Itraconazole

Itraconazole is an antifungal azole. It is a synthetic triazole analogue with a wide spectrum of antifungal activity. It was first synthesized in 1980, and approved in Europe in 1987.
It was approved by the FDA in 1992 for systemic mycoses, and then for onychomycoses in 1995, and for use by pulse therapy in 1997. In 2000, itraconazole was also approved to treat blastomycosis, histoplasmosis, and aspergellosis in patients intolerant of amphotericin B.

Itraconazole is used effectively in the treatment of onychomycosis and candidal infection.

It is lipophylic and quickly achieves high skin and mucous membrane concentrations, and may still be found in the stratum corneum 4 weeks after discontinuation of therapy.

Trade Name:

• Sporanox*   Janssen

Dosage Types:

• Oral: Capsules: Itraconazole 100mg Sporanox*
• Solution: Itraconazole 100mg/10 mL Sporanox*

Uses

Therapeutic Regimen

Patient Monitoring

Hepatic function tests should be monitored periodically during treatment. Serum potassium may be monitored as hypokalemia has lead to ventricular fibrillation in patients on itraconazole.

Drug Safety Information

!! Warnings & Contraindications !!

• Concurrent use with cisapride, azemizole and terfenadine is contraindicated.
• Iatroconazole capsules not to be prescribed for onychomycosis in patients with history of congestive heart failure.
• Hypokalemia has lead to ventricular fibrillation in patients on itraconazole

• Cutaneous effects may include hypersensitivity reactions including exfoliative dermatitis and Stevens-Johnson syndrome
• Gastrointestinal effects may include nausea, abdominal pain, diarrhea, constipation, loss of appetite and rarely, hepatotoxicity.
• Other effects may include headache, dizziness and drowsiness.

Major Drug Interactions

Concurrent use of itraconazole anticholinergics, omeprazole, and antacids may reduce the absorption of itraconazole; with digoxin levels may be increased and should be monitored; lovstatin and simvastatin concentrations may be increased, and have been associated with rhabdomyolysis; Didanosene may decrease the absorption of itroconazole; antidiabetic agents can lead to hypoglycemia; cyclosporine and phenytoin plasma concentrations may be increased; triazolam and midazolam serum concentrations may be increased; isoniazid, rifampin metabolism may be affected; anticoagulant effects may be increased.

General References

Elewski BE: Treatment of Tinea Capitis With Itraconazole. Int. Jour. Derm. 1997: 36: 539-541

Gupta AK, Maddin S, Arlette J, et al: Itraconazole pulse therapy is effective in dermatophyte onychomycosis of the toenail: a double-blind placebo-controlled study. Jour. Derm. Treat. 1999: 11: 33-37

Gupta AK, Solomon RS, Adam P: Itraconazole for the treatment of tinea capitis. Br. Jour. Derm. 1998: 139: 104-106

Heikkila H, Stubb S: Long-term Results of Patients with Onychomycosis Treated with Itraconazole. Acta Derm. Ven. 1997: 77: 70 -71

Gupta AK, Adam P, De Donker P: Itraconazole Pulse Therapy for Tinea Capitis: A Novel Treatment Schedule. Pediatr. Derm. 1998: 15: 225-228

Gupta AK, Hopstader SLR, Summerbell RC, et al: Treatment of Tinea Capitis With Itraconazole Capsule Pulse Therapy. Jour. Am. Acad. Derm. 1998: 39: 216-219

Havu V, Brandt H, Haikkila H et al: Continuous and intermittent itraconazole dosing schedules for the treatment of onychomycosis: a pharmacokinetic comparison. Br. Jour. Derm. 1999: 140: 96-101

Gupta AK, Katz HI, Shear NH: Drug interactions with itraconazole, fluconazole, and terbinafine, and their management. Jour. Am. Acad. Derm. 1999: 41: 237-239

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