A synthetic derivative of phenylpiperazine with broad antifungal properties and potential antineoplastic activity.
Ketoconazole inhibits sterol 14-a-dimethylase, a microsomal cytochrome P450-dependent enzyme, thereby disrupting synthesis of ergosterol, an important component of the fungal cell wall.
Fungal infections: 200 mg once daily, up to 400 mg once daily if needed.
Seborrhoeic dermatitis - 2% foam: apply bid for 4 wk. - 1 or 2% shampoo: Apply twice wkly for 2-4 wk. Prophylaxis: As 2% shampoo, use once every 1-2 wk.
Pityriasis versicolor; skin fungal infections - 2% cream: apply 1-2 times/day. - 2% shampoo: Apply once daily for up to 5 days. Prophylaxis - 2% shampoo: use once daily for up to 3 days before exposure to sunshine.
Adverse drug reactions: adrenal insufficiency; GI disturbances, dermatitis, burning sensation, dizziness, somnolence, fever, photophobia, photosensitivity.