Ketoconazole (oral)

Category: pharmacological

Aliases: Nizoral

Pharmacological Mechanism

Imidazole antifungal — inhibits fungal CYP51 ergosterol synthesis. Potent CYP3A4 inhibitor in human liver — historically the gold-standard "strong CYP3A4 perpetrator" for DDI studies. Oral use restricted by FDA 2013 to mycoses unresponsive to alternatives due to hepatotoxicity + adrenal suppression.

Half-Life (t½)

PO: 7.7h

Dosing Guidelines

• PO: Typical 200mg (Range: 200 - 400 mg)

Target Organ Systems

• endocrine
• digestive
• immune-hematologic

Interactions

• Cyclosporine
• Midazolam
• Triazolam
• Alprazolam
• Sildenafil
• Nifedipine