克霉唑（拜耳b 5097）：体外及临床药理学研究。
Clotrimazole (Bay b 5097): in vitro and clinical pharmacological studies.
作者信息
Burgess M A, Bodey G P
出版信息
Antimicrob Agents Chemother. 1972 Dec;2(6):423-6. doi: 10.1128/AAC.2.6.423.
Abstract
Clotrimazole (Bay b 5097) is a new synthetic antifungal drug with in vitro activity against Candida spp., Torulopsis glabrata, and Saccharomyces spp. Pharmacological studies in man after the oral administration of 1.5 and 3 g of clotrimazole produced mean peak concentrations in the serum of 1.16 and 1.29 mug/ml, respectively, 2 hr after administration. In six patients taking 1.5 g of clotrimazole every 6 hr, there was a progressive decline in the serum concentrations after administration of a dose on days 1, 4, and 8. Nine other patients begun on a similar schedule manifested gastrointestinal symptoms attributed to the clotrimazole and were unable to complete the study. Concentrations of active drug in the urine were less than 1% of the administered dose.
摘要
克霉唑（拜耳b 5097）是一种新型合成抗真菌药物，对念珠菌属、光滑球拟酵母菌和酿酒酵母属具有体外活性。口服1.5克和3克克霉唑后，人体药理学研究显示给药后2小时血清中的平均峰值浓度分别为1.16微克/毫升和1.29微克/毫升。在6名每6小时服用1.5克克霉唑的患者中，在第1天、第4天和第8天给药后血清浓度呈逐渐下降趋势。另外9名开始采用类似给药方案的患者出现了归因于克霉唑的胃肠道症状，无法完成研究。尿液中活性药物的浓度低于给药剂量的1%。
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