Sugammadex
(Synonyms: Org25969 free acid) 目录号 : GC67613
A steroid-based neuromuscular blocker reversing agent
Cas No.:343306-71-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sugammadex is a synthetic derivative of γ-cyclodextrin and a steroid-based neuromuscular blocker reversing agent.1 It binds rocuronium within its cyclodextrin ring and selectively reverses rocuronium-induced neuromuscular blockade over that induced by mivacurium or atracurium in anesthetized rhesus monkeys. Sugammadex also prevents formation of postoperative peritoneal adhesions in rats.2 In a rat model of ischemia-reperfusion injury, sugammadex (16 and 100 mg/kg) increases the total number of neurons in the hippocampus compared to control and improves motor coordination in a beam walking test.3
1.de Boer, H.D., van Egmond, J., van de Pol, F., et al.Sugammadex, a new reversal agent for neuromuscular block induced by rocuronium in the anaesthetized Rhesus monkeyBr. J. Anaesth.96(4)473-479(2006) 2.?ahin, H., Toman, H., Kiraz, H.A., et al.Effects of sugammadex on the prevention of postoperative peritoneal adhesionsKaohsiung J. Med. Sci.31(9)463-467(2015) 3.Ozbilgin, S., Yilmaz, O., Ergur, B.U., et al.Effectiveness of sugammadex for cerebral ischemia/reperfusion injuryKaohsiung, J. Med. Sci.32(6)292-301(2016)
| Cas No. | 343306-71-8 | SDF | Download SDF |
| 别名 | Org25969 free acid | ||
| 分子式 | C72H112O48S8 | 分子量 | 2002.15 |
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4995 mL | 2.4973 mL | 4.9946 mL |
| 5 mM | 0.0999 mL | 0.4995 mL | 0.9989 mL |
| 10 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Sugammadex for Reversal of Neuromuscular Blockade: Uses and Limitations
Curr Pharm Des 2019;25(19):2140-2148.PMID:31272347DOI:10.2174/1381612825666190704101145.
Sugammadex is a reversal agent that was engineered to reverse the effects of aminosteroid muscle relaxants. It is a modified gamma-cyclodextrin, i.e. a large glucose molecule bound in a ring-like structure. Sugammadex, when injected intravenously, creates a concentration gradient favoring the movement of aminosteroid muscle relaxants from the neuromuscular junction back into the plasma, and then encapsulates the aminosteroid muscle relaxants within its inner structure by forming tight water-soluble complexes. The dissociation of the aminosteroidal muscle relaxant from the post-synaptic acetylcholine receptors is responsible for the termination of neuromuscular blockade. This review article presents the current indication, mechanism of action, limitations, side effects and contraindications of Sugammadex. An overview of monitoring of the adequacy of reversal of aminosteroid muscle relaxants with Sugammadex is presented. Moreover, the use of Sugammadex in special situations, including "cannot intubate cannot oxygenate" scenarios is also described.
Sugammadex versus Neostigmine for Reversal of Neuromuscular Blockade and Postoperative Pulmonary Complications (STRONGER): A Multicenter Matched Cohort Analysis
Anesthesiology 2020 Jun;132(6):1371-1381.PMID:32282427DOI:10.1097/ALN.0000000000003256.
Background: Five percent of adult patients undergoing noncardiac inpatient surgery experience a major pulmonary complication. The authors hypothesized that the choice of neuromuscular blockade reversal (neostigmine vs. Sugammadex) may be associated with a lower incidence of major pulmonary complications. Methods: Twelve U.S. Multicenter Perioperative Outcomes Group hospitals were included in a multicenter observational matched-cohort study of surgical cases between January 2014 and August 2018. Adult patients undergoing elective inpatient noncardiac surgical procedures with general anesthesia and endotracheal intubation receiving a nondepolarizing neuromuscular blockade agent and reversal were included. Exact matching criteria included institution, sex, age, comorbidities, obesity, surgical procedure type, and neuromuscular blockade agent (rocuronium vs. vecuronium). Other preoperative and intraoperative factors were compared and adjusted in the case of residual imbalance. The composite primary outcome was major postoperative pulmonary complications, defined as pneumonia, respiratory failure, or other pulmonary complications (including pneumonitis; pulmonary congestion; iatrogenic pulmonary embolism, infarction, or pneumothorax). Secondary outcomes focused on the components of pneumonia and respiratory failure. Results: Of 30,026 patients receiving Sugammadex, 22,856 were matched to 22,856 patients receiving neostigmine. Out of 45,712 patients studied, 1,892 (4.1%) were diagnosed with the composite primary outcome (3.5% Sugammadex vs. 4.8% neostigmine). A total of 796 (1.7%) patients had pneumonia (1.3% vs. 2.2%), and 582 (1.3%) respiratory failure (0.8% vs. 1.7%). In multivariable analysis, Sugammadex administration was associated with a 30% reduced risk of pulmonary complications (adjusted odds ratio, 0.70; 95% CI, 0.63 to 0.77), 47% reduced risk of pneumonia (adjusted odds ratio, 0.53; 95% CI, 0.44 to 0.62), and 55% reduced risk of respiratory failure (adjusted odds ratio, 0.45; 95% CI, 0.37 to 0.56), compared to neostigmine. Conclusions: Among a generalizable cohort of adult patients undergoing inpatient surgery at U.S. hospitals, the use of Sugammadex was associated with a clinically and statistically significant lower incidence of major pulmonary complications.
