CAJ | 학술논문

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(dorsal root ganglia,DRG)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.齐考诺肽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.
배경 전압의뢰성개통도(voltage dependent calcium channels,VDCCs)삼여료동통적발생급유지궤제,개통도조체제재림상전급림상시험중현시출량호적진통작용. 목적 대주요적개통도조체제적진통작용급기궤제진행회고화총결. 내용 배근신경절(dorsal root ganglia,DRG)급척수배각감수상해성자격적신경원상유대량VDCCs분포,가조공거겁화유도적Ca2+내류,종이영향곡안산화P물질등여동통유관적신경체질석방.제고낙태등개통도조체제구유명학적진통작용,차불역형성내수성급인기호흡억제,단급약도경수한,치료창협착. 추향 개통도조체제적진통작용환수진행경심입적연구화탐토,종이개발경가안전방편적신형약물,위림상용약제공경다선택.
Background Voltage-dependent calcium channels (VDCCs) are involved in the mechanism of occurrence and maintenance of pain,calcium channel blockers show well analgesic effect.Objective To review and summarize the analgesic effect and its mechanisms of main types of calcium channel blockers.Content Neurons which can feel noxious stimuli distributed in dorsal root ganglia (DRG) 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 blockers,such as Ziconotide,have a clear analgesic effect and are not easy to form tolerance and cause respiratory depression,but the routes of administration are limited,and therapeutic window narrow.Trend In order to develop more convenient and safe drugs,and to provide more choices for the clinical use,the analgesic effect of calcium channel blockers needs more further research and discussion.