Nikaido A M, Ellinwood E H
Psychopharmacology (Berl). 1987;92(4):459-64. doi: 10.1007/BF00176478.
The pharmacological activity of quazepam, a BZ1 specific benzodiazepine, was compared to the effects of triazolam, a BZ1, BZ2 nonspecific benzodiazepine. Using a double-blind procedure, single oral doses of quazepam (15 or 30 mg), triazolam (0.5 or 1.0 mg) and placebo were administered to 21 healthy young men according to a random Latin square design balanced for order of drug administration. The drug effects on the performance of motor coordination and cognitive tasks were monitored for 7 h following drug ingestion. The results did not indicate any differential effects on cognitive-neuromotor performance for the BZ1 specific quazepam and 2-oxoquazepam compared with the BZ1, BZ2 nonspecific N-desalkylflurazepam metabolite. The impairment magnitude for 30 mg quazepam was closer to that of 0.5 mg triazolam. The onset of the initial drug effect was considerably slower for quazepam than for triazolam. The time course of the impairment profiles for the tasks was compared to pharmacokinetic data from previous studies and suggested that published pharmacokinetic rate constants explain only a limited portion of the impairment time course. In particular, the performance scores were already showing recovery from peak impairment 2 h post-drug ingestion, although quazepam's potent N-desalkylflurazepam metabolite has been found to maintain a maximum plateau level from 2 to 24 h.
将BZ1特异性苯二氮䓬类药物夸西泮的药理活性与BZ1、BZ2非特异性苯二氮䓬类药物三唑仑的作用进行了比较。采用双盲程序，根据药物给药顺序平衡的随机拉丁方设计，对21名健康年轻男性单次口服夸西泮（15或30毫克）、三唑仑（0.5或1.0毫克）和安慰剂。在服药后7小时监测药物对运动协调和认知任务表现的影响。结果表明，与BZ1、BZ2非特异性N-去烷基氟西泮代谢物相比，BZ1特异性夸西泮和2-氧代夸西泮对认知-神经运动表现没有任何差异影响。30毫克夸西泮的损害程度更接近0.5毫克三唑仑。夸西泮初始药物作用的起效时间比三唑仑慢得多。将任务损害情况的时间进程与先前研究的药代动力学数据进行比较，结果表明，已发表的药代动力学速率常数仅能解释损害时间进程的有限部分。特别是，尽管已发现夸西泮的强效N-去烷基氟西泮代谢物在2至24小时内维持最大平台水平，但服药后2小时性能分数就已从峰值损害开始恢复。
