局部麻醉药的研究进展

局部麻醉药的研究进展

摘要

局部麻醉药是一类能在用药局部可逆性地阻断感觉神经冲动发生与传导的药物。一般来说，局麻药液的浓度决定阻滞的性质和范围。但是局麻药除了局部麻醉作用外，还会产生一定的吸收作用。目前的局部麻醉需小剂量频繁给药以维持有效治疗浓度。剂量较大时，有效治疗浓度的维持时间长，但最大血药浓度Cmax超出治疗窗，导致副反应。如:局麻药吸收入血并达到一定浓度，产生毒性反应，作用于中枢神经系统，表现为神志错乱，肌肉震颤等。而剂量过小则不能有效缓解患者病痛。另外局麻药有不同程度的扩展外周血管的作用，使药物经血管吸收加速，作用时间缩短。近年来，针对局麻药在临床应用中存在的问题以及临床治疗需要缓释的长效局部麻醉制剂来缓患者术中、术后、癌症和神经系统疾病引起的各种疼痛。采用现代制剂技术设计了各种缓释给药系统，来延缓药物在体内的释放和吸收，旨在延长局麻药效，减少体循环吸收，减轻不良反应，从而提高药物的治疗指数。

关键词：局部麻醉药无痛研究发展

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Abstract

In drug called is familiar to everyone，with health care，medical treatment，diagnosis of A local anesthetic is a kind of can in topical reversible to blocking sensory nerve impulse generation and conduction of drug. Generally, the concentration of local anesthetic solution decide the nature and scope of the block. But local anesthetics in addition to the local anaesthesia effect, will produce certain absorption. Current topical anesthesia for small dose frequently administered to maintain the effective therapeutic concentration. Dose is large, effective therapeutic concentration to maintain a long time, but the maximum plasma concentration Cmax beyond therapeutic window, resulting in adverse reactions. Such as: local anesthetic absorption into the blood and reached a certain concentration, toxicity, in the central nervous system, for the mental disorder, muscle tremors. And dosage is too small can effectively relieve the pain of patients. Also local anesthetics have of varying degrees of expansion of peripheral vascular, the drug by vascular absorption speed, shorten the time. In recent years, according to local anesthetics in the clinical application of existing problems and clinical treatment need for controlled release of long-acting local anesthetized preparations to relieve patients, after operation, pain caused by cancer, and diseases of the nervous system. The modern preparation technology design a variety of sustained release drug delivery system, to delay the drug in vivo release and absorption, seeks to extend the anesthetic efficacy and reduce systemic absorption, reduce adverse reaction, so as to improve the therapeutic index.

Key words: local anesthetics, painless, research and development

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目录

摘要..................................................................................................................................... I Abstract .............................................................................................................................. I I 1. 心脏钠通道与局部麻醉药的研究进展 (4)

1.1心脏钠通道的状态对局部麻醉药作用的影响 (4)

1.2 钠通道上局部麻醉药的结合部位 (4)

2 局部麻醉药新型剂的研究[3] (5)

2.1 局部麻醉药微球 (5)

2.2 局部麻醉药脂质体:脂质体具有以下特点 (5)

2.3 局部麻醉药乳剂 (5)

2.4 局部麻醉药微型胶囊 (5)

3 神经系统与局部麻醉药的研究 (6)

3.1 中枢神经系统反应:中枢神经系统局部麻醉药的作用 (6)

3.2 心血管系统局部麻醉药对之有直接抑制作用 (6)

4. 参考文献 (7)

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