国际麻醉学与复苏杂志   2013, Issue (8): 10-10
    
钙通道阻滞剂的镇痛作用及其机制研究进展
尹晴, 屠伟峰1()
1.广州军区广州总医院
Research progress of analgesic effect and its mechanisms of calcium channel antagonists.
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摘要:

背景 电压依赖性钙通道(voltage dependent calcium channels,VDCCs)参与了疼痛的发生及维持机制,钙通道阻滞剂在临床前及临床试验中显示出良好的镇痛作用。目的 对主要的钙通道阻滞剂的镇痛作用及其机制进行回顾和总结。内容 背根神经节及脊髓背角感受伤害性刺激的神经元上有大量VDCCs分布,可调控去极化诱导的Ca2+内流,从而影响谷氨酸和P物质等与疼痛有关的神经递质释放。Ziconotide等钙通道阻滞剂具有明确的镇痛作用,且不易形成耐受性及引起呼吸抑制,但给药途径受限,治疗窗狭窄。趋向 钙通道阻滞剂的镇痛作用还需进行更深入的研究和探讨,从而开发更加安全方便的新型药物,为临床用药提供更多选择。

关键词: 慢性疼痛;钙通道阻滞剂;镇痛;机制。
Abstract:

Background Voltage dependent calcium channels(VDCCs ) are involved in the mechanism of occurrence and maintenance of pain, calcium channel antagonists show well analgesic effect.Objective Reviewe and summarize the analgesic effect and its mechanisms of main types of calcium channel antagonists.Content Neurons which can feel noxious stimuli distributed in dorsal root ganglia and spinal cord dorsal horn have a large number of VDCCs, can regulate depolarization-induced influx of Ca2+, thus affect the release of glutamate and substance P and other pain-related neurotransmitter. Calcium channel antagonists,such as ziconotide, have a clear analgesic effect and is not easy to form tolerance and cause respiratory depression, but the route of administration is limited,and with narrow therapeutic window. Trend The analgesic effects of calcium channel antagonists need more further research and discussion, in order to develop more convenient and safe drugs, and to provide more choices for the clinical use.

Key words: Chronic pain; Calcium channel antagonists; Analgesia; Mechanism