Heavner James E
Department of Anesthesiology and Physiology, Texas Technology University Health Sciences Center, Lubbock, TX 79430, USA.
Curr Opin Anaesthesiol. 2007 Aug;20(4):336-42. doi: 10.1097/ACO.0b013e3281c10a08.
Local anesthetics are used in a wide range of clinical situations to prevent acute pain and to stop or ameliorate pain produced by cancer or pain associated with chronic painful conditions. Knowledge of the pharmacology of local anesthetics is essential for their safe use and selection of specific agents to achieve intended goals.
Local anesthetics are a group of drugs defined by their ability to prevent sodium entry into axons, thereby preventing the generation of propagated action potentials in axons. They have other actions, however, such as prevention of axonal sprouting and effects on G-protein-coupled receptors, and on conductance of ions in addition to sodium that might be important in the management of pain. The recent literature focuses on the spectrum of pharmacodynamic actions of local anesthetics, on comparison of pharmacodynamic and pharmacokinetic properties of racemic mixtures versus solutions of pure enantiomer, and on formulations to prolong duration of action. There is new evidence that lipid suspension is useful in the treatment of bupivacaine cardiac toxicity.
Local anesthetics have similar chemical structure but differing pharmacokinetic properties and spectra of pharmacodynamic effects that influence selection of agents for use in various clinical situations.
局部麻醉药在广泛的临床情况下用于预防急性疼痛，并终止或减轻癌症引起的疼痛或与慢性疼痛性疾病相关的疼痛。了解局部麻醉药的药理学知识对于其安全使用以及选择特定药物以实现预期目标至关重要。
局部麻醉药是一类通过阻止钠离子进入轴突从而防止轴突中动作电位传播的药物。然而，它们还有其他作用，如预防轴突发芽以及对G蛋白偶联受体的影响，并且除了钠离子外，还对其他离子的电导有影响，这些在疼痛管理中可能很重要。最近的文献聚焦于局部麻醉药的药效学作用谱、外消旋混合物与纯对映体溶液的药效学和药代动力学特性比较，以及延长作用持续时间的制剂。有新证据表明脂质乳剂可用于治疗布比卡因心脏毒性。
局部麻醉药具有相似的化学结构，但药代动力学特性和药效学效应谱不同，这会影响在各种临床情况下药物的选择。
