[en] Itraconazole is a broad spectrum antifungal agent of the bis-triazole class. The drug is an important option in the management of many human mycoses including various clinical presentations of aspergillosis. Indeed, the compound exhibits potent in vitro antifungal activity against Aspergillus spp. and shows variable fungicidal effect against the different species and strains. After amphotericin B, itraconazole has been the very first agent, and the first azole antifungal to have demonstrated clinical efficacy in aspergillosis. In vivo, the antifungal efficacy of itraconazole has been demonstrated in several types of aspergillosis both in immunocompetent and immunocompromised animal models. The drug administered in its oral or intravenous formulations displays non-linear plasma pharmacokinetics.
Despite best current therapies, the outcome of invasive aspergillosis may remain dismal. Fungal cells can induce enormous damage on a background of immunosuppression. Medical help comes often too slow or is too weak. It will be a long time before the ideal strategy is found for an effective prophylaxis or for the optimal therapy of disseminated and invasive aspergillosis. In spite of this limitation, itraconazole has a definite chemotherapeutic effect in experimental aspergillosis. Non-comparative clinical data of itraconazole in the treatment of suspected or proven invasive aspergillosis indicate response rates at least similar and possibly superior to those of amphotericin B. Itraconazole has clearly improved the clinical outcome in some of the less immunosuppressed patients with invasive aspergillosis. The experience with itraconazole for induction therapy of invasive aspergillosis is more limited in profoundly neutropenic patients. Itraconazole has an important role for consolidation and maintenance therapy of patients with invasive aspegillosis. Itraconazole oral cyclodextrin solution is particularly suitable in these indications. Novel combination and sequential therapies involving itraconazole with other antifungals are promising. Itraconazole is usually well tolerated, but a potential for drug interactions exists, mediated through the cytochrome P450 3A4 system. This possibility should be considered when itraconazole is used as part of a multi-drug regimen.