Jochemsen R, Breimer D D
Acta Psychiatr Scand Suppl. 1986;332:20-31. doi: 10.1111/j.1600-0447.1986.tb08976.x.
When the various benzodiazepine hypnotics are studied, large differences are seen with regard to their pharmacokinetic properties and metabolism in man. Some are eliminated from the body at a relatively slow rate (e.g. nitrazepam), others are metabolized rather rapidly (temazepam, triazolam). Some benzodiazepine hypnotics have major active metabolites that are slowly eliminated (flurazepam, quazepam), while others have non-active metabolites (temazepam, lormetazepam). In hypnotic treatment, the duration of drug action should be restricted to the duration of the night, hence a compound with a relatively short elimination half-life may represent a more rational choice. An overview is given of the pharmacokinetics of the currently available benzodiazepine hypnotics with emphasis on temazepam and other hydroxylated benzodiazepines.
在对各种苯二氮䓬类催眠药进行研究时，发现它们在人体中的药代动力学性质和代谢存在很大差异。有些药物从体内消除的速度相对较慢（如硝西泮），另一些则代谢较快（替马西泮、三唑仑）。一些苯二氮䓬类催眠药有主要的活性代谢产物，这些代谢产物消除缓慢（氟西泮、夸西泮），而另一些则有非活性代谢产物（替马西泮、氯美扎酮）。在催眠治疗中，药物作用时间应限制在夜间，因此消除半衰期相对较短的化合物可能是更合理的选择。本文概述了目前可用的苯二氮䓬类催眠药的药代动力学，重点是替马西泮和其他羟基化苯二氮䓬类药物。
