Sugammadex sodium (Org-25969)   中文名称: 舒更葡糖钠

Neuromuscular block

50和100μg/mL浓度的Sugammadex在谷氨酸诱导的细胞毒性后显著增强C6细胞的细胞活力（p＜0.001）。此外，sugammadex显著降低了nNOS、NO和TOS的水平以及凋亡细胞的数量，并增加了TAS的水平（p<0.001）。Sugammadex在细胞毒性方面具有保护和抗氧化特性，如果进一步的体内研究支持这一说法，它可能是阿尔茨海默病和帕金森病等神经退行性疾病的有效补充[5]。

在缺血后一小时再灌注开始时给予舒更葡糖（100 mg/kg，静脉注射，一次）的大鼠显示出对肾损伤的保护作用[2

本实验旨在评估sugammadex对谷氨酸诱导的细胞毒性的影响，包括一氧化氮和氧化应激途径。本研究使用C6胶质瘤细胞。谷氨酸组细胞给予谷氨酸24小时。Sugammadex组细胞给予不同浓度的sugammadex24小时。用不同浓度的Sugammadex+谷氨酸组细胞预处理1小时，然后暴露于谷氨酸中24小时。使用XTT法评估细胞活力。使用商业试剂盒计算细胞中一氧化氮（NO）、神经元一氧化氮合酶（nNOS）、总抗氧化剂（TAS）和总氧化剂（TOS）的水平。TUNEL法检测细胞凋亡[5]。

Methods: Four female rhesus monkeys each underwent three experiments. In each experiment, first, a 100-microg/kg dose of rocuronium was injected and spontaneous recovery was monitored. After full recovery, a 500-microg/kg dose of rocuronium was injected. Up to this point, all three experiments in a single monkey were identical. One minute after this rocuronium injection, either one of the two tested dosages of sugammadex (1.0 or 2.5 mg/kg) was injected or saline was injected.[1]
Results: Injection of 100 microg/kg rocuronium resulted in a mean neuromuscular blockade of 93.0% (SD = 4%), and profound blockade was achieved by injection of 500 microg/kg. In all experiments, a 100% neuromuscular blockade was achieved at this dose. After injection of the high rocuronium dose, the 90% recovery of the train-of-four ratio took 28 min (SD = 7 min) after saline, 26 min (SD = 9.5 min) after 1 mg/kg sugammadex, and 8 min (SD = 3.6 min) after 2.5 mg/kg sugammadex. Signs of residual blockade or recurarization were not observed. Injection of sugammadex had no significant effects on blood pressure or heart rate.[1]
Conclusions: Chemical encapsulation of rocuronium by sugammadex is a new therapeutic mechanism allowing effective and rapid reversal of profound neuromuscular blockade induced by rocuronium in anesthetized rhesus monkeys.[1]

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Currently, there is no information on the clinical use of sugammadex sodium during lactation. Because sugammadex sodium is a large, highly polar drug with a molecular weight of 2002 Da, its concentration in breast milk is likely to be very low, and oral absorption by the infant is unlikely. Use of sugammadex sodium during lactation is acceptable.
◉ Effects on Breastfed Infants
As of the revision date, no relevant published information was found.
◉ Effects on Lactation and Breast Milk
As of the revision date, no relevant published information was found.

[1]. de Boer HD, et al. Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkey. Br J Anaesth. 2006 Apr;96(4):473-9. Epub 2006 Feb 7.
[2]. Tercan M, Yılmaz İnal F, Seneldir H, Kocoglu H. Nephroprotective Efficacy of Sugammadex in Ischemia-Reperfusion Injury: An Experimental Study in a Rat Model. Cureus. 2021 Jun 17;13(6):e15726.
[3]. de Boer HD, et al. Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys. Anesthesiology. 2006 Apr;104(4):718-23.
[4]. de Boer HD, et al. 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. Br J Anaesth. 2006 Nov;97(5):681-6. Epub 2006 Oct.
[5]. Fundam Clin Pharmacol . 2023 Aug;37(4):786-793. doi: 10.1111/fcp.12890. Epub 2023 Mar 14.

