Kanto J, Klotz U
Acta Anaesthesiol Scand. 1982 Dec;26(6):554-69. doi: 10.1111/j.1399-6576.1982.tb01817.x.
Despite extensive and numerous pharmacokinetic studies on benzodiazepines, the published pharmacokinetic data do not adequately explain the clinical differences found between different benzodiazepine derivatives after intravenous administration. Especially, correlations between initial drug responses and distributional changes of the benzodiazepines are limited. However, during the elimination phase some relationships exist between the kinetic and dynamic phenomena. Age, sex, diseases and concomitantly given drugs cause clinically important alterations in the pharmacokinetics of benzodiazepines. Generally these anxiolytics and sedatives should be considered as adjuvants to general anaesthesia, but not primarily as routine induction agents. The major reasons for this limitation are a high variability in drug response, a relatively slow onset of action and long-lasting residual effects. However, benzodiazepines have many important advantages (see Table 5) when used as intravenous inducing agents of general anaesthesia.
尽管针对苯二氮䓬类药物进行了广泛且大量的药代动力学研究,但已发表的药代动力学数据并不能充分解释静脉给药后不同苯二氮䓬衍生物之间所发现的临床差异。特别是,苯二氮䓬类药物的初始药物反应与分布变化之间的相关性有限。然而,在消除阶段,动力学和动态现象之间存在一些关系。年龄、性别、疾病以及同时服用的药物会导致苯二氮䓬类药物的药代动力学发生具有临床重要意义的改变。一般来说,这些抗焦虑药和镇静剂应被视为全身麻醉的辅助药物,而不是主要作为常规诱导剂。这种局限性的主要原因是药物反应高度可变、起效相对缓慢以及残留效应持久。然而,当用作全身麻醉的静脉诱导剂时,苯二氮䓬类药物具有许多重要优势(见表5)。