Yang Lily P H, Keam Susan J
Wolters Kluwer Health, Adis, Auckland, New Zealand.
Drugs. 2009;69(7):919-42. doi: 10.2165/00003495-200969070-00008.
Sugammadex (Bridion), a modified gamma-cyclodextrin, is the first selective relaxant binding agent indicated to reverse the neuromuscular blockade induced during general anaesthesia to facilitate surgical procedures. The mechanism of action of sugammadex differs from that of other commonly used reversal agents, such as neostigmine and edrophonium. In the EU, sugammadex is recommended for use in the reversal of rocuronium- or vecuronium-induced moderate or deep muscle relaxation in adult (including elderly) patients and reversal of rocuronium-induced moderate muscle relaxation in paediatric patients (aged 2-17 years). Sugammadex is also approved in Australia, Iceland, New Zealand and Norway. In clinical trials in adult surgical patients with relatively good health, sugammadex at recommended doses provided rapid reversal of rocuronium- or vecuronium-induced neuromuscular blockade with a low incidence of residual or recurrent neuromuscular blockade and was generally well tolerated. In paediatric patients, sugammadex effectively reversed rocuronium-induced neuromuscular blockade and was generally well tolerated. Several factors associated with the use of sugammadex have yet to be determined, such as the efficacy and safety in patients with poorer health or in those with neuromuscular disorders, the incidence of infrequent adverse events in larger patient populations and the cost effectiveness of the drug relative to existing reversal agents. Nevertheless, sugammadex is a useful addition to the reversal agents commonly employed in anaesthetic practice.
舒更葡糖钠(布瑞亭)是一种改性γ-环糊精,是首个被批准用于逆转全身麻醉期间诱导的神经肌肉阻滞以促进手术操作的选择性肌松药结合剂。舒更葡糖钠的作用机制不同于其他常用的逆转剂,如新斯的明和依酚氯铵。在欧盟,推荐舒更葡糖钠用于逆转成年(包括老年)患者中罗库溴铵或维库溴铵诱导的中度或深度肌肉松弛,以及儿科患者(2至17岁)中罗库溴铵诱导的中度肌肉松弛。舒更葡糖钠在澳大利亚、冰岛、新西兰和挪威也已获批。在健康状况相对良好的成年外科手术患者的临床试验中,推荐剂量的舒更葡糖钠能快速逆转罗库溴铵或维库溴铵诱导的神经肌肉阻滞,残余或复发性神经肌肉阻滞的发生率较低,且总体耐受性良好。在儿科患者中,舒更葡糖钠能有效逆转罗库溴铵诱导的神经肌肉阻滞,且总体耐受性良好。与舒更葡糖钠使用相关的几个因素尚未确定,如健康状况较差或患有神经肌肉疾病患者的疗效和安全性、更大患者群体中罕见不良事件的发生率以及该药物相对于现有逆转剂的成本效益。尽管如此,舒更葡糖钠仍是麻醉实践中常用逆转剂的有益补充。