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逆转神经肌肉阻滞:乙酰胆碱酯酶抑制剂与包封剂舒更葡糖钠和卡拉巴多因的比较

Reversing neuromuscular blockade: inhibitors of the acetylcholinesterase versus the encapsulating agents sugammadex and calabadion.

作者信息

Haerter Friederike, Eikermann Matthias

机构信息

a Department of Anesthesia, Critical Care and Pain Medicine , Massachusetts General Hospital and Harvard Medical School , Boston , MA , USA.

b Department of Anesthesia and Critical Care Medicine , University Hospital Essen, University Duisburg-Essen , Essen , Germany.

出版信息

Expert Opin Pharmacother. 2016;17(6):819-33. doi: 10.1517/14656566.2016.1145667. Epub 2016 Mar 14.

Abstract

INTRODUCTION

Acetylcholinesterase inhibitors (neostigmine, edrophonium) and encapsulating agents (sugammadex and calabadion) can be used to reverse residual neuromuscular blockade (NMB).

AREAS COVERED

This review provides information about efficacy, effectiveness, and side effects of drugs (acetylcholinesterase inhibitors and encapsulating agents) used to reverse neuromuscular blocking agents (NMBAs).

EXPERT OPINION

The therapeutic range of acetylcholinesterase-inhibitors is narrow and effectiveness studies demonstrate clinicians don't use these unspecific reversal agents effectively to increase postoperative respiratory safety. The encapsulating drugs sugammadex and calabadion reverse all levels of NMB, and complete recovery of muscle strength can be achieved almost immediately after administration. For this reason encapsulating agents can be used as a solution for "cannot intubate cannot ventilate"- situations. Poor binding selectivity of encapsulating agents carries the risk of displacement of the NMBA by a competitively binding drug, which may lead to recurarization. In order to avoid side-effects, related to unspecific binding of endogenous proteins and drugs administered perioperatively it is prudent to titrate the dose of reversal agents to the minimal effective dose, depending on the depth of neuromuscular transmission block identified by neuromuscular transmission monitoring. Calabadions provide a diversified (increased binding selectivity) and expanded (reversal of benzylisoquinolines) spectrum of possible indications.

摘要

引言

乙酰胆碱酯酶抑制剂(新斯的明、依酚氯铵)和包封剂(舒更葡糖和卡拉巴腙)可用于逆转残余的神经肌肉阻滞(NMB)。

涵盖领域

本综述提供了有关用于逆转神经肌肉阻滞剂(NMBAs)的药物(乙酰胆碱酯酶抑制剂和包封剂)的疗效、有效性及副作用的信息。

专家观点

乙酰胆碱酯酶抑制剂的治疗范围较窄,有效性研究表明临床医生并未有效使用这些非特异性逆转剂来提高术后呼吸安全性。包封药物舒更葡糖和卡拉巴腙可逆转所有程度的NMB,给药后几乎可立即实现肌肉力量的完全恢复。因此,包封剂可作为“无法插管无法通气”情况的解决方案。包封剂的结合选择性较差,存在被竞争性结合药物取代NMBA的风险,这可能导致再次出现肌松作用。为避免与内源性蛋白质的非特异性结合及围手术期给药相关的副作用,根据神经肌肉传递监测确定的神经肌肉传递阻滞深度,谨慎地将逆转剂剂量滴定至最小有效剂量是明智的。卡拉巴腙提供了多样化(增加结合选择性)且扩大(逆转苄基异喹啉类)的可能适应症范围。

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