1、 2004 By Default 2004 By Default十香软筋散 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default作用机制作用机制时效时效去极化去极化非去极化非去极化超短效超短效短短 效效中中 效效长长 效效肌松药肌松药 2004 By Default 2004 By Default 2004 By Default 2004 By Default离子通道仅在与两个乙离子通道仅在与两个乙酰胆碱分子结合时开放酰胆碱分子结合时开放 2004 By D
2、efaultk+Na+Ca2+k+k+k+k+Na+Ca2+Na+40k40k蛋白亚基蛋白亚基内外 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default相阻滞)2004 By Default二)非竞争性阻滞 1、离子通道阻滞:是由于药物阻塞离子通道,影响离子流通,使终板膜不能正常去极化,从而减弱或阻滞了神经肌肉的兴奋传递 2004 By Default二)非竞争性阻滞 1、离子通道阻滞分为两种:(1)关闭型阻滞:是药物阻塞在离子通道口部,在离子通道关闭时即可发生(2)开放型阻滞:仅在激动药
3、激活开放离子通道后药物才能进入通道内,发挥其阻滞效应,其效应强弱取决于离子通道开放的多少和开放的频率 2004 By Default二)非竞争性阻滞 2、受体脱敏感阻滞:是受体对激动药开放离子通道的作用不敏感,受体虽与激动药结合,但不发生受体蛋白构型的变化,不能使离子通道开放 2004 By Default二)非竞争性阻滞 2、受体脱敏感阻滞:表现:在持续应用激动药时,突触后膜上受体的敏感性进行性下降,受体与激动药的亲和力虽增加,但结合复合物的解离延缓,受体恢复原状的速率减慢 2004 By Default二)非竞争性阻滞 2、受体脱敏感阻滞:结果:脱敏感受体增加可使正常受体总量减少,脱敏感受
4、体增至受体所产生的终板膜电位达不到引起肌纤维收缩的阈值时,则不再发生神经肌肉兴奋传递 2004 By Default作用于突触外和突触前乙酰胆碱受体 2004 By Default作用于突触外和突触前乙酰胆碱受体 2004 By Default25%75%张力减弱95%肌颤搐完全抑制 2004 By Default 2004 By Default阿罗维哌泮0.20.050.30.05-0.06 0.07 2004 By Default 2004 By Default选择性 躯体肌 四肢肌 喉内收肌膈肌 拇内收肌 2004 By Default 2004 By Default 2004 By D
5、efault 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default临床上大剂量或多次重复应用去极化肌松药后,接头后膜神经肌肉阻滞的性质容易发生改变,肌松时间延长,阻滞特征类似于非去极化阻滞 此时已由I相去极
6、化阻滞演变为相阻滞,曾称为双相阻滞或脱敏感阻滞 2004 By Default 相阻滞经历了从快速耐药期到非去极化阻滞期的发展过程 确切发生机制尚不清楚 临床表现为呼吸抑制延长,可有不同程度的衰减和强直后易化现象 至于用抗胆碱酯酶药拮抗相阻滞,目前尚有争议 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Def
7、ault 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default哌库溴铵(pipecuronium)2004 By Default哌库溴铵(pipecuronium)2004 By Default维库溴铵(vecuronium)2004 By Default维库溴铵(vecuronium)2004 By Default维库溴铵(vecuronium)2004 By
8、Default维库溴铵(vecuronium)2004 By Default罗库溴铵(rocuronium)2004 By Default罗库溴铵(rocuronium)2004 By Default阿曲库铵(atracurium)2004 By Default阿曲库铵(atracurium)2004 By Default阿曲库铵(atracurium)2004 By Default顺式阿曲库铵(cis-atracurium)2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default作用机制 2004 By Default不良反应 2004 By Default 2004 By Default图7-8 布瑞亭与罗库溴铵结合 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By Default 2004 By DefaultT T THHHAA ANNNKKKYY YOOOUUUT T THHHAA ANNNKKKYY YOOOUUU