Moracizine
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| Clinical data | |
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| Trade names | Ethmozine |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a601214 |
| Pregnancy category |
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| ATC code | C01BG01 (WHO) |
| Pharmacokinetic data | |
| Bioavailability | 34–38% |
| Protein binding | 95% |
| Biological half-life | 3–4 hours (healthy volunteers), 6–13 hours (cardiac disease) |
| Identifiers | |
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| CAS Number | 31883-05-3  |
| PubChem (CID) | 34633 |
| IUPHAR/BPS | 7244 |
| DrugBank | DB00680  |
| ChemSpider | 31872 |
| UNII | 2GT1D0TMX1 |
| KEGG | D05077 |
| ChEBI | CHEBI:6997 |
| ChEMBL | CHEMBL1075 |
| ECHA InfoCard | 100.046.216 |
| Chemical and physical data | |
| Formula | C22H25N3O4S |
| Molar mass | 427.518 g/mol |
| 3D model (Jmol) | Interactive image |
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Moracizine (INN[1]) or moricizine (USAN) (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It was used for the prophylaxis and treatment of serious and life-threatening ventricular arrhythmias,[3] but was withdrawn in 2007 for commercial reasons.[4]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 statistically 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" (PDF). 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.
- ^ 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.
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