Welliver Mark, McDonough John, Kalynych Nicholas, Redfern Robert
Nurse Anesthetist Program, Department ofAnesthesiology, University of North Florida, 655 West 8th Street, Jacksonville, FL 32209, USA.
Drug Des Devel Ther. 2009 Feb 6;2:49-59. doi: 10.2147/dddt.s2757.
Neuromuscular blockade, induced by neuromuscular blocking agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking agents. Sugammadex sodium is the first in a new class of drug called selective relaxant binding agents. Currently, in clinical trials, sugammadex, a modified gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential perioperative benefits.
神经肌肉阻滞剂诱导的神经肌肉阻滞能够实现规定的制动，改善手术视野，创造最佳气道管理条件，并便于机械通气。然而，迄今为止，神经肌肉阻滞剂作用的终止仍受到限制。一种新型环糊精包封工艺可更好地终止氨基甾体类非去极化神经肌肉阻滞剂的麻痹作用。舒更葡糖钠是一类名为选择性肌松药结合剂的新型药物中的首个药物。目前，在临床试验中，舒更葡糖（一种改性γ-环糊精）已显示出能持续且迅速地终止神经肌肉阻滞，且副作用极少。本文综述了环糊精尤其是舒更葡糖的药理学以及当前临床研究结果。将舒更葡糖通过直接包封终止神经肌肉阻滞剂作用的能力与胆碱酯酶抑制剂对其作用的间接竞争性拮抗作用进行了比较。还讨论了除快速、有效逆转之外的临床意义，包括众多潜在的围手术期益处。
