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舒更葡糖钠,首个用于逆转神经肌肉阻滞的选择性肌松药结合剂。

Sugammadex, the first selective relaxant binding agent for neuromuscular block reversal.

作者信息

Stair C, Fernandez-Bustamante A

机构信息

Department of Anesthesiology, University of Colorado Denver, Aurora, Colorado, USA.

出版信息

Drugs Today (Barc). 2012 Jun;48(6):405-13. doi: 10.1358/dot.2012.48.6.1813474.

Abstract

Neuromuscular blocking agents (NMBAs) are widely used to provide muscle relaxation for endotracheal intubation, certain modes of mechanical ventilation and surgical procedures. Full and rapid reversal of this muscle relaxation is needed to prevent residual muscle paralysis and respiratory compromise. The novel selective reversal binding agent, sugammadex, rapidly reverses muscle paralysis from steroidal NMBAs. Sugammadex encapsulates steroidal NMBAs in the plasma and renders them unavailable to the neuromuscular junction receptors. Unlike other reversal agents, sugammadex has the ability to provide fast and thorough reversal of neuromuscular paralysis regardless of the level of blockade. Sugammadex has shown limited adverse effects and avoids the cardiovascular and autonomic effects commonly seen with the conventional reversal of NMBAs (anticholinesterase plus anticholinergic). This review summarizes the current knowledge about sugammadex, its pharmacology and safety profile, dosing recommendations, potential clinical applications and economic impact.

摘要

神经肌肉阻滞剂(NMBAs)被广泛用于为气管插管、某些机械通气模式和外科手术提供肌肉松弛作用。需要完全且快速地逆转这种肌肉松弛,以防止残留肌肉麻痹和呼吸功能受损。新型选择性逆转结合剂舒更葡糖能迅速逆转甾体类NMBAs所致的肌肉麻痹。舒更葡糖在血浆中包裹甾体类NMBAs,使其无法作用于神经肌肉接头受体。与其他逆转剂不同,无论阻滞程度如何,舒更葡糖都能快速、彻底地逆转神经肌肉麻痹。舒更葡糖已显示出有限的不良反应,并且避免了传统NMBAs逆转(抗胆碱酯酶加抗胆碱能药物)常见的心血管和自主神经效应。本综述总结了关于舒更葡糖的现有知识,包括其药理学、安全性概况、给药建议、潜在临床应用和经济影响。

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