Chung M, Hilbert J M, Gural R P, Radwanski E, Symchowicz S, Zampaglione N
Clin Pharmacol Ther. 1984 Jun;35(6):838-42. doi: 10.1038/clpt.1984.122.
Halazepam is a benzodiazepine used in the management of anxiety disorders or short-term relief of anxiety. Our study was undertaken to evaluate its steady-state kinetics and those of its major active plasma metabolite N- desalkylhalazepam . Eleven healthy men aged 19 to 35 yr were given oral, 40-mg halazepam tablets every 8 hr for 14 days. Plasma samples were analyzed by gas chromatography to determine levels of halazepam and N- desalkylhalazepam . Halazepam kinetics can best be described by a two-compartment open model with first-order absorption kinetics. The elimination phase t1/2s of halazepam and N- desalkylhalazepam were 34.7 and 57.9 hr. Steady-state levels were predictable from kinetic data and were reached by the third day for halazepam and by the eleventh day for N- desalkylhalazepam .
哈拉西泮是一种苯二氮䓬类药物，用于治疗焦虑症或短期缓解焦虑。我们进行这项研究是为了评估其稳态动力学以及其主要活性血浆代谢物N-去烷基哈拉西泮的稳态动力学。11名年龄在19至35岁的健康男性，每8小时口服40毫克哈拉西泮片，共服用14天。通过气相色谱法分析血浆样本，以测定哈拉西泮和N-去烷基哈拉西泮的水平。哈拉西泮的动力学最好用具有一级吸收动力学的二室开放模型来描述。哈拉西泮和N-去烷基哈拉西泮的消除相半衰期分别为34.7小时和57.9小时。稳态水平可根据动力学数据预测，哈拉西泮在第三天达到稳态水平，N-去烷基哈拉西泮在第十一天达到稳态水平。
