Moracizine ( INN, or [1 ] moricizine, trade name Ethmozine) is an antiarrhythmic of class IC. It was used for the prophylaxis and treatment of serious and life-threatening ventricular arrhythmias, [2 ] but was withdrawn in 2007 for commercial reasons. [3 ] [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. Compared with disopyramide and quinidine, moracizine was equally or more effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia.
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 ]
Synthesis [ edit ]
Moricizine synthesis: A Gritsenko, J Vikhlyaev, Z Senova, O Ulyanova, S Zhuravlev, N Kaverina;
U.S. Patent 3,740,395
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.; Furuse, Y.; Kato, M.; Yamamoto, Y.; Ogura, K.; Shimoyama, M.; Miake, J.; Sasaki, N.; Ogino, K.; Igawa, O.; Yoshida, A.; Shigemasa, C. (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. doi: 10.1016/S1537-1891(02)00213-6. PMID 12402511.
^ (59th ed.). British National Formulary 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.