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Name: Ketoconazole

Pregnancy Category C

Drug classes

• Antifungal

Therapeutic actions

Impairs the synthesis of ergosterol, the main sterol of fungal cell membranes, allowing increased permeability and leakage of cellular components and causing cell death.

Indications

1. Treatment of systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis
2. Treatment of dermatophytosis (recalcitrant infections not responding to topical or griseofulvin therapy)
3. Unlabeled uses: treatment of onychomycosis, pityriasis versicolor, vaginal candidiasis; CNS fungal infections at high doses (800-1,200 mg/d); treatment of advanced prostate cancer at doses of 400 mg q8h
4. Topical treatment of tinea corporis and tinea cruris caused by
5. Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum and the treatment of tinea versicolor caused by Malassezia furfur (topical administration)
6. Reduction of scaling due to dandruff (shampoo)
7. Orphan drug use: with cyclosporine to diminish cyclosporine-induced nephrotoxicity in organ transplant

Contraindications/cautions

• Contraindicated in the presence of allergy to ketoconazole; fungal meningitis; pregnancy; lactation.
• Use caution in the presence of hepatocellular failure (increased risk of hepatocellular necrosis).

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Adverse effects

• CNS: Headache, dizziness, somnolence, photophobia
• GI: Hepatotoxicity, nausea, vomiting, abdominal pain
• GU: Impotence, oligospermia (with very high doses)
• Hematologic: Thrombocytopenia, leudopenia, hemolytic anemia
• Hypersensitivity: Urticaria to anaphylaxis
• General: Pruritus, fever, chills, gynecomastia
• Local: Severe irritation, pruritus, stinging with topical application

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