Fujii R, Matsumoto S, Sakiyama Y, Ishikawa Y, Takeda T, Hatae Y, Takase A, Sunakawa K, Yokota T, Kobayashi M
Department of Pediatrics, School of Medicine, Teikyo University.
Jpn J Antibiot. 1993 Aug;46(8):654-85.
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.
氟康唑（FLCZ）是辉瑞公司研发的一种三唑类抗真菌药物。自1989年6月起，其口服和注射剂型在日本上市。FLCZ对念珠菌属、曲霉菌属和隐球菌属具有强大的抗真菌活性，口服或静脉给药后可广泛分布于各器官和组织。由于其在成人中的蛋白结合率约为10%，血清半衰期约为30小时，FLCZ已被证明在治疗成人深部真菌病方面高效且有用。在本研究中，我们调查了该药物的新剂型FLCZ颗粒剂以及静脉剂型对患有深部真菌病的儿科患者的临床疗效和抗真菌活性。共有72例患者接受了颗粒剂口服或静脉注射治疗，其中47例患者可对药物的临床疗效进行评估。此外，还对包括早产儿/新生儿在内的儿科患者进行了药代动力学研究，共27例患者采用多剂量方案。念珠菌病的临床有效率为79.5%（44例中的35例），曲霉菌病的临床有效率为100.0%（3例中的3例）。对63例患者评估了该药物的安全性。未观察到副作用。部分患者出现临床实验室检查异常，发生率为9.7%（62例中的6例），但大多数异常仅为轻度且短暂。重复给药后的药代动力学表明，颗粒剂或静脉剂型首次给药后4天达到稳态。从这些结果可以得出结论，FLCZ是治疗儿科患者深部真菌病非常有用的药物。
