[In-vitro and in-vivo activity of itraconazole]

Itraconazole is a lipophilic triazole with potent in vitro activity. It is also highly efficacious after topical, oral and parenteral administration. The antifungal activity of itraconazole has been evaluated against more than 6500 different strains, belonging to more than 260 fungal species using the serial decimal dilution test in fluid media (BHI broth). Candida, Torulopsis, Cryptococcus, Pityrosporum (Dixon broth), various other yeasts, dermatophytes, Aspergillus, Penicillium, Sporothrix, dimorphic fungi (MP and YP), Phaeohyphomycetes, Entomophthorales and various Hyalohyphomycetes are sensitive. Most strains of Fusarium and Zygomycetes are poorly sensitive. Itraconazole was administered orally and parenterally in normal and in immunocompromised guinea-pigs, infected with C. albicans, Cr. neoformans, H. duboisii, Sp. schenckii, P. marneffei and A. fumigatus. It was efficacious both in survival of the animals and in eliminating the fungi from the various tissues. Itraconazole was superior to fluconazole in candidosis, cryptococcosis, sporotrichosis and aspergillosis, to amphotericin B and to flucytosine in candidosis, cryptococcosis and aspergillosis. No comparative studies were done up to now for the other deep mycoses. The results of combination therapy of itraconazole with fluconazole in cryptococcosis were indifferent, with 5-flucytosine or amphotericin B, additive or synergistic in systemic candidosis, cryptococcosis and aspergillosis. No drug-related side-effects were observed after oral or parenteral administration of itraconazole.