Sugammadextrose sodium is an organic sodium salt, the octasodium salt of sugammadextrose. It is used to reverse neuromuscular blockade induced by rocuronium and vecuronium bromide in adult surgery. It is a neuromuscular blocking agent. It contains a sugammadextrose (8-) group. Sugammadextrose sodium is the sodium salt form of sugammadextrose, a bioinert selective muscle relaxant binder (SRBA) composed of a modified anionic γ-cyclodextrin derivative with a hydrophilic outer layer and a hydrophobic core, exhibiting neuromuscular blocking agent (NMBD) reversal activity. After administration, the negatively charged carboxysulfide group of sugammadextrose selectively and reversibly binds to the positively charged quaternary ammonium nitrogen atom of previously used steroidal NMBDs (such as rocuronium and vecuronium bromide) for anesthesia. The encapsulation of neuromuscular blocking agents (NMBDs) by sugammadextrose sodium blocks their binding to nicotine receptors at the neuromuscular junction, thereby reversing NMBD-induced neuromuscular blockade.
A gamma-cyclodextrin that can be used as a reversal agent for the neuromuscular blocking agent rocuronium bromide.
See also: Sugampazone sodium (containing the active ingredient).

---

Drug Indications
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults. For children: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide. For pediatric patients: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide. For pediatric patients: Sugampazone sodium is recommended only for routine reversal of neuromuscular blockade caused by rocuronium bromide in children and adolescents aged 2 to 17 years.
Reversal of neuromuscular blockade caused by rocuronium bromide or vecuronium bromide in adults. For pediatric patients: Sugammadex sodium is recommended only for routine reversal of rocuronium-induced neuromuscular blockade in children and adolescents aged 2 to 17 years. It is also recommended for reversing rocuronium or vecuronium-induced neuromuscular blockade in adults. For pediatric patients: Sugammadex sodium is recommended only for routine reversal of rocuronium-induced neuromuscular blockade in children and adolescents aged 2 to 17 years.

C72H104NA8O48S8

2177.9742

2176.26

C, 39.71; H, 4.81; Na, 8.44; O, 35.26; S, 11.78

343306-79-6

Sugammadex;343306-71-8

6918584

Typically exists as white to off-white solids at room temperature

1.275g/cm3 （计算值）

994.8

16

56

32

136

2790

40

S(C([H])([H])C([H])([H])C(=O)[O-])C([H])([H])[C@]1([H])[C@]2([H])[C@@]([H])([C@]([H])([C@]([H])(O1)O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O[C@]1([H])[C@@]([H])(C([H])([H])SC([H])([H])C([H])([H])C(=O)[O-])O[C@@]([H])([C@@]([H])([C@@]1([H])O[H])O[H])O2)O[H])O[H].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

KMGKABOMYQLLDJ-LHCKBTHCSA-F

InChI=1S/C72H112O48S8.8Na/c73-33(74)1-9-121-17-25-57-41(89)49(97)65(105-25)114-58-26(18-122-10-2-34(75)76)107-67(51(99)43(58)91)116-60-28(20-124-12-4-36(79)80)109-69(53(101)45(60)93)118-62-30(22-126-14-6-38(83)84)111-71(55(103)47(62)95)120-64-32(24-128-16-8-40(87)88)112-72(56(104)48(64)96)119-63-31(23-127-15-7-39(85)86)110-70(54(102)46(63)94)117-61-29(21-125-13-5-37(81)82)108-68(52(100)44(61)92)115-59-27(19-123-11-3-35(77)78)106-66(113-57)50(98)42(59)90;;;;;;;;/h25-32,41-72,89-104H,1-24H2,(H,73,74)(H,75,76)(H,77,78)(H,79,80)(H,81,82)(H,83,84)(H,85,86)(H,87,88);;;;;;;;/q;8*+1/p-8/t25?,26?,27?,28?,29?,30?,31?,32?,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57+,58+,59+,60+,61+,62+,63+,64+,65+,66+,67+,68+,69+,70+,71+,72?;;;;;;;;/m0......../s1

6A,6B,6C,6D,6E,6F,6G,6H-octakis-S-(2-Carboxyethyl)-6A,6B,6C,6D,6E,6F,6G,6H-octathio-γ-cyclodextrin sodium salt

trade name: Bridion. Sugammadex sodium; Org25969; Org-25969; Org 25969; 361LPM2T56; Sugammadex; trade name: Bridion. Sugammadex sodium

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~45.91 mM)

配方 1 中的溶解度: 100 mg/mL (45.91 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。