Next generation of neuromuscular blockade reversal agents.

IF 2.3 3区医学 Q2 ANESTHESIOLOGY

Current Opinion in Anesthesiology Pub Date : 2025-03-25 DOI:10.1097/ACO.0000000000001485

Hans D de Boer, Ricardo Vieira Carlos

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引用次数: 0

Abstract

Purpose of the review: The purpose of this review is to explore emerging pharmacological strategies for neuromuscular blockade (NMB) reversal, focusing on their mechanisms of action, efficacy, and potential advantages over existing agents like sugammadex and neostigmine.

Recent findings: Several novel reversal agents are under investigation: calabadions, synthetic molecular containers that effectively reverse aminosteroidal and benzylisoquinolinium neuromuscular blocking agents (NMBAs) with rapid clearance; l-cysteine adduction, a promising method for reversing ultrashort-acting NMBAs by accelerating metabolism; adamgammadex, a modified γ-cyclodextrin with improved binding to rocuronium and reduced hypersensitivity risks, showing noninferiority to sugammadex; acyclic cucurbit[n]urils, broad-spectrum reversal agents with superior water solubility and biocompatibility; and ClC-1 channel blockers, a novel approach that enhances muscle excitability rather than directly binding to NMBAs.

Summary: Emerging NMBA reversal agents offer potential improvements in safety, efficacy, and broader NMBA compatibility. These alternatives to sugammadex and neostigmine show promise in preclinical and early clinical trials. Further studies are necessary to confirm their clinical applicability and regulatory approval.

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综述的目的：本综述旨在探讨新出现的神经肌肉阻滞（NMB）逆转药理策略，重点关注其作用机制、疗效以及与现有药物（如苏加麦考酚酯和新斯的明）相比的潜在优势：目前正在研究几种新型逆转剂：calabadions，一种合成分子容器，可有效逆转氨基甾醇类和苄基异喹啉类神经肌肉阻滞剂（NMBA），并能快速清除；l-半胱氨酸诱导，一种通过加速新陈代谢逆转超短效神经肌肉阻滞剂（NMBA）的有前途的方法；adamgammadex，一种改良的 γ-环糊精，可改善与罗库溴铵的结合，降低超敏风险，与苏甘麦得相比无劣势；无环葫芦[n]脲，一种广谱逆转剂，具有优异的水溶性和生物相容性；以及 ClC-1 通道阻断剂，一种增强肌肉兴奋性而非直接与 NMBAs 结合的新方法。摘要：新出现的 NMBA 逆转剂在安全性、有效性和更广泛的 NMBA 兼容性方面都有潜在的改进。在临床前和早期临床试验中，这些替代苏甘麦角和新斯的明的药物显示出了前景。要确认它们的临床适用性并获得监管部门的批准，还需要进一步的研究。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current Opinion in Anesthesiology 医学-麻醉学

CiteScore

4.90

自引率

8.00%

发文量

207

审稿时长

12 months

期刊介绍： Published bimonthly and offering a unique and wide ranging perspective on the key developments in the field, each issue of Current Opinion in Anesthesiology features hand-picked review articles from our team of expert editors. With fifteen disciplines published across the year – including cardiovascular anesthesiology, neuroanesthesia and pain medicine – every issue also contains annotated references detailing the merits of the most important papers.