Ketoconazole

Ketoconazole is evaluated for the following indications with varying evidence strength: Seborrheic dermatitis (evidence tier A), Refractory systemic mycoses (evidence tier B), Cushing syndrome (evidence tier B). See the full indication matrix with dosing and citations above on this page.

Common side effects of Ketoconazole (≥ 1 in 100): Nausea, vomiting, abdominal discomfort, Rash, pruritus, Headache, dizziness, ALT/AST increase within 2× ULN. See the Safety section for uncommon and serious reactions.

FDA category C. FDA category C. Animal studies show embryotoxicity and teratogenicity at high systemic doses. Human data are insufficient. Systemic forms are not used during pregnancy; alternative azoles or echinocandins are preferred. Topical formulations (shampoo) are acceptable.

Systemic forms are not used while breastfeeding – ketoconazole transfers into breast milk. Topical use of shampoo or cream on areas not in contact with the infant is safe.

Ketoconazole is contraindicated in: Acute or chronic liver disease; ALT or AST > 2× ULN before therapy initiation; QT prolongation or history of ventricular arrhythmia; Co-administration with QT-prolonging drugs: cisapride, pimozide, quinidine, dofetilide; Co-administration with simvastatin, lovastatin, triazolam, oral midazolam, ergot alkaloids. Full list in the Safety section.

FDA boxed warning: systemic ketoconazole causes severe hepatotoxicity, including fulminant hepatic failure with death or need for transplantation. The drug is not used for superficial fungal infections. A separate boxed warning addresses clinically significant drug interactions and QT prolongation.

the FDA restricted these indications in 2013; terbinafine and itraconazole are used for onychomycosis.

systemic absorption of the shampoo is minimal, with no hepatotoxic risk. Topical and systemic forms are different safety categories.

fulminant hepatic failure occurs in approximately 1 in 15 000 patients, which prompted FDA and EMA restrictions.