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更新于：2024-12-31
Atracurium Besylate
苯磺阿曲库铵
更新于：2024-12-31
概要
基本信息
原研机构 |
在研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1983-11-23), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C59H77N2O15S |
InChIKeyGLLXELVDCIFBPA-UHFFFAOYSA-M |
CAS号64228-81-5 |
关联
55
项与 苯磺阿曲库铵 相关的临床试验CTRI/2024/12/077526
A comparative study of action of atracurium vs action of vecuronium in general anesthesia - NIL
CTRI/2024/11/076818
A comparative study of efficacy of atracurium and cisatracurium for hemodynamic stability in patients undergoing laparoscopic surgeries - NIL
CTRI/2024/10/075659
Compare Atracurium Versus Cis-atracurium on basis of Haemodynamic parameters, Time of Onset and Intubating Conditions during General anaesthesia - NIL
100 项与 苯磺阿曲库铵 相关的临床结果
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100 项与 苯磺阿曲库铵 相关的转化医学
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100 项与 苯磺阿曲库铵 相关的专利（医药）
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2,098
项与 苯磺阿曲库铵 相关的文献（医药）2024-12-12JOURNAL OF MEDICINAL CHEMISTRY
Efficient Reversal of Neuromuscular Blocking Agent-Induced Biological Functions and Side Effects by an Extended Biphen[3]arene Carboxylate
Article
作者: Li, Shenghui ; Meng, Qingbin ; Li, Chunju ; Zhang, Ziliang ; Chen, Junyi ; Zhou, Yuanru ; Fang, Zihan ; Lin, Shujie ; Wang, Ruotong
Neuromuscular blocking agents (NMBAs) are widely administered during anethesia to prevent the patient from moving and optimize surgical conditions. Timely reversal of the muscle relaxation state induced by NMBAs at the end of surgery is necessary to recover autonomous respiration and muscle function. Herein, an extended biphen[3]arene carboxylate (ExBP3C) was designed and synthesized by a supramolecular sequestration approach as a reversal agent with high efficiency and generality against several representative NMBAs. ExBP3C exhibited robust host-guest complexation toward atracurium, rocuronium, vecuronium, pancuronium, and gallamine with an association constant of up to 108 M-1. A series of in vitro and in vivo safety tests preliminarily demonstrated that this synthetic macrocycle had good biocompatibility. Compared to sugammadex, post-treatment by an equivalent dose of ExBP3C could produce a more efficient reversal function. Additionally, a single dose of such a reversal agent was also able to completely recover overdose atracurium-induced heart rate abnormalities within 2 min.
2024-10-01JOURNAL OF MEDICAL PRIMATOLOGY
An Experimental Study to Optimize Neuromuscular Blockade Protocols in Cynomolgus Macaques: Monitoring, Doses, and Antagonism
Article
作者: Bruhns, Pierre ; Letscher, Hélène ; Gouel‐Chéron, Aurélie ; Le Grand, Roger ; Relouzat, Francis ; Burban, Emma ; Lemaitre, Julien
ABSTRACT:
Background:
Neuromuscular blocking agents (NMBAs) are a crucial component of anesthesia and intensive care through the relaxation of skeletal muscles. They can lead to adverse reactions such as postoperative residual neuromuscular block. Only one agent is capable of an instant block reversal in deep block situations, but is restricted to aminosteroid agents. Among animal models, non‐human primates are an essential model for a great diversity of human disease models. The main objective of this study was to establish a model for NMBA monitoring with current available drugs before testing new reversal agents.
Methods:
Seven healthy male cynomolgus macaques were randomly assigned to this study. Experiments using macaques were approved by the local ethical committee (CEtEA #44). All animals were anesthetized according to institutional guidelines, with ketamine and medetomidine, allowing IV line placement and tracheal intubation. Anesthesia was maintained with isoflurane. Either rocuronium bromine (with or without sugammadex reversal) or atracurium besylate was evaluated. Monitoring was performed with two devices, TOF‐Watch and ToFscan, measuring the T4/T1 and the T4/Tref ratios, respectively. Nonparametric Mann–Whitney statistical analyses were done when indicated.
