Itraconazole: Pharmacologic Studies in Animals and Humans

High-dose itraconazole in the treatment of severe mycoses

“…The wider spectrum of activity and greater potency are advantages over ketoconazole (3,7,32,36,37). Itraconazole therapy has been effective in some patients who have experienced failures of prior therapy with either ketoconazole or AMB (8).…”

“…It is more potent and has a wider spectrum of activity than ketoconazole in vitro and in vivo (3,7,32,36,37). Clinical responses have been reported in patients with systemic mycoses, including coccidioidomycosis, sporotrichosis, chromoblastomycosis, and aspergillosis.…”

“…Usual treatment regimens have included daily dosing at 400 mg or less (2,4,8,21,23,28,29,34). Few adverse effects have been noted in the treatment of human mycoses with doses of up to 400 mg/day (2,4,8,21,23,28,29,34,36).…”

“…In contrast to ketoconazole, itraconazole has no significant effects on testicular and adrenal hormones during treatment with doses of up to 400 mg/day (9, 19, 25-27, 30, 33, 35). The lack of these effects may be due to a more selective inhibition of P-450 enzymes in fungal cells than in mammalian cells by itraconazole (19,36).…”

Aspergillosis of the CNS in a Pediatric Liver Transplant Recipient: Case Report and Review

“…In vivo evaluation with use of a murine model revealed greater activity than that achieved by ketoconazole, but no comparison was made with the activity of amphotericin B [37,38]. It is unfortunate that only a limited number of case repons have described the use of itraconazole for the treatment of aspeg illosis in humans, with variable results [39][40][41]. Fluconazole is a newer triazole agent that has been extremely promising in the treatment of systemic fungal infection [42 J.…”