Caldwell J E, Miller R D
Department of Anesthesia and Perioperative Medicine, University of California, San Francisco, CA, USA.
Anaesthesia. 2009 Mar;64 Suppl 1:66-72. doi: 10.1111/j.1365-2044.2008.05872.x.
Sugammadex is a cyclodextrin molecule that encapsulates and inactivates rocuronium and vecuronium. As a result, any degree of neuromuscular block produced by rocuronium or vecuronium can be rapidly and completely reversed without autonomic effects. Because sugammadex is optimised for reversing rocuronium it is most likely to be used in conjunction with this drug. Sugammadex will allow deep levels of block to be maintained until the very end of surgery, and will allow block to be reversed at any time after rocuronium administration, even just a few minutes. The recommended dose-range is 2-16 mg.kg-1 (ascender), depending on the level of block. The availability of sugammadex reversal may increase the use of rocuronium, and decrease the use of suxamethonium and benzylisoquinoline neuromuscular blocking drugs. In addition, it will certainly increase pharmacy costs, which may be offset by faster recovery and discharge from the post-anesthesia recovery unit. Sugammadex may also change monitoring practices in that post-tetanic count will be required to quantify deep block, and quantitative monitoring of recovery may be driven by cost concerns in order to allow the use of the smallest dose of sugammadex that gives a satisfactory train-of-four ratio. Alternatively, monitoring may essentially be abandoned since a large dose of sugammadex will reliably reverse any degree of rocuronium-induced block. The ultimate clinical utility of sugammadex will be clear only after large-scale clinical use.
舒更葡糖是一种环糊精分子,可包裹并使罗库溴铵和维库溴铵失活。因此,罗库溴铵或维库溴铵产生的任何程度的神经肌肉阻滞都能迅速且完全逆转,且无自主神经效应。由于舒更葡糖针对逆转罗库溴铵进行了优化,所以它最有可能与该药物联合使用。舒更葡糖可使深度阻滞维持至手术结束,并且在给予罗库溴铵后的任何时间,哪怕仅几分钟后,都能使阻滞逆转。推荐剂量范围为2 - 16 mg·kg⁻¹(递增),具体取决于阻滞程度。舒更葡糖用于逆转神经肌肉阻滞可能会增加罗库溴铵的使用,并减少琥珀胆碱和苄异喹啉类神经肌肉阻滞药物的使用。此外,这肯定会增加药房成本,不过更快的恢复以及从麻醉后恢复室出院可能会抵消这一成本。舒更葡糖还可能改变监测方法,即需要采用强直后计数来量化深度阻滞,出于成本考虑可能会推动对恢复情况进行定量监测,以便使用能给出满意的四个成串刺激比值的最小剂量舒更葡糖。或者,由于大剂量舒更葡糖能可靠地逆转罗库溴铵所致的任何程度的阻滞,监测可能基本上会被放弃。只有在大规模临床应用后,舒更葡糖的最终临床实用性才会明晰。