Aeschbacher H U, Atkinson J, Domahidy B
J Pharmacol Exp Ther. 1975 Mar;192(3):635-41.
The effect of caffeine and coffee on the sleeping time induced by barbital was tested in rats. It was found that caffeine pretreatment shortened barbital-induced sleeping time and that coffee had an effect in direct proportion to its caffeine content; decaffeinated coffee was without effect. It was hypothesized that the shortening was due to an interaction at the brain level. This hypothesis was tested using hexobarbital which is metabolized by the liver whereas barbital is only negligibly so metabolized. Pretreatment with caffeine was found to shorten the hexobarbital sleeping time even though the brain concentration of the latter was actually elevated. It was also shown that caffeine pretreatment was much less effective than phenobarbital pretreatment in stimulating the enzyme systems in the liver which metabolize hexobarbital, aminopyrine and ethylmorphine (in vitro). Consequently, it is concluded that caffeine stimulation of liver metabolism is a relatively minor factor in the shortening of barbiturate sleeping time by caffeine in comparison to the brain interaction of these two drugs.
在大鼠身上测试了咖啡因和咖啡对巴比妥诱导睡眠时间的影响。结果发现，咖啡因预处理可缩短巴比妥诱导的睡眠时间，且咖啡的作用与其咖啡因含量成正比；脱咖啡因咖啡则无此作用。据推测，睡眠时间缩短是由于在大脑水平上的相互作用所致。使用己巴比妥对这一假设进行了验证，己巴比妥由肝脏代谢，而巴比妥的肝脏代谢量可忽略不计。结果发现，即使己巴比妥的脑内浓度实际上有所升高，咖啡因预处理仍可缩短己巴比妥的睡眠时间。研究还表明，在体外刺激肝脏中代谢己巴比妥、氨基比林和乙基吗啡的酶系统方面，咖啡因预处理的效果远不如苯巴比妥预处理。因此，得出结论，与这两种药物在大脑中的相互作用相比，咖啡因对肝脏代谢的刺激在咖啡因缩短巴比妥睡眠时间方面是一个相对次要的因素。
