• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

使用复合物形成平衡的简单模型,研究舒更葡糖钠(Org 25969)对恒河猴罗库溴铵诱导的阻滞作用的时效过程。

Time course of action of sugammadex (Org 25969) on rocuronium-induced block in the Rhesus monkey, using a simple model of equilibration of complex formation.

作者信息

de Boer H D, van Egmond J, van de Pol F, Bom A, Driessen J J, Booij L H D J

机构信息

Department of Anaesthesiology, Radboud University Medical Centre Nijmegen The Netherlands.

出版信息

Br J Anaesth. 2006 Nov;97(5):681-6. doi: 10.1093/bja/ael240. Epub 2006 Oct 3.

DOI:10.1093/bja/ael240
PMID:17018564
Abstract

BACKGROUND

Reversal of neuromuscular block can be accomplished by chemical encapsulation of rocuronium by sugammadex (Org 25969), a synthetic gamma-cyclodextrin derivative. The present study determined the time course of the reversal action of sugammadex on rocuronium-induced block in the anaesthetized Rhesus monkey using train-of-four stimulation.

METHODS

A bolus injection of rocuronium 100 microg kg(-1) (about 1xED(90)) was given to determine the degree of neuromuscular block reached by this dose. After complete spontaneous recovery, a rapid bolus injection of sugammadex, 1 mg kg(-1), was given and at different time intervals (15, 30 or 60 min, in three different experiments) the effect of another rocuronium bolus injection of 100 microg kg(-1) was determined.

RESULTS

Injection of the first dose of rocuronium resulted in a mean neuromuscular block (depression of first twitch) of 93 (SEM=1.6)%. Fifteen minutes after injection of sugammadex the same rocuronium dose resulted in 17% (SEM=5.6) block. After 30 and 60 min these maximum blocks amounted to 49% (SEM=7.6) and 79% (SEM=4.2), respectively. The estimated half-life of sugammadex in Rhesus monkey is 30 (SEM=4.9) min.

CONCLUSIONS

The half-life of sugammadex (Org 25969), a new fast and efficient reversal agent for rocuronium-induced block, is relatively short in the Rhesus monkey, implying the possibility to perform neuromuscular block by rocuronium shortly after reversal of a prior block. In translation to the human situation differences in rocuronium sensitivity and kinetics should be taken into account.

摘要

背景

通过化学包裹罗库溴铵的新型γ-环糊精衍生物舒更葡糖(Org 25969)可实现神经肌肉阻滞的逆转。本研究采用四个成串刺激法,测定了舒更葡糖对麻醉状态下恒河猴罗库溴铵诱导的神经肌肉阻滞的逆转作用时程。

方法

静脉注射100 μg/kg(约1倍90%有效剂量)罗库溴铵,以确定该剂量所达到的神经肌肉阻滞程度。在自发完全恢复后,快速静脉注射1 mg/kg舒更葡糖,在不同时间间隔(在三个不同实验中分别为15、30或60分钟),测定再次静脉注射100 μg/kg罗库溴铵的效果。

结果

注射首剂罗库溴铵后,平均神经肌肉阻滞(第一个肌颤搐抑制)为93%(标准误=1.6)。注射舒更葡糖15分钟后,相同剂量罗库溴铵导致的阻滞为17%(标准误=5.6)。30分钟和60分钟后,这些最大阻滞分别为49%(标准误=7.6)和79%(标准误=4.2)。舒更葡糖在恒河猴体内的估计半衰期为30分钟(标准误=4.9)。

结论

舒更葡糖(Org 25969)作为罗库溴铵诱导阻滞的一种新型快速高效逆转剂,在恒河猴体内半衰期相对较短,这意味着在前次阻滞逆转后不久,有可能再次使用罗库溴铵进行神经肌肉阻滞。在应用于人体时,应考虑罗库溴铵敏感性和动力学方面的差异。

