Azoles antifungals, aka ergosterol synthesis inhibitors or 14-alpha demethylase inhibitors, are a class of medications used to treat many fungal infections such as topical infections like candidiasis (cutaneous, vulvovaginal, oropharyngeal), tinea (corporis, cruris, pedis, versicolor), onychomycosis, dandruff, and systemic infections like aspergillosis, cryptococcal meningitis, blastomycosis, mucomycosis, histoplasmosis, etc…
Azole antifungals work by inhibiting lanosterol 14-alpha
demethylase which catalyzes the conversion of lanosterol to ergosterol (a
molecule found in the fungi cell membrane) decreasing the membrane permeability
and leading to the fungus cell lysis.
Azole antifungals are divided into two subclasses: triazoles
(fluconazole, voriconazole, itraconazole, posaconazole, and isavuconazole), and
imidazoles ( clotrimazole, oxiconazole, miconazole, econazole, tioconazole,
ketoconazole).
All azole antifungals are strong inhibitors of CYP3A4
(especially itraconazole, voriconazole, and ketoconazole) CYP2C9, and CYP2C19
(especially fluconazole).
Azole antifungals are relatively safe medications but are no
stranger to side effects. Side effects may include nausea, vomiting, diarrhea,
pruritis, allergic rash, hepatitis, lethargy, anorexia, prolonged QT interval,
and visual disturbance.
Contraindications of azole antifungals include impaired
liver function, chronic kidney disease, hypokalemia, hypomagnesemia, abnormal
QT interval, torsades de pointes, and pregnancy.
Ketoconazole, posaconazole, and itraconazole oral forms need
gastric acidity for a good absorption rate so many medications may decrease
their absorption like PPI, histamine H-2 blockers, and antacids.
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