Kapp W
Anasth Intensivther Notfallmed. 1981 Jun;16(3):125-7.
The fact that the benzodiazepines, like the neuroleptic drugs, combine with receptors makes the duration of their combination with the receptors and differences in their affinity to them a matter of great importance. Correlation between the blood levels of the drugs and the duration of their effects obtains only within certain dose limits. Barbiturates inhibit the effect of excitatory mechanisms whereas benzodiazepines enhance the effect of physiological inhibitory mechanisms. The shape of the dose response curve is greatly influenced by the so-called ceiling phenomenon. A new compound of the benzodiazepine family has been developed which holds out hope of better control on account of its pharmacological and pharmacokinetic properties. As it is water-soluble local tolerance is also likely to be improved.
苯二氮䓬类药物与抗精神病药物一样,能与受体结合,这使得它们与受体结合的持续时间以及对受体亲和力的差异变得至关重要。药物血药浓度与作用持续时间之间的相关性仅在特定剂量范围内成立。巴比妥类药物抑制兴奋机制的作用,而苯二氮䓬类药物增强生理抑制机制的作用。剂量反应曲线的形状受所谓的“天花板效应”影响很大。一种新型苯二氮䓬类化合物已被研发出来,鉴于其药理和药代动力学特性,有望实现更好的控制。由于它是水溶性的,局部耐受性也可能得到改善。