Schaller Stefan Josef, Lewald Heidrun
a Klinik für Anaesthesiologie, Klinikum rechts der Isar , Technische Universität München , Munich , Germany.
Expert Opin Drug Metab Toxicol. 2016 Sep;12(9):1097-108. doi: 10.1080/17425255.2016.1215426. Epub 2016 Aug 3.
Sugammadex is the first clinical representative of a class of drugs called steroidal muscle relaxant encapsulators. Due to its 1:1 binding of rocuronium or vecuronium, sugammadex can reverse any depth of neuromuscular block and has therefore revolutionized the way anesthetists think about drug reversal.
This review gives an overview of the clinical pharmacology and efficacy of sugammadex in healthy patients as well as in patients with pre-existing diseases.
After approval in Europe in 2008 and Asia in 2010, sugammadex has recently been approved in the USA and Canada. This will open the field for further research especially for the use in special patient populations and specific diseases. Due to its pharmacodynamic profile, sugammadex in combination with rocuronium might have the potential to displace succinylcholine as the gold standard muscle relaxant for rapid sequence inductions. The use of rocuronium or vecuronium with the potential to reverse its action with sugammadex seems to be safe in patients with impaired neuromuscular transmission, i.e. (neuro)muscular diseases including myasthenia gravis. Data from long-term use of sugammadex is not yet available. Evidence towards an economic advantage of using sugammadex, justifying the relatively high costs for an anesthesia-related drug, is missing.
舒更葡糖钠是一类名为甾体类肌肉松弛剂包裹剂的药物中的首个临床代表药物。由于其与罗库溴铵或维库溴铵具有1:1的结合能力,舒更葡糖钠能够逆转任何深度的神经肌肉阻滞,因此彻底改变了麻醉医生对药物逆转的看法。
本综述概述了舒更葡糖钠在健康患者以及患有基础疾病患者中的临床药理学和疗效。
舒更葡糖钠于2008年在欧洲获批,2010年在亚洲获批,最近在美国和加拿大也已获批。这将为进一步研究开辟领域,尤其是在特殊患者群体和特定疾病中的应用。鉴于其药效学特性,舒更葡糖钠与罗库溴铵联合使用可能有潜力取代琥珀酰胆碱,成为快速顺序诱导的金标准肌肉松弛剂。对于神经肌肉传递受损的患者,即患有包括重症肌无力在内的(神经)肌肉疾病的患者,使用罗库溴铵或维库溴铵并有可能用舒更葡糖钠逆转其作用似乎是安全的。目前尚无舒更葡糖钠长期使用的数据。缺乏使用舒更葡糖钠具有经济优势的证据,无法证明这种麻醉相关药物相对较高的成本是合理的。