Sugammadex
Crit Care Resusc 2013 Mar;15(1):57-62.PMID:23432503doi
Sugammadex is the first selective antagonist to reverse neuromuscular blockade induced by rocuronium and vecuronium. The mechanism by which Sugammadex works is superior to current neuromuscular block reversal strategies in terms of speed, efficacy and side effects. There is little contemporary guidance on the use of Sugammadex in intensive care medicine. This review covers the key pharmacological features, clinical uses and cost- effectiveness in the context of intensive care practice.
Sugammadex in Colorectal Surgery: A Systematic Review and Meta-analysis
J Surg Res 2022 Feb;270:221-229.PMID:34710702DOI:10.1016/j.jss.2021.09.026.
Background: Traditionally, reversal of neuromuscular blocking agents following the completion of surgery was achieved with cholinesterase inhibitors. Recently, Sugammadex has been increasingly relied upon. Sugammadex is a γ-cyclodextrin molecule that rapidly reverses steroidal neuromuscular blocking drugs. Its use following colorectal surgery has become more common, and while the rapidity of reversal is undoubtedly improved, whether Sugammadex impacts clinical postoperative outcomes is unknown. This systematic review and meta-analysis aims to compare postoperative outcomes in patients receiving Sugammadex to those receiving a control during colorectal surgery. Methods: Medline, Embase, and CENTRAL were systematically searched. Articles were included if they compared Sugammadex with a control (e.g., neostigmine, pyridostigmine, placebo) in patients undergoing colorectal surgery in terms of total hospital length of stay and frequency of postoperative adverse respiratory events. Pairwise meta-analyses using inverse variance random effects was performed. Results: From 269 citations, five studies with 535 patients receiving Sugammadex (45.8% female; mean age: 64.4) and 569 patients receiving a control (45.0% female; mean age: 64.3) were included. There was no significant difference in length of stay between the two groups (MD -0.01, 95% CI -0.27 to 0.25, P = 0.95). The risk of adverse respiratory events postoperatively was similar between the two groups (RR 1.33, 95% CI 0.81-2.19, P = 0.25). Conclusion: There are no current data to suggest an improvement in postoperative outcomes with the use of Sugammadex in patients undergoing colorectal surgery. This study is limited by the number of included studies. Further prospective studies comparing Sugammadex and a control in colorectal surgery is required.
Sugammadex for reversal of neuromuscular blockade in pediatric patients: Results from a phase IV randomized study
Paediatr Anaesth 2022 Mar;32(3):436-445.PMID:34878707DOI:10.1111/pan.14370.
Background: Few randomized studies have assessed recovery from rocuronium- or vecuronium-induced moderate or deep neuromuscular blockade with Sugammadex in pediatric participants. Aim: To assess Sugammadex for reversal of neuromuscular blockade in pediatric participants. Methods: This was a randomized, phase IV, active comparator-controlled, double-blind study. Participants aged 2 to <17 years, under moderate or deep neuromuscular blockade, were administered Sugammadex (2 or 4 mg/kg) or neostigmine (50 µg/kg; for moderate neuromuscular blockade only). Predefined adverse events of clinical interest, including clinically relevant bradycardia, hypersensitivity, and anaphylaxis, were monitored. The primary efficacy endpoint was time to recovery to a train-of-four ratio of ≥0.9 in participants receiving Sugammadex 2 mg/kg versus neostigmine for reversal of moderate neuromuscular blockade, analyzed by analysis of variance adjusted for neuromuscular blocking agent and age. Results: Of 288 randomized participants, 272 completed the study and 276 were included in the analyses. Clinically relevant bradycardia was experienced by 2.0%, 1.6%, and 5.9% of participants in the Sugammadex 2 mg/kg, Sugammadex 4 mg/kg, and neostigmine groups, respectively. No hypersensitivity or anaphylaxis events were observed. Recovery to a train-of-four ratio of ≥0.9 with Sugammadex 2 mg/kg was faster than neostigmine (1.6 min, 95% CI 1.3 to 2.0 vs. 7.5 min, 95% CI 5.6 to 10.0; p < .0001) and was comparable to Sugammadex 4 mg/kg (2.0 min, 95% CI 1.8 to 2.3). Conclusions: Pediatric participants recovered from rocuronium- or vecuronium-induced moderate neuromuscular blockade significantly faster with Sugammadex 2 mg/kg than with neostigmine. Time to reversal of deep neuromuscular blockade with Sugammadex 4 mg/kg was consistent with that of moderate neuromuscular blockade reversal. No meaningful differences in clinically relevant bradycardia, hypersensitivity, or anaphylaxis were seen with Sugammadex vs neostigmine. These results support the use of Sugammadex for reversal of moderate and deep rocuronium- and vecuronium-induced neuromuscular blockade in patients aged 2 to <17 years. Clinical trial registration: NCT03351608/EudraCT 2017-000692-92.