Bruce M, Scott N, Lader M, Marks V
Br J Clin Pharmacol. 1986 Jul;22(1):81-7. doi: 10.1111/j.1365-2125.1986.tb02883.x.
The effects of single doses of anhydrous caffeine (250 mg and 500 mg) and placebo on physiological, psychological measures and subjective feelings were studied in a double-blind, cross-over study in nine healthy subjects who had abstained from caffeine-containing beverages for 24 h before each occasion. Caffeine and caffeine metabolites in plasma and urine were assayed. Peak plasma concentrations were observed at 1 to 2 h with an approximate half-life of 5 h. The concentrations of the metabolite 1,7-dimethylxanthine increased during the 5 h. The major urine metabolite was 1-methyluric acid. The EEG showed a dose-related decrease in log 'theta' power and a decrease in log 'alpha' power. Other dose-related effects were an increase in skin conductance level (sweat-gland activity) and self rating of alertness. Ratings of headache and tiredness were decreased by the caffeine. The study illustrates the complexities of studying a drug which is widely taken and which is often associated with withdrawal effects.
在一项双盲交叉研究中,对9名健康受试者进行了研究,观察单剂量无水咖啡因(250毫克和500毫克)及安慰剂对生理、心理指标和主观感受的影响。这些受试者在每次试验前24小时都未饮用含咖啡因的饮料。检测了血浆和尿液中的咖啡因及咖啡因代谢物。血浆浓度在1至2小时达到峰值,半衰期约为5小时。代谢物1,7 - 二甲基黄嘌呤的浓度在5小时内升高。主要的尿液代谢物是1 - 甲基尿酸。脑电图显示,“θ”波功率对数和“α”波功率对数呈剂量相关下降。其他剂量相关效应包括皮肤电导水平(汗腺活动)增加和警觉性自评升高。咖啡因降低了头痛和疲劳的评分。该研究说明了研究一种广泛使用且常伴有戒断效应的药物的复杂性。