ATRACURIUM BESYLATE

First approved in 1983

Description
Sources: http://www.sagentpharma.com/wp-content/uploads/2015/04/Atracurium-Besylate_PI.pdf
Curator's Comment: description was created based on several sources, including: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5176be07-3121-49fb-9eb9-638903753a31 | https://www.drugs.com/monograph/atracurium-besylate.html | http://www.wikidoc.org/index.php/Atracurium

Atracurium is an intermediate-duration, nondepolarizing, skeletal muscle relaxant for intravenous administration. It is used, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Most adverse reactions were suggestive of histamine release. Common side effects include flushing of the skin and low blood pressure. Drugs which may enhance the neuromuscular blocking action of atracurium include: enflurane; isoflurane; halothane; certain antibiotics, especially the aminoglycosides and polymyxins; lithium; magnesium salts; procainamide; and quinidine.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Muscle-type nicotinic acetylcholine receptor 65 Target ID: CHEMBL2362997 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19417616	Inhibitor 8504		169.5 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Skeletal muscle relaxation 17 Sources: http://www.sagentpharma.com/wp-content/uploads/2015/04/Atracurium-Besylate_PI.pdf	Palliative		Approved 8583	ATRACURIUM BESYLATE Approved Use Atracurium Besylate Injection, USP is indicated, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Launch Date 1997

PubMed

Title	Date	PubMed
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010-12	21818443
Marfan syndrome with acute abdomen: a case report.	2010-11-10	21116341
Wound contraction and macro-deformation during negative pressure therapy of sternotomy wounds.	2010-09-30	20920290
Cisatracurium in different doses versus atracurium during general anesthesia for abdominal surgery.	2010-09	21189851
Comparison between Culture Conditions Improving Growth and Differentiation of Blood and Bone Marrow Cells Committed to the Endothelial Cell Lineage.	2010-02-06	21406067
Modulation of temporal precision in thalamic population responses to natural visual stimuli.	2010	21151356
Anaesthetic management of post-burn contractures, a recurrent challenge from oil pipeline vandalization in Nigeria: a case report.	2009-12-03	20062658
Leaking abdominal aortic aneurysm on anticoagulants-thromboelastography assisted management.	2009-06	20640143
A prospective randomized double blind study to evaluate the effect of infusion of amino Acid enriched solution on recovery from neuromuscular blockade.	2009-06	20640140
Timing precision in population coding of natural scenes in the early visual system.	2008-12-16	19090624
Donepezil in Alzheimer's disease: From conventional trials to pharmacogenetics.	2007-06	19300564
[Establishment of a hypothermic dog model to investigate airway rewarming].	2006-08	21158096
Dynamic encoding of natural luminance sequences by LGN bursts.	2006-07	16756389
A comparison of the efficacy of cisatracurium and atracurium in kidney transplantation operation.	2004-01	14971538
[Interaction of donepezil and muscular blockers in Alzheimer's disease].	2003-02	12712872
[Relaxation and the electromyographic identification of the recurrent laryngeal nerve].	2002-09	12297961
Synthesis and structure-activity relationships of neuromuscular blocking agents.	2002-08	12171561

Patents

Sample Use Guides

In Vivo Use Guide

An atracurium besylate dose of 0.4 to 0.5 mg/kg (1.7 to 2.2 times the ED95), given as an intravenous bolus injection, is the recommended initial dose for most patients. Maximum neuromuscular block achieved approximately 3 to 5 minutes after injection.

Route of Administration: Intravenous

In Vitro Use Guide

Exposure of isolated rat hepatocytes to atracurium produced cellular damage evidenced by extrusion of an intracellular enzyme, lactate dehydrogenase (LDH), into the incubation medium. Leakage of LDH was directly related to the concentration of atracurium in the medium (250 to 800 microM). When atracurium was added to the medium and the medium immediately added to hepatocytes, the leakage of LDH increased as the concentration of atracurium increased (P < 0.001 for the comparison with cells not exposed to atracurium).

Name

Type

Language

ATRACURIUM BESILATE

Preferred Name

English

ATRACURIUM BESYLATE

Official Name

English

ISOQUINOLINIUM, 2,2'-(1,5-PENTANEDIYLBIS(OXY(3-OXO-3,1-PROPANEDIYL)))BIS(1-((3,4-DIMETHOXYPHENYL)METHYL)-1,2,3,4-TETRAHYDRO-6,7-DIMETHOXY-2-METHYL-, (1R,2R,1'R,2'R)- BISBENZENESULFONATE

Common Name

English

NSC-760047

Code

English

(1R,2R,1'R,2'R)-2,2'-(PENTANE-1,5-DIYLBIS(OXY(3-OXOPROPANE-3,1-DIYL)))BIS(1-(3,4-DIMETHOXYBENZYL)-6,7-DIMETHOXY-2-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINIUM) BISBENZENESULFONATE

Common Name

English

ATRACURIUM BESYLATE [MI]

Common Name

English

ATRACURIUM BESYLATE [USAN]

Common Name

English

TRACRIUM

Brand Name

English

ATRACURIUM BESYLATE [VANDF]

Common Name

English

ATRACURIUM BESYLATE [USP-RS]

Common Name

English

atracurium besilate [INN]

Common Name

English

2-(2-Carboxyethyl)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium benzenesulfonate, pentamethylene ester

Common Name

English

BW-33A

Code

English

ATRACURIUM DIBESYLATE

Common Name

English

WELLCOME 33-A-74

Code

English

ATRACURIUM BESYLATE [ORANGE BOOK]

Common Name

English

BW 33A

Code

English

ATRACURIUM BESILATE [MART.]

Common Name

English

Atracurium besilate [WHO-DD]

Common Name

English

ATRACURIUM BESYLATE [USP MONOGRAPH]

Common Name

English

ATRACURIUM BESILATE [EP MONOGRAPH]

Common Name

English

ISOQUINOLINIUM, 2,2'-(1,5-PENTANEDIYLBIS(OXY(3-OXO-3,1-PROPANEDIYL)))BIS(1-((3,4-DIMETHOXYPHENYL)METHYL)-1,2,3,4-TETRAHYDRO-6,7-DIMETHOXY-2-METHYL-, DIBENZENESULFONATE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29696