Vol.54 No.S-1 October 2006
Treatment of systemic fungal infections with Itraconazole preparations
Department of Microbiology and Immunology, Nagasaki University Graduate School of Biomedical Science,
1-7-1 Sakamoto, Nagasaki, Japan
Abstract
Itraconazole is an anti-fungal agent of the triazole family that has been shown to exhibit potent activity against fungi of Candida including non-albicans Candida and Aspergillus,. Currently, only capsule form is available for clinical use. However, with the development of a technique to dissolve the drug in hydroxypropyl-β-cyclodextrin, itraconazole oral solution and injection have begun to be developed. Itraconazole oral solution is better absorbed from the digestive tract capsule form. Itraconazole injection is administered at a loading dose level (200 mg/day in two divided doses) on the first two days, to allow rapid increase and maintenance of the plasma level of the drug to the level needed for the treatment of systemic fungal infections.
In foreign countries, trials of targeted therapy and empiric therapy using itraconazole oral solution and injection administration have been carried out and obtained excellent results. In regard to targeted therapy for patients with invasive aspergillosis (including many cases failure to intravenous amphotericin B (AMPH) therapy), itraconazole injection treatment followed by itraconazole capsules has obtained excellent results, with a remission (remission+partial remission) rate of 32% at the end of the injection treatment and 48% at the end of the study. In regard to empiric therapy for cases of persistent fever due to fungal infection (associated with neutropenia and failure to broad-spectrum antimicrobial agents), the efficacy of itraconazole injection and oral solution was found to be comparable to that of intravenous AMPH therapy, with, in addition, a significantly lower incidence of adverse reactions (nephrotoxicity, etc.) and dropouts.
In Japan, itraconazole capsules began to be marketed in 1993, and they have been used clinically for the treatment of skin and systemic fungal infections. When itraconazole oral solution and injection become available, the drug may become one of the major alternatives for the treatment of systemic fungal infections.
Key word
itraconazole, fungal infection, aspergillosis, candidiasis
Received
September 6, 2006
Accepted
October 2, 2006
Jpn. J. Chemother. 54 (S-1): 1-5, 2006
