Mamelak M, Bunting P, Galin H, Price V, Csima A, Young T, Klein D, Pelchat J R
Sleep Disorders Centre, Sunnybrook Medical Centre, University of Toronto, Ontario, Canada.
J Clin Pharmacol. 1988 Apr;28(4):376-83. doi: 10.1002/j.1552-4604.1988.tb03162.x.
This study was undertaken to determine the serum pharmacokinetic parameters of loprazolam, a new benzodiazepine hypnotic, in elderly subjects and to compare these with the kinetics of the drug as determined by quantitative EEG analysis. In addition, a 14-day study was undertaken to determine the steady-state serum levels achieved in this population with repeated drug administration. The study was conducted on 16 male and female subjects between the ages of 62 and 72 years, randomly assigned to two groups treated with 0.5 or 1.0 mg of loprazolam. The serum half-life of loprazolam was found to be 5 hours, and the peak serum concentration was reached after 2 hours. Quantitative EEG changes were observed after 30 minutes suggesting rapid access of the drug into the nervous system. Quantitative EEG changes were evident for 9.5 hours, suggesting the persistent effects of an active metabolite. The 14-day study indicated that loprazolam did not accumulate with continued use.
本研究旨在测定新型苯二氮䓬类催眠药氯普唑仑在老年受试者中的血清药代动力学参数，并将其与通过定量脑电图分析所确定的药物动力学进行比较。此外，还进行了一项为期14天的研究，以确定该人群重复给药后达到的稳态血清水平。该研究针对16名年龄在62至72岁之间的男性和女性受试者进行，他们被随机分为两组，分别接受0.5毫克或1.0毫克氯普唑仑治疗。结果发现氯普唑仑的血清半衰期为5小时，给药后2小时达到血清峰值浓度。30分钟后观察到定量脑电图变化，表明药物迅速进入神经系统。定量脑电图变化在9.5小时内明显，表明活性代谢物具有持续作用。为期14天的研究表明，氯普唑仑持续使用不会蓄积。
