Intravenous itraconazole

OBJECTIVE: TO review the pharmacology, mycology, chemistry, pharmacokinetic s, efficacy, safety, tolerability, dosage, administration, and economic iss ues of intravenous itraconazole. DATA SOURCES: A MEDLINE search from 1978 to June 2000 of the English-langua ge literature and an extensive review of meeting abstracts was conducted. D ue to the paucity of published information concerning the pharmacokinetics, efficacy, and safety of the intravenous formulation of intravenous itracon azole, additional information was obtained from the manufacturer. DATA EXTRACTION: Data from in vitro and preclinical studies, as well as Pha se II and III clinical trials, were included. DATA SYNTHESIS: The triazole antifungal agent itraconazole is available in a cyclodextrin-based intravenous formulation. Intravenous itraconazole is i ndicated for the treatment of pulmonary and extrapulmonary blastomycosis; h istoplasmosis, including chronic cavitary pulmonary disease and disseminate d, nonmeningeal histoplasmosis; and pulmonary and extrapulmonary aspergillo sis in patients who are intolerant of or who are refractory to amphotericin B. This formulation provides quicker and more consistent therapeutic conce ntrations than the oral formulations. Clinical data comparing the efficacy of intravenous itraconazole with that of amphotericin B are lacking. CONCLUSIONS: Intravenous itraconazole offers a less toxic alternative for p atients with pulmonary and extrapulmonary blastomycosis, histoplasmosis, an d aspergillosis who cannot receive oral medications or who are intolerant o f or refractory to amphotericin B.