(1997; 132 pages) [French] [Spanish]
Capsule, 100 mg
Itraconazole is a triazole derivative with a broad spectrum of antifungal activity. It is well absorbed and passes readily across the blood-brain barrier into the cerebrospinal fluid. The plasma half-life is about 30 hours. It is metabolized in the liver and eliminated in the urine.
The drug is currently expensive, which may limit its availability.
• oropharyngeal and vulvovaginal candidosis
• resistant dermatophyte infections of the skin
• subcutaneous fungal infections, including sporotrichosis, chromomycosis and zygomycosis
• systemic fungal infections, including histoplasmosis and paracoccidioido-mycosis,1 with skin involvement.
1 For further information, see WHO model prescribing information: drugs used in sexually transmitted diseases and HIV infection. Geneva, World Health Organization, 1995.
Dosage and administration
All doses are suitable for adults and children over 12 years.
100 mg daily for 15 days.
400 mg in two divided doses taken on the same day.
Resistant dermatophyte infections of the skin:
200 mg daily for 15-30 days.
Higher dosages may be needed in patients with associated infections of the nails: 400 mg daily for 7 consecutive days per month for 3 months.
Subcutaneous and systemic fungal infections:
200-400 mg daily for as long as lesions persist.
• Known hypersensitivity to azole derivatives.
• Severe hepatic impairment.
• Age under 12 years.
Dosage should be reduced in accordance with the creatinine clearance rate in patients with renal impairment.
Hepatic function should be monitored when treatment is prolonged.
Women of child-bearing age should take effective contraceptive precautions during treatment and for several weeks thereafter.
Use in pregnancy and lactation
Itraconazole has been shown to have teratogenic potential when given in high doses to experimental animals. The need for treatment must be determined by the condition of the mother. Breast-feeding should be interrupted during treatment.
Itraconazole is generally well tolerated. Nausea is the most frequently reported adverse effect. Vomiting and abdominal distension and discomfort have also been reported.
Elevation of hepatic enzyme levels, which occurs in a small percentage of individuals, is readily reversible in the early stages. Treatment should be discontinued if signs develop that are suggestive of hepatic disease.
Itraconazole should be withdrawn if skin rashes progress during treatment. Exfoliative skin disorders have been reported, but a causal association has not been established.
Anaphylaxis occurs rarely.
The hepatic metabolism of other lipid-soluble drugs, including ciclosporin, phenytoin, sulfonylureas, theophylline and warfarin, is inhibited.
Rifampicin accelerates the clearance of itraconazole.
Concomitant administration of terfenadine should be avoided since it has been associated with serious, sometimes fatal, cardiac dysrhythmias.
No experience has been gained with overdosage of itraconazole. Induction of emesis and gastric lavage may be tried in the case of accidental overdosage.
Capsules should be kept in well-closed containers, protected from light.