西咪替丁导致咖啡因的全身清除率降低。
Decreased systemic clearance of caffeine due to cimetidine.
作者信息
Broughton L J, Rogers H J
出版信息
Br J Clin Pharmacol. 1981 Aug;12(2):155-9. doi: 10.1111/j.1365-2125.1981.tb01194.x.
Abstract
1 Five normal subjects received pre-treatment with cimetidine 200 mg three times daily and 400 mg at night for 6 days, or matching placebo. 2 Caffeine (300 mg) was given orally before any treatment and at the beginning of the last day of each treatment course. Treatments were randomly allocated and separated by at least one week. 3 A significant reduction occurred in the systemic clearance of caffeine and the half-life was prolonged as determined from measurement of caffeine in plasma and saliva. No change occurred in the apparent volume of distribution. 4 The oral bioavailability of caffeine was found to be complete in the one subject studied. 5 It is suggested that cimetidine inhibits the microsomal metabolism of caffeine. Although the steady state plasma caffeine would increase by approximately 70%, it is unlikely that this would produce adverse clinical effects.
摘要
五名正常受试者接受了西咪替丁预处理，每日三次，每次200毫克，夜间400毫克，共6天，或服用匹配的安慰剂。
在任何治疗前以及每个治疗疗程最后一天开始时口服给予咖啡因（300毫克）。治疗随机分配，且间隔至少一周。
根据血浆和唾液中咖啡因的测量结果，咖啡因的全身清除率显著降低，半衰期延长。分布容积无变化。
在研究的一名受试者中发现咖啡因的口服生物利用度是完全的。
提示西咪替丁抑制咖啡因的微粒体代谢。虽然稳态血浆咖啡因会增加约70%，但这不太可能产生不良临床影响。
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