相似文献

1
Time course of action of sugammadex (Org 25969) on rocuronium-induced block in the Rhesus monkey, using a simple model of equilibration of complex formation.使用复合物形成平衡的简单模型,研究舒更葡糖钠(Org 25969)对恒河猴罗库溴铵诱导的阻滞作用的时效过程。
Br J Anaesth. 2006 Nov;97(5):681-6. doi: 10.1093/bja/ael240. Epub 2006 Oct 3.
2
Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkey.舒更葡糖钠,一种用于麻醉恒河猴中罗库溴铵诱导的神经肌肉阻滞的新型逆转剂。
Br J Anaesth. 2006 Apr;96(4):473-9. doi: 10.1093/bja/ael013. Epub 2006 Feb 7.
3
Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys.在麻醉恒河猴中,舒更葡糖钠逆转罗库溴铵所致深度神经肌肉阻滞的作用
Anesthesiology. 2006 Apr;104(4):718-23. doi: 10.1097/00000542-200604000-00016.
4
Chemical encapsulation of rocuronium by synthetic cyclodextrin derivatives: reversal of neuromuscular block in anaesthetized Rhesus monkeys.合成环糊精衍生物对罗库溴铵的化学包封:麻醉恒河猴神经肌肉阻滞的逆转
Br J Anaesth. 2006 Feb;96(2):201-6. doi: 10.1093/bja/aei306. Epub 2005 Dec 23.
5
Repeat dosing of rocuronium 1.2 mg kg-1 after reversal of neuromuscular block by sugammadex 4.0 mg kg-1 in anaesthetized healthy volunteers: a modelling-based pilot study.在麻醉健康志愿者中,使用 sugammadex 4.0mg/kg 逆转神经肌肉阻滞后,重复给予罗库溴铵 1.2mg/kg-1 的剂量:基于模型的初步研究。
Br J Anaesth. 2010 Oct;105(4):487-92. doi: 10.1093/bja/aeq167. Epub 2010 Jul 14.
6
Reversal of rocuronium-induced neuromuscular block with sugammadex is faster than reversal of cisatracurium-induced block with neostigmine.与新斯的明用于顺式阿曲库铵诱导的神经肌肉阻滞逆转相比,舒更葡糖用于罗库溴铵诱导的神经肌肉阻滞逆转更快。
Br J Anaesth. 2008 May;100(5):622-30. doi: 10.1093/bja/aen037. Epub 2008 Apr 2.
7
Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block.Org 25969(舒更葡糖钠),一种用于拮抗罗库溴铵诱导的长时间神经肌肉阻滞的选择性肌松药结合剂。
Br J Anaesth. 2006 Jan;96(1):36-43. doi: 10.1093/bja/aei314.
8
Reversal of profound rocuronium-induced blockade with sugammadex: a randomized comparison with neostigmine.舒更葡糖钠逆转罗库溴铵所致深度神经肌肉阻滞的效果:与新斯的明的随机对照比较
Anesthesiology. 2008 Nov;109(5):816-24. doi: 10.1097/ALN.0b013e31818a3fee.
9
Sugammadex reversal of rocuronium-induced neuromuscular block in Caesarean section patients: a series of seven cases.七例剖宫产患者罗库溴铵诱导的神经肌肉阻滞用苏伽 939 逆转的研究
Br J Anaesth. 2010 Nov;105(5):657-60. doi: 10.1093/bja/aeq227. Epub 2010 Aug 24.
10
Reversal of rocuronium-induced neuromuscular block by the selective relaxant binding agent sugammadex: a dose-finding and safety study.选择性肌松药结合剂舒更葡糖钠逆转罗库溴铵诱导的神经肌肉阻滞:一项剂量探索与安全性研究。
Anesthesiology. 2006 Apr;104(4):667-74. doi: 10.1097/00000542-200604000-00009.

引用本文的文献

1
Effects of sugammadex on heart rate variability in anesthetized male rats.舒更葡糖钠对麻醉雄性大鼠心率变异性的影响。
Physiol Rep. 2025 Aug;13(15):e70507. doi: 10.14814/phy2.70507.
2
Novel Insights on MRGPRX2-Mediated Hypersensitivity to Neuromuscular Blocking Agents And Fluoroquinolones.MRGPRX2 介导的神经肌肉阻滞剂和氟喹诺酮类药物过敏的新见解。
Front Immunol. 2021 Jul 27;12:668962. doi: 10.3389/fimmu.2021.668962. eCollection 2021.
3
Sugammadex.舒更葡糖钠
Hosp Pharm. 2016 Jul;51(7):585-96. doi: 10.1310/hpj5107-585.
4
Postoperative Delirium in Elderly Patients Undergoing Hip Fracture Surgery in the Sugammadex Era: A Retrospective Study.舒更葡糖钠时代老年髋部骨折手术患者的术后谵妄:一项回顾性研究
Biomed Res Int. 2016;2016:1054597. doi: 10.1155/2016/1054597. Epub 2016 Feb 22.
5
[Sugammadex. New pharmacological concept for antagonizing rocuronium and vecuronium].[舒更葡糖钠。拮抗罗库溴铵和维库溴铵的新药理学概念]
Anaesthesist. 2009 Jan;58(1):66-80. doi: 10.1007/s00101-008-1455-2.
6
Neostigmine but not sugammadex impairs upper airway dilator muscle activity and breathing.新斯的明而非舒更葡糖会损害上气道扩张肌活动及呼吸。
Br J Anaesth. 2008 Sep;101(3):344-9. doi: 10.1093/bja/aen176. Epub 2008 Jun 16.