Delving into the Latest Updates on Atracurium Besylate with Synapse

Overview

Basic Info

Drug Type

Chemical drugs

Synonyms

Atracurium besilate, Atracurium besilate (INN), Atracurium besylate (USP)

+ [8]

Target

CHRNA2

Mechanism

CHRNA2 inhibitors(cholinergic receptor nicotinic alpha 2 subunit inhibitors)

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication

Muscle Hypotonia

Originator Organization

Hospira, Inc.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inactive Organization

Hospira, Inc.

Drug Highest PhaseApproved

First Approval Date

US (23 Nov 1983),

Muscle Hypotonia

Regulation-

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Structure

Molecular FormulaC59H77N2O15S

InChIKeyGLLXELVDCIFBPA-UHFFFAOYSA-M

CAS Registry64228-81-5

ABSTRACTBackgroundNeuromuscular 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.MethodsSeven 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.ResultsNMBA 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.ConclusionThese 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.

01 Aug 2024·Bioorganic & Medicinal Chemistry Letters

Design, synthesis, and biological evaluation of new bis-benzylisoquinoline-based analogues as potential neuromuscular blocking agents

Article

Author: Chen, Gang ; Song, Hao ; Fu, Lin ; Gan, Yu ; Qin, Yong ; Liu, Xiaofeng ; Ke, Bowen ; Chen, Chen ; 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.

02 Apr 2024·Strabismus

An atypical case of bilateral optic neuritis after strabismus surgery under general anesthesia

Article

Author: Kumar, Barun ; Shrestha, Sandhya ; Sharawat, Indar Kumar ; Singh, Anupam ; Panda, Prateek Kumar ; Pal, Himani

INTRODUCTIONStrabismus surgery under general anesthesia is a common procedure with rare complications in the form of hemorrhage, infection, slipped muscle, lost muscle, scleral perforation, and anterior segment ischemia. We report a unique case of bilateral optic neuritis following squint surgery under general anesthesia in a 15-year-old girl.METHODSA 15-year-old girl presented with accommodative esotropia with V pattern. She underwent uneventful bilateral inferior oblique recession surgery under general anesthesia with Propofol 60 mg, Atracurium 30 mg, and Fentanyl 70 mcg. On the first post-operative day, the patient had an acute onset of temporal headache which was non-radiating. She responded to supportive treatment and was discharged. However, on the 7th postoperative day, she presented with a constant severe headache in the bitemporal region (left > right) for 3 days. She also experienced a painless diminution of vision for 2 days. There was no vomiting, fever, loose stools, diplopia, difficulty in breathing, peripheral sensation loss, generalized weakness, or bowel/bladder incontinence.RESULTSThe best corrected visual acuity was 6/9 in right eye, and 6/9p in left eye with a relative afferent pupillary defect (RAPD) in the left eye. Both optic discs appeared hyperemic with blurred margins. Magnetic resonance imaging (MRI) of the brain and orbit showed hyperintensity along the intraorbital and intracanalicular parts of bilateral optic nerves on T2 weighted image suggesting bilateral optic neuritis. She received intravenous methylprednisolone pulse therapy followed by oral steroids and responded to the medical treatment with improvement in vision but developed steroid-induced glaucoma requiring medical management over several weeks.DISCUSSIONNeuro-ophthalmic complication in the form of non-arteritic ischemic optic neuropathy has been reported after various ophthalmic surgeries, but bilateral optic neuritis has not been reported to date. This possibility should be kept in mind if any patient presents with similar symptoms. This report also highlights IOP monitoring in pediatric patients receiving systemic steroids to prevent loss of vision due to steroid-induced glaucoma.

100 Deals associated with Atracurium Besylate

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