Fisher M A, Shen S H, Haddad J, Tarry W F
Department of Medicine, West Virginia University Health Sciences Center, Morgantown 26506.
Antimicrob Agents Chemother. 1989 Sep;33(9):1443-6. doi: 10.1128/AAC.33.9.1443.
Fluconazole (UK-49,858) is a new oral bis-triazole antifungal agent with demonstrated activity against Candida albicans. Because of the increasing importance of infections due to other species of Candida, we studied the efficacy of fluconazole in a rat model of established systemic candidiasis, using clinical isolates of C. tropicalis, C. glabrata, and C. Krusei. In normal rats, oral fluconazole at both 20 and 80 mg/kg per day for 7 days reduced both kidney and liver titers of C. tropicalis and C. glabrata compared with those in control animals and was only slightly inferior to amphotericin B. Both fluconazole and amphotericin B were ineffective in reducing kidney titers of C. krusei, but amphotericin B was more effective than fluconazole in reducing liver titers. Fluconazole showed no increased efficacy at the higher dose of 80 mg/kg per day compared with 20 mg/kg per day in any experiment. These results suggest that oral fluconazole may be useful in the treatment of established disseminated candidiasis caused by species other than C. albicans. Further in vivo studies are needed, however, to define minimum effective doses and length of therapy and to test additional Candida isolates.
氟康唑（UK - 49,858）是一种新型口服双三唑类抗真菌药物，已证实对白色念珠菌有活性。由于由其他念珠菌属引起的感染日益重要，我们使用热带念珠菌、光滑念珠菌和克柔念珠菌的临床分离株，在已建立的系统性念珠菌病大鼠模型中研究了氟康唑的疗效。在正常大鼠中，每天口服20毫克/千克和80毫克/千克氟康唑，持续7天，与对照动物相比，热带念珠菌和光滑念珠菌在肾脏和肝脏中的菌量均有所减少，且仅略逊于两性霉素B。氟康唑和两性霉素B在降低克柔念珠菌肾脏菌量方面均无效，但两性霉素B在降低肝脏菌量方面比氟康唑更有效。在任何实验中，与每天20毫克/千克的剂量相比，每天80毫克/千克的高剂量氟康唑均未显示出更高的疗效。这些结果表明，口服氟康唑可能对治疗由白色念珠菌以外的其他念珠菌引起的已确诊播散性念珠菌病有用。然而，需要进一步的体内研究来确定最小有效剂量和治疗时长，并测试更多的念珠菌分离株。
