関: moricizine、moricizine hydrochloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/07/24 19:15:04」(JST)

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Moracizine (INN,^[1] or moricizine, trade name Ethmozine) is an antiarrhythmic of class IC.^[2] It was used for the prophylaxis and treatment of serious and life-threatening ventricular arrhythmias,^[3] but was withdrawn in 2007 for commercial reasons.^[4]

Pharmacology[edit]

Moracizine, a phenothiazine derivative, undergoes extensive first-pass metabolism and is also extensively metabolized after it has entered the circulation. It may have pharmacologically active metabolites. A clinical study has shown that moracizine is slightly less effective than encainide or flecainide in suppressing ventricular premature depolarizations.^{[citation needed]} Compared with disopyramide and quinidine, moracizine was equally or more effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia.^{[citation needed]}

In the Cardiac Arrhythmia Suppression Trial (CAST), a large study testing the influence of antiarrhythmics on mortality, showed a non-significant increase of mortality from 5.4 to 7.2% under moracizine. This is in line with other class IC antiarrhythmics.^[5]

References[edit]

^ "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances". World Health Organization. 2009. p. 103.
^ Ahmmed, G. U.; Hisatome, I.; Kurata, Y.; Makita, N.; Tanaka, Y.; Tanaka, H.; Okamura, T.; Sonoyama, K. et al. (2002). "Analysis of moricizine block of sodium current in isolated guinea-pig atrial myocytes. Atrioventricular difference of moricizine block". Vascular pharmacology 38 (3): 131–141. PMID 12402511. |displayauthors= suggested (help) edit
^ British National Formulary (59th ed.). British Medical Journal Publishing Group, Pharmaceutical Press. 2010.
^ "Shire Announces Ethmozine will be Available until December 31, 2007". Heart Rhythm Society.
^ "Effect of the Antiarrhythmic Agent Moricizine on Survival after Myocardial Infarction". New England Journal of Medicine 327 (4): 227–233. 1992. doi:10.1056/NEJM199207233270403. PMID 1377359. edit

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English Journal

[Appearance of ECG signs of the Brugada syndrome during therapy with class 1C antiarrhythmic drug ethacizine].

Makarov LM, Komoliatova VN.
Kardiologiia.Kardiologiia.2011;51(4):93-5.
PMID 21623727

[The role of reflexotherapy and physical training in the combined treatment and the prevention of paroxysmal form of idiopathic atrial fibrillation].

Kobel'kov SN, Lebedeva OD.
Voprosy kurortologii, fizioterapii, i lechebnoĭ fizicheskoĭ kultury.Vopr Kurortol Fizioter Lech Fiz Kult.2008 Nov-Dec;(6):36-8.
PMID 19175054

Effect of drugs on defibrillation capacity.

Dopp AL, Miller JM, Tisdale JE.SourceExtension Services in Pharmacy, University of Wisconsin-Madison School of Pharmacy, Madison, WI 53705-2222, USA. alegreiddopp@pharmacy.wisc.edu
Drugs.Drugs.2008;68(5):607-30.
Over 300,000 people die of sudden cardiac death (SCD) in the US annually. Implantable cardioverter-defibrillators (ICDs) have been shown to be more effective than antiarrhythmic drugs for the prevention of SCD in specific susceptible populations. Many patients in whom ICDs have been implanted receiv
PMID 18370441

Japanese Journal

Effects of Class I Antiarrhythmic Agents on Electrophysiological Changes during Acute Myocardial Ischemia and after Reperfusion in Dogs; Comparative Effects of Administration by the Intravenous and Coronary Sinus Retroperfusion Routes

YAMAMOTO Katsuhito,BANDO Shigenobu,SHINOHARA Akihiro,IKEFUJI Hiroyuki,NISHIKADO Akiyoshi,ITO Susumu
日本臨床生理学会雑誌 = Japanese journal of applied physiology 26(5), 253-262, 1996-10-01
NAID 10008696876

新しい Class I 抗不整脈薬 Moracizine (EN-313) の臨床第1相試験

新博次,斎藤寛和,井野威,早川弘一
臨床薬理 = JAPANESE JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS 26(1), 21-22, 1995-03-31
NAID 10013841420

Pharmacokinetics and Pharmacodynamics of Moracizine (EN-313) in Healthy Japanese Volunteers.

, ,
臨床薬理 25(2), 441-454, 1994
We administered single oral doses of 100, 200, 300 and 400 mg of EN-313 and repeated oral doses of 300 mg t.i.d., for 1 and 7 days to healthy adult men to confirm the safety and pharmacokinetics of th …
NAID 130002045290

Related Pictures

★リンクテーブル★

リンク元	「モラシジン」「moricizine hydrochloride」

「モラシジン」

Moracizine
Systematic (IUPAC) name
	ethyl [10-(3-morpholin-4-ylpropanoyl)-10H-phenothiazin-2-yl]carbamate
Clinical data
Trade names	Ethmozine
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a601214
Pregnancy cat.	B (U.S.)
Legal status	?
Pharmacokinetic data
Bioavailability	34–38%
Protein binding	95%
Half-life	3–4 hours (healthy volunteers), 6–13 hours (cardiac disease)
Identifiers
CAS number	31883-05-3
ATC code	C01BG01
PubChem	CID 34633
DrugBank	DB00680
ChemSpider	31872
UNII	2GT1D0TMX1
KEGG	D05077
ChEBI	CHEBI:6997
ChEMBL	CHEMBL1075
Chemical data
Formula	C22H25N3O4S
Mol. mass	427.518 g/mol
	SMILES O=C(OCC)Nc2cc1N(c3c(Sc1cc2)cccc3)C(=O)CCN4CCOCC4;
	InChI InChI=1S/C22H25N3O4S/c1-2-29-22(27)23-16-7-8-20-18(15-16)25(17-5-3-4-6-19(17)30-20)21(26)9-10-24-11-13-28-14-12-24/h3-8,15H,2,9-14H2,1H3,(H,23,27) ; Key:FUBVWMNBEHXPSU-UHFFFAOYSA-N ;
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