Department of Anaesthesiology and Intensive Care, University of Debrecen Clinical Center, Nagyerdei krt. 98, 4012, Debrecen, Hungary.
Cyclolab Ltd, Budapest, Hungary.
BMC Anesthesiol. 2021 Aug 17;21(1):206. doi: 10.1186/s12871-021-01424-4.
Residual neuromuscular block at the end of surgery may compromise the patient's safety. The risk of airway complications can be minimized through monitoring of neuromuscular function and reversal of neuromuscular block if needed. Effective reversal can be achieved with selective relaxant binding agents, however, sugammadex is the only clinically approved drug in this group. We investigated the concentration-response properties of a novel selective relaxant binding agent, carboxymethyl-γ-cyclodextrin for the reversal of neuromuscular block. We evaluated the hypothesis that it is equally potent for reversing neuromuscular block as sugammadex.
Phrenic nerve - hemidiaphragm tissue preparations were isolated from male Wistar rats and suspended in a tissue holder allowing electrical stimulation of the nerve and monitoring of muscle contraction force. Concentration-response relationships were constructed for the neuromuscular blocking agents rocuronium, pipecuronium, and vecuronium. The half-effective concentrations of sugammadex and carboxymethyl-γ-cyclodextrin for reversal of neuromuscular block were determined.
The half effective concentrations (95% confidence interval, CI) were 7.50 (6.93-8.12) μM for rocuronium, 1.38 (1.33-1.42) μM for pipecuronium, and 3.69 (3.59-3.80) μM for vecuronium. The half effective concentrations (95% CI) of carboxymethyl-γ-cyclodextrin and sugammadex were 35.89 (32.67-39.41) μM and 3.67 (3.43-3.92) μM, respectively, for the reversal of rocuronium-induced block; 10.14 (9.61-10.70) μM and 0.67 (0.62-0.74) μM, respectively, for the reversal of pipecuronium-induced block; and 376.1 (341.9-413.8) μM and 1.45 (1.35-1.56) μM, respectively, for the reversal of vecuronium-induced block.
Carboxymethyl-γ-cyclodextrin is an effective, but less potent agent for reversal of neuromuscular block than sugammadex.
手术结束时残留的神经肌肉阻滞可能危及患者安全。通过监测神经肌肉功能和必要时逆转神经肌肉阻滞，可以将气道并发症的风险降至最低。选择性松弛剂结合剂可实现有效逆转，但在该类药物中，只有 sugammadex 是唯一经临床批准的药物。我们研究了一种新型选择性松弛剂结合剂羧甲基 -γ-环糊精逆转神经肌肉阻滞的浓度 - 反应特性。我们假设它与 sugammadex 一样具有同等的逆转神经肌肉阻滞的效力。
从雄性 Wistar 大鼠中分离出膈神经 - 半膈肌组织标本，并将其悬挂在组织固定器中，允许神经电刺激和监测肌肉收缩力。构建了神经肌肉阻滞剂罗库溴铵、哌库溴铵和维库溴铵的浓度 - 反应关系。确定了逆转神经肌肉阻滞的 sugammadex 和羧甲基 -γ-环糊精的半有效浓度。
罗库溴铵的半有效浓度（95%置信区间，CI）为 7.50（6.93-8.12）μM，哌库溴铵为 1.38（1.33-1.42）μM，维库溴铵为 3.69（3.59-3.80）μM。羧甲基 -γ-环糊精和 sugammadex 逆转罗库溴铵诱导阻滞的半有效浓度（95%CI）分别为 35.89（32.67-39.41）μM 和 3.67（3.43-3.92）μM，逆转哌库溴铵诱导阻滞的半有效浓度（95%CI）分别为 10.14（9.61-10.70）μM 和 0.67（0.62-0.74）μM，逆转维库溴铵诱导阻滞的半有效浓度（95%CI）分别为 376.1（341.9-413.8）μM 和 1.45（1.35-1.56）μM。
羧甲基 -γ-环糊精是一种有效的神经肌肉阻滞逆转剂，但效力不如 sugammadex。
