Donati F, McCarroll S M, Antzaka C, McCready D, Bevan D R
Anesthesiology. 1987 Apr;66(4):471-6. doi: 10.1097/00000542-198704000-00004.
To determine the potencies of neostigmine, pyridostigmine, and edrophonium in reversing pancuronium and d-tubocurarine blockade, dose-response curves were established for first twitch height recovery and train-of-four ratio. One hundred and twenty ASA physical status I or II patients scheduled for elective surgery received either 0.06 mg/kg pancuronium or 0.36 mg/kg d-tubocurarine during a thiopental-nitrous oxide-enflurane anesthetic. Train-of-four stimulation was applied every 12 s, and the force of contraction of the adductor pollicis muscle was recorded. When first twitch height had recovered spontaneously to 10% of its initial value, neostigmine (0.005, 0.01, 0.02 or 0.05 mg/kg), pyridostigmine (0.02, 0.04, 0.1, or 0.2 mg/kg), or edrophonium (0.1, 0.2, 0.4 or 1 mg/kg) was injected by random allocation. Recovery was measured 10 min after the injection of the antagonist. First twitch ED50's were 0.013, 0.085, and 0.17 mg/kg after pancuronium, and 0.017, 0.11, and 0.27 mg/kg after d-tubocurarine, for neostigmine, pyridostigmine, and edrophonium, respectively. The ED50 for pyridostigmine and edrophonium obtained after d-tubocurarine was significantly larger (P less than 0.05) than that after pancuronium. The train-of-four dose-response curves were significantly flatter for edrophonium than for the other two agents, indicating a greater ability of edrophonium to antagonize fade at low doses. It is concluded that the potency of reversal agents may be different for different relaxants, and that potency ratios might depend upon the end-point chosen as full neuromuscular recovery.
为了确定新斯的明、吡啶斯的明和依酚氯铵逆转泮库溴铵和筒箭毒碱阻滞作用的效能,建立了首次颤搐高度恢复和四个成串刺激比值的剂量-反应曲线。120例拟行择期手术的ASAⅠ或Ⅱ级患者,在硫喷妥钠-氧化亚氮-安氟醚麻醉期间,给予0.06mg/kg泮库溴铵或0.36mg/kg筒箭毒碱。每12秒施加一次四个成串刺激,并记录拇内收肌的收缩力。当首次颤搐高度自发恢复至其初始值的10%时,随机给予新斯的明(0.005、0.01、0.02或0.05mg/kg)、吡啶斯的明(0.02、0.04、0.1或0.2mg/kg)或依酚氯铵(0.1、0.2、0.4或1mg/kg)。注射拮抗剂10分钟后测量恢复情况。新斯的明、吡啶斯的明和依酚氯铵在泮库溴铵后的首次颤搐ED50分别为0.013、0.085和0.17mg/kg,在筒箭毒碱后的首次颤搐ED50分别为0.017、0.11和0.27mg/kg。筒箭毒碱后获得的吡啶斯的明和依酚氯铵的ED50显著大于(P<0.05)泮库溴铵后的ED50。依酚氯铵的四个成串刺激剂量-反应曲线比其他两种药物明显更平坦,表明依酚氯铵在低剂量时拮抗衰减的能力更强。得出的结论是,不同的肌松拮抗剂对不同的肌松药的效能可能不同,效能比值可能取决于选择作为完全神经肌肉恢复的终点。