肌松药拮抗.ppt

plasma concentration of free rocuronium molecules = 0 more rocuronium molecules are bound to Org 25969 Org 25969 molecules are moving into the tissue more rocuronium molecules are bound sugammadex 分子量为 2,178 Daltons ，而rocuronium 是 610 Daltons。 它们的结合是1:1 molar ratio。所以拮抗1 mg of rocuronium 大约需要4 mg (3.57 mg to be exact) of sugammadex 。即如需拮抗rocuronium 0.6 mg·kg–1 大约需要 sugammadex 2.4 mg·kg–1。 但它们的结合是动态的，即在一部分结合时，另一部分在解离。在2 μM sugammadex与2 μM rocuronium结合时，大约20%处于游离状态。但此浓度对一般病人的肌松影响不大，对肌松药敏感的病人就有危险，如重症肌无力病人。可通过增加sugammadex剂量来解决。 ORG 25969 specificity Sugammadex in volunteers 0.1-8.0 mg/kg doses Without prior rocuronium Administered 3 min after rocuronium Neuromuscular measurements Safety Assessments 1.0 mg/kg Org 25969 (23 min) Placebo (45 min) 2.0 mg/kg Org 25969 (13 min) 4.0 mg/kg Org 25969 (3.2 min) TOF recordings after administration of 0.6 mg/kg rocuronium and Org 25969 Gijsenbergh F, et al. 2002 ASA Meeting　A-1008 Rocuronium 0.6 mg/kg Time of antagonism: Appearance of T2 Dose of sugammadex Placebo, 0.5, 1.0, 2.0, 3.0 or 4.0 mg/kg Sugammadex 4 mg/kg Placebo Rocuronium 0.6 mg/kg followed by sugammadex at reappearance of T2 21 4.3 3.3 1.3 1.2 1.1 对深度阻滞的拮抗作用 Miller等研究其拮抗深度神经肌肉阻滞作用，环糊精与新斯的明拮抗罗库溴铵产生90%阻滞（ED90）和深度阻滞（3×ED90）的拮抗作用不同。T1抑制90%的阻滞，环糊精和新斯的明都有拮抗作用，而3×ED90深度阻滞只有环糊精能拮抗，而新斯的明即使给予很高剂量效果仍不明显。 Rocuronium 0.6 mg/kg followed by increments to maintain deep block at 10 PTCs Reversal after 2hrs of deep block at recovery of T2 Doses of Org 25969 0.5, 1.0, 2.0, 4.0 and 6.0 mg/kg Times to TOF ratio of 0.9 with reversal at T2 after deep block for 2 hours Dose (mg/kg) Time (Median (range)) 0.5 5:29 (4:50-11:26) 1.0 2:42 (1:49-3:40) 2.0 1:46 (1:00-2:31) 4.0 1:04 (0:57-2:19) 6.0 2:41 (1:08-3:56) 肌松药的拮抗与Sugammadex 南京医科大学一附院 麻醉科 刘存明 Australia近20年麻醉死亡的主要原因之－ 是残余肌松作用拮抗不全 残余肌松作用 是麻醉恢复期的杀手 ! Tiret(法国） 20万例全麻病人中，麻醉死亡65例。