Azole antifungal agents prevent the synthesis of ergosterol, a major component of fungal plasma membranes, by inhibiting the cytochrome P-450-dependent enzyme lanosterol demethylase (also referred to as 14α-sterol demethylase or P-450DM). This enzyme also plays an important role in cholesterol synthesis in mammals. Exposure of fungi to an azole causes depletion of ergosterol and accumulation of 14α-methylated sterols. This interferes with the “bulk” functions of ergosterol in fungal membranes and disrupts both the structure of the membrane and several of its functions such as nutrient transport and chitin synthesis.
Remember the pharmacology of Azoles using these simple mnemonics.
Azoles antifungals indications include:
Fluconazole – Fluid Fluco flows into CNS (used for cryptococcal meningitis)
Clotrimazole – Cutaneous (topical) (also Miconazole, a stretch!)
Voriconazole – inVasive aspergillosis, Visual disturbances
Posaconazole – Potent Posa – decreases Potassium levels, Platelet count, Prophylaxis for invasive aspergillosis, candida in immunocompromised.
Classification of Azoles Antifungals IMIDAZOLES – Remember COMET-K:
Clotrimazole
Oxiconazole
Miconazole
Econazole
Tioconazole
Ketoconazole
Classification of Azoles Antifungals TRIAZOLES – Remember FIT VIP
Fluconazole
Itraconazole
Terconazole
Voriconazole
Isavuconazole
Posaconazole

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