ATRACURIUM

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 8297		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 8429	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
Synthesis and structure-activity relationships of neuromuscular blocking agents.	2002 Aug	12171561
[Relaxation and the electromyographic identification of the recurrent laryngeal nerve].	2002 Sep	12297961
[Interaction of donepezil and muscular blockers in Alzheimer's disease].	2003 Feb	12712872
[Establishment of a hypothermic dog model to investigate airway rewarming].	2006 Aug	21158096
Dynamic encoding of natural luminance sequences by LGN bursts.	2006 Jul	16756389
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010 Dec	21818443
Marfan syndrome with acute abdomen: a case report.	2010 Nov 10	21116341
Cisatracurium in different doses versus atracurium during general anesthesia for abdominal surgery.	2010 Sep	21189851
Wound contraction and macro-deformation during negative pressure therapy of sternotomy wounds.	2010 Sep 30	20920290

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).

Substance Class	Mixture Created by `admin` on `Fri Dec 15 16:22:30 GMT 2023` Edited by `admin` on `Fri Dec 15 16:22:30 GMT 2023`
Record UNII	2GQ1IRY63P
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ATRACURIUM

Common Name

English

ATRACURIUM CATION

Common Name

English

ATRACURIUM [VANDF]

Common Name

English

2-(2-CARBOXYETHYL)-1,2,3,4-TETRAHYDRO-6,7-DIMETHOXY-2-METHYL-1-VERATRYLISOQUINOLINIUM, PENTAMETHYLENE ESTER

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

Common Name

English

ATRACURIUM ION

Common Name

English

Atracurium [WHO-DD]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175720