Results:
NMBA monitoring required adaptation compared to humans, such as stimulus intensity and electrode placement, to be efficient and valid in cynomolgus macaques. When administered, both NMBAs induced deep and persistent neuro‐muscular block at equivalent doses to clinical doses in humans. The rocuronium‐induced profound neuromuscular block could be reversed using the cyclodextrin sugammadex as a reversal agent. We report no adverse effects in these models by clinical observation, blood chemistry, or complete blood count.
Conclusion:
These results support the use of non‐human primate models for neuromuscular block monitoring. This represented the first step before the forthcoming testing of new NMBA‐reversal agents.
2024-08-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Design, synthesis, and biological evaluation of new bis-benzylisoquinoline-based analogues as potential neuromuscular blocking agents
Article
作者: Song, Hao ; Chen, Chen ; Fu, Lin ; Ke, Bowen ; Liu, Xiaofeng ; Chen, Gang ; Qin, Yong ; Gan, Yu ; Zhao, Yi
Neuromuscular blocking agents (NMBAs) are widely used in anesthesia for intubation and surgical muscle relaxation. Novel atracurium and mivacurium derivatives were developed, with compounds 18c, 18d, and 29a showing mivacurium-like relaxation at 27.27 nmol/kg, and 15b, 15c, 15e, and 15h having a shorter duration at 272.7 nmol/kg. The structure-activity and configuration-activity relationships of these derivatives and 29a's binding to nicotinic acetylcholine receptors were analyzed through molecular docking. Rabbit trials showed 29a has a shorter duration compared to mivacurium. This suggests that linker properties, ammonium group substituents, and configuration are crucial for NMBA activity and duration, with compound 29a emerging as a potential ultra-short-acting NMBA.
100 项与 苯磺阿曲库铵 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 麻醉 | 中国 | 1997-01-01 | |
| 肌张力过低 | 美国 | 1983-11-23 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 34 | (Bispectral Index) | 構餘觸餘築鏇鬱壓網衊(鹽蓋艱糧鹽願選糧獵齋) = 繭醖醖鹽餘淵獵鏇製繭 壓廠選憲襯鬱夢壓廠獵 (壓淵繭壓夢壓網淵構餘, 範簾膚積鑰淵廠鏇鬱糧 ~ 糧顧醖糧齋蓋齋廠窪艱) 更多 | - | 2020-07-13 | ||
(Clinical Signs) | 構餘觸餘築鏇鬱壓網衊(鹽蓋艱糧鹽願選糧獵齋) = 淵糧鹽網鏇夢蓋艱築獵 壓廠選憲襯鬱夢壓廠獵 (壓淵繭壓夢壓網淵構餘, 鬱積積廠範鬱艱築範憲 ~ 選糧衊餘廠鹹淵鬱窪蓋) 更多 | ||||||
临床2/3期 | - | 173 | Atropine-propofol | 膚鬱製觸範願窪醖製襯(簾蓋鹹蓋鑰餘鏇醖艱齋): adjusted RD = -6.4 (95% CI, -21.0 ~ 8.1) 更多 | - | 2018-05-01 | |
Atropine-atracurium-sufentanil | |||||||
N/A | 691 | 選製窪艱齋鹽獵鏇衊鹽(衊鬱積齋窪積鬱壓觸餘) = 窪鑰廠築製簾衊糧鬱糧 蓋選醖鹽艱廠獵鹹膚觸 (選獵鹹壓遞鏇夢積顧鑰 ) 更多 | 积极 | 1997-10-01 | |||
Atracurium/Vecuronium | 選製窪艱齋鹽獵鏇衊鹽(衊鬱積齋窪積鬱壓觸餘) = 餘餘獵艱鬱衊襯膚願艱 蓋選醖鹽艱廠獵鹹膚觸 (選獵鹹壓遞鏇夢積顧鑰 ) 更多 | ||||||
N/A | - | 艱齋積廠鹹範餘襯艱簾(壓夢範顧範襯選願構艱) = 醖網鏇膚衊淵齋範憲衊 簾顧獵壓廠簾夢鏇壓網 (壓願願觸繭淵築衊壓範 ) 更多 | - | 1995-03-01 | |||
艱齋積廠鹹範餘襯艱簾(壓夢範顧範襯選願構艱) = 鏇艱醖製範憲鏇壓夢夢 簾顧獵壓廠簾夢鏇壓網 (壓願願觸繭淵築衊壓範 ) 更多 |
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