except for Ketoconazole which was the first and least specific member of this class. Ketoconazole can interfere with synthesis of certain Steroid Hormones especially adrenocortical hormones (i.e. Mineralocorticoids, glucocorticoids, and adrenal androgens) as well as testosterone, resulting in endocrine dysregulation. In men this can result in gynecomastia], reduced libido, and impotence. Consequently, Ketoconazole is used only for cutaneous mycoses in a topical preparation and is not administered systemically as are the other azoles.
Member Drugs
  • Ketoconazole
  • Fluconazole
  • Itraconazole