Itraconazole

Last updated on: 29.10.2020

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Definition
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Triazole antifungal.

Indication
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Infections with dermatophytes, yeasts and moulds, especially Aspergillus species. Agent of choice for the interval treatment of Tinea unguium.

Limited indication
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Up to now not permitted for children ( off-label use). In studies, however, good results, e.g. in a randomized study with 34 children (< 12 years) in the treatment of tinea capitis with 500 mg/day griseofulvin versus 100 mg/day itraconazole for a total of 6 weeks. Identical treatment success in both groups with 88% cure. No side effects occurred in the group treated with itraconazole.

Dosage and method of use
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Vulvovaginitis candidamycetica: ED with 2 times 200 mg p.o.

skin mycoses ( tinea): 100-200 mg/day p.o. over 2-4 weeks.

Onychomycosis: Interval therapy week 1, 4 and 7: 2 times/day 100 mg p.o.

System mycoses (peroral therapy): 200-300 mg/day p.o. over 8-10 weeks, maintenance therapy 200 mg/day.

System mycoses (histoplasmosis, aspergillosis, candidiasis, cryptococcosis including cryptococcal meningitis): Day 1 and day 2: 2 times/day 200 mg (60 ml prepared infusion solution) slowly over 1 hour i.v. From day 3: 1 times/day 200 mg slowly over 1 hour i.v.

For children ( off-label use!): 10-20 kg bw: 100 mg every 2nd day; 20-40 kg bw: 100 mg once/day; 40-50 kg bw: 100 mg and 200 mg alternating daily, > 50 kg bw: 200 mg once/day p.o.

Remember! Pregnancy must be ruled out before and up to 4 weeks after the therapy. Women of childbearing age must be adequately protected against contraception during therapy! Itraconazole should only be prescribed for a maximum of 3 months due to potential toxic effects. Applies to both tinea unguium and tinea capitis.

Note: Alternatively, a "low-dose" microencapsulated form can be prescribed (Itraisdin®). In this case the same effect can be achieved with 50 mg as with 100 mg of the conventional preparation.

Undesirable effects
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Fever, allergic reactions, headaches, fatigue, dizziness, hypertension, gastrointestinal disorders, liver dysfunction.

Notice! For longer use, check liver enzymes at 4-weekly intervals!

Interactions
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S.u. Ketoconazole.

Contraindication
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Pregnancy, lactation, liver diseases, children and adolescents < 18 years.

Preparations
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Sempera®, Canifug Itra®, Itraisdin® (compared to the standard itraconazole preparations, Itraisdin is given in low doses - 50mg/100mg- due to an improved solubility but characterized by a high bioavailability) It is postulated that 50mg of low-dose itraconazole is as effective as the usual 100mg dose.

Note(s)
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In addition to its antifungal activity, itraconazole is an antagonist of the hedgehog signal transduction pathway, which is essential in embryogenesis for the growth and establishment of cell patterns. In vivo the effect could be shown in a mouse model for basal cell carcinomas and medulloblastomas.

Literature
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  1. Seebacher C et al (2006) Tinea capitis. J Dtsch Dermatol Ges 4: 1085-1091
  2. Seebacher C et al (2007) Tinea of the free skin. J Dtsch Dermatol Ges 11: 921-926
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Last updated on: 29.10.2020