Covino B G
Br J Anaesth. 1986 Jul;58(7):701-16. doi: 10.1093/bja/58.7.701.
The most important clinical properties of local anaesthetic agents are potency, onset, duration of action and relative blockade of sensory and motor fibres. These qualities are related primarily to the physicochemical properties of the various compounds. In general, lipid solubility determines the relative intrinsic potency of the various agents, while protein binding influences the duration of anaesthesia and pKa is correlated with the onset of action. In general, the local anaesthetics for infiltration, peripheral nerve blockade, and extradural anaesthesia can be classified into three groups: agents of low potency and short duration, for example procaine and chloroprocaine; agents of moderate potency and duration, for example lignocaine, mepivacaine and prilocaine; and agents of high potency and long duration, for example amethocaine, bupivacaine and etidocaine. These local anaesthetics also vary in terms of onset: chloroprocaine, lignocaine, mepivacaine, prilocaine and etidocaine have a rapid onset, while procaine, amethocaine and bupivacaine are characterized by a longer latency period.
局部麻醉药最重要的临床特性包括效能、起效时间、作用持续时间以及对感觉和运动纤维的相对阻滞作用。这些特性主要与各种化合物的物理化学性质有关。一般来说,脂溶性决定了各种药物的相对内在效能,而蛋白质结合影响麻醉持续时间,pKa与起效时间相关。一般而言,用于浸润麻醉、外周神经阻滞和硬膜外麻醉的局部麻醉药可分为三类:低效和短效药物,如普鲁卡因和氯普鲁卡因;中效和中时药物,如利多卡因、甲哌卡因和丙胺卡因;高效和长效药物,如丁卡因、布比卡因和依替卡因。这些局部麻醉药在起效方面也有所不同:氯普鲁卡因、利多卡因、甲哌卡因、丙胺卡因和依替卡因起效迅速,而普鲁卡因、丁卡因和布比卡因的潜伏期较长。