Itraconazole is a lipophilic substance which is practically insoluble in water and dilute acidic solutions. Partition coefficient in n-octanol/aqueous buffer of pH 8.1: 5.66. The triazole antimycotic itraconazole was first synthesized at Janssen Pharmaceuticals.

Trade Names

Itrizole (Cilag), Sempera (Janssen), Siros (Cilag), Sporanox (Edward Keller, Janssen), Triasporin (Lifepharma).

Indications

Therapy of dermatophytoses and onychomycoses with a dosing regimen of 100 to 200 mg per day. Vaginal candidosis with 200 mg/d for 3 days. Therapy of systemic infections such as candidosis and aspergillosis including disseminated infections, blastomycosis, coccidioidomycosis, histoplasmosis, and cryptococcosis with a dosing regimen of 100 to 400 (or up to 600) mg/d. Especially in aspergillosis, an early onset of therapy is important for the clinical outcome.

Side Effects

Itraconazole is generally well tolerated. CNS. Vertigo and headache: 10 %. GIT. Stomachache, vomiting, and diarrhoea were observed. Liver. Rise in transaminases and other reversible liver affections: 7 %. Metabolism. Hypokaliemia and rise in serum triglycerides.