Vozeh S
Schweiz Med Wochenschr. 1981 Nov 21;111(47):1789-93.
The elimination half-life of chlordiazepoxide and diazepam increases with age, and this may cause prolongation of action after a single dose and delayed accumulation on multiple dosing in elderly patients. Since the total body clearance of chlordiazepoxide is also reduced, higher steady-state serum concentration is to be expected in patients over 60 years of age. Desmethyldiazepam, one of the active metabolites of diazepam and chlordiazepoxide with a long elimination half-life, also shows impaired elimination in old persons. Prolongation of half-life without changes in total body clearance has been demonstrated for nitrazepam and temazepam. In contrast, oxazepam and lorazepam do not show clinically significant changes of pharmacokinetics with age. The clinical implications of the different pharmacokinetic characteristics are discussed.
氯氮䓬和地西泮的消除半衰期随年龄增长而延长，这可能导致老年患者单次给药后作用时间延长，以及多次给药后延迟蓄积。由于氯氮䓬的全身清除率也降低，预计60岁以上患者的稳态血清浓度会更高。去甲地西泮是地西泮和氯氮䓬的活性代谢产物之一，消除半衰期长，在老年人中其消除也受损。硝西泮和替马西泮已被证明半衰期延长但全身清除率无变化。相比之下，奥沙西泮和劳拉西泮的药代动力学不会随年龄出现具有临床意义的变化。文中讨论了不同药代动力学特征的临床意义。
