A clinical study of fluconazole-granules and -injectable in pediatric patients with deep-seated mycoses

: Fluconazole (FLCZ) is an antifungal agent of triazole class developed by Pfizer, Inc. Its oral and injectable forms have been available on the market since June 1989 in Japan. FLCZ exhibits potent antifungal activities against Candida spp., Aspergillus spp. and Cryptococcus spp. and, as orally or intravenously administered, is widely distributed into organs and tissues. For its low protein binding rate of about 10 per cent and long serum half life of about thirty hours in adults, FLCZ has been proved highly effective and useful in the treatment of deep-seated mycosis in adult patients. In the present study, we have investigated the clinical effectiveness and antifungal activities of FLCZ granules, a new dosage form of the drug, and of intravenous form in pediatric patients with deep mycosis. A total of 72 patients were treated either with granules orally or with intravenous injection and 47 patients among them were evaluable on the clinical efficacy of the drug. Also, a study on the pharmacokinetics of pediatric patients including premature/new born babies was conducted employing multiple dose regimens in a total of 27 patients. The clinical efficacy rates were 79.5% (35 patients out of 44) in candidiasis and 100.0% (3 of 3) in aspergillosis. The safety of the drug was assessed in 63 patients. No side effects were observed. Clinical laboratory test abnormalities were observed in some patients with an incidence of 9.7% (6 patients out of 62) but most of the abnormalities were only mild and transient. The pharmacokinetics at repeated doses indicated that a steady-state is reached in 4 days after the initial administration of either granules or intravenous form. From these results, it may be concluded that FLCZ is a very useful medication in the treatment of deep mycosis in pediatric patients.