WordNet

intravenous beta blocker (trade name Brevibloc) that acts for only a short time; used primarily for cardiac arrhythmias (同)Brevibloc
a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/10/17 12:08:43」(JST)

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Esmolol (trade name Brevibloc) is a cardioselective beta₁ receptor blocker with rapid onset,^[1] a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.

It is a class II antiarrhythmic.^[2]

Esmolol decreases the force and rate of heart contractions by blocking beta-adrenergic receptors of the sympathetic nervous system, which are found in the heart and other organs of the body. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine.

Dosing

Esmolol is given by slow intravenous injection. It is commonly used in patients during surgery to prevent or treat tachycardia, and is also used in treatment of acute supraventricular tachycardia. Esmolol is also the drug of choice when aortic dissection is suspected.

Metabolism

Esmolol is rapidly hydrolyzed by plasma esterases and not by plasma cholinesterases. Esmolol's short duration of action is based on the ester-methyl side chain which allows for quick hydrolysis. Esmolol's structure is reflected in its name, Es-molol as in ester-methyl. Plasma cholinesterases and red cell membrane acetylcholinesterase do not have any action. This metabolism results in the formation of a free acid and methanol. The amount of methanol produced is similar to endogenous methanol production. Its elimination half-life is about 9 minutes.

References

^ Deng CY, Lin SG, Zhang WC et al. (December 2006). "Esmolol inhibits Na+ current in rat ventricular myocytes". Methods Find Exp Clin Pharmacol 28 (10): 697–702. doi:10.1358/mf.2006.28.10.1037498. PMID 17235414.
^ Jaillon P, Drici M (December 1989). "Recent antiarrhythmic drugs". Am. J. Cardiol. 64 (20): 65J–69J. doi:10.1016/0002-9149(89)91203-4. PMID 2688391.

UpToDate Contents

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English Journal

A Case of Near-fatal Flecainide Overdose in a Neonate Successfully Treated with Sodium Bicarbonate.

Jang DH, Hoffman RS, Nelson LS.SourceNew York University School of Medicine and Bellevue Hospital, New York, New York and New York City Poison Control Center, New York, New York.
The Journal of emergency medicine.J Emerg Med.2013 Apr;44(4):781-3. doi: 10.1016/j.jemermed.2012.07.050. Epub 2012 Sep 13.
BACKGROUND: Flecainide is a class IC antidysrhythmic primarily indicated for ventricular dysrhythmias and supraventricular tachycardia (SVT). Class IC antidysrhythmic overdose has a reported mortality of 22%, and death results from dysrhythmias and cardiovascular collapse. We report a near-fatal fle
PMID 22981658

Cardioprotection with esmolol cardioplegia: efficacy as a blood-based solution.

Fujii M, Chambers DJ.SourceCardiac Surgical Research/Cardiothoracic Surgery, The Rayne Institute (King's College London), St Thomas' Hospital, London, UK.
European journal of cardio-thoracic surgery : official journal of the European Association for Cardio-thoracic Surgery.Eur J Cardiothorac Surg.2013 Mar;43(3):619-27. doi: 10.1093/ejcts/ezs365. Epub 2012 Jun 19.
OBJECTIVES: Current cardiac surgery patients are older, sicker, with more diffuse disease and hence a reduced tolerance to ischaemia-reperfusion injury. We previously demonstrated that esmolol, an ultra-short-acting β-blocker, can be used as an arresting agent at high (millimolar) concentrations, a
PMID 22715477

Carbamylated erythropoietin-FC fusion protein and recombinant human erythropoietin during porcine kidney ischemia/reperfusion injury.

Matějková Š, Scheuerle A, Wagner F, McCook O, Matallo J, Gröger M, Seifritz A, Stahl B, Vcelar B, Calzia E, Georgieff M, Möller P, Schelzig H, Radermacher P, Simon F.SourceSektion Anästhesiologische Pathophysiologie und Verfahrensentwicklung, Klinik für Anästhesiologie, Universitätsklinikum, Helmholtzstrasse 8-1, 89081 Ulm, Germany. sarka_matejkova@web.de
Intensive care medicine.Intensive Care Med.2013 Mar;39(3):497-510. doi: 10.1007/s00134-012-2766-y. Epub 2013 Jan 5.
PURPOSE: To test the hypothesis that a carbamylated EPO-FC fusion protein (cEPO-FC) or recombinant human erythropoietin (rhEPO) would protect against kidney ischemia/reperfusion (I/R) injury in pigs with atherosclerosis.METHODS: Anesthetized and mechanically ventilated animals received cEPO-FC (50 �
PMID 23291730

Japanese Journal

Esmolol hydrochloride for management of the cardiovascular stress responses to laryngoscopy and tracheal intubation

VUCEVIC M
Br J Anaesth 68, 529-530, 1992
NAID 30024564273

「エスモロール」

Esmolol
Systematic (IUPAC) name
	methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	AU: C; US: C;
Legal status	?
Routes	iv
Pharmacokinetic data
Bioavailability	-
Protein binding	60%
Metabolism	Erythrocytic
Half-life	9 minutes
Excretion	Renal
Identifiers
CAS number	103598-03-4
ATC code	C07AB09
PubChem	CID 59768
DrugBank	DB00187
ChemSpider	53916
UNII	MDY902UXSR
KEGG	D07916
ChEBI	CHEBI:4856
ChEMBL	CHEMBL768
Chemical data
Formula	C16H25NO4
Mol. mass	295.374 g/mol
	SMILES O=C(OC)CCc1ccc(OCC(O)CNC(C)C)cc1;
	InChI InChI=1S/C16H25NO4/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3/h4-5,7-8,12,14,17-18H,6,9-11H2,1-3H3 ; Key:AQNDDEOPVVGCPG-UHFFFAOYSA-N ;
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