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词条 Moracizine
释义

  1. Pharmacology

  2. References

{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 462253689
| IUPAC_name = ethyl [10-(3-morpholin-4-ylpropanoyl)-10H-phenothiazin-2-yl]carbamate
| image = Moricizin.svg
| USAN = Moricizine
| tradename = Ethmozine
| Drugs.com = {{drugs.com|CDI|moricizine}}
| MedlinePlus = a601214
| pregnancy_category = B (U.S.)
| legal_status =
| routes_of_administration =
| bioavailability = 34–38%
| protein_bound = 95%
| metabolism =
| elimination_half-life = 3–4 hours (healthy volunteers), 6–13 hours (cardiac disease)
| IUPHAR_ligand = 7244
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 31883-05-3
| ATC_prefix = C01
| ATC_suffix = BG01
| ATC_supplemental =
| PubChem = 34633
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = DB00680
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 31872
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 2GT1D0TMX1
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D05077
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 6997
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 1075
| C=22 | H=25 | N=3 | O=4 | S=1
| molecular_weight = 427.518 g/mol
| smiles = O=C(OCC)Nc2cc1N(c3c(Sc1cc2)cccc3)C(=O)CCN4CCOCC4
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = FUBVWMNBEHXPSU-UHFFFAOYSA-N
}}Moracizine[1] or moricizine, sold under the 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It was used for the prophylaxis and treatment of serious and life-threatening ventricular arrhythmias,[3] but was withdrawn in 2007 for commercial reasons.[4]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

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|date=February 2007}} Compared with disopyramide and quinidine, moracizine was equally or more effective in suppressing premature ventricular contractions, couplets, and nonsustained ventricular tachycardia.{{Citation needed|date=February 2007}}

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

1. ^{{cite web|url=http://www.who.int/medicines/services/inn/StemBook2009.pdf|title=The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances|year=2009|publisher=World Health Organization|page=103}}
2. ^{{Cite journal | doi = 10.1016/S1537-1891(02)00213-6 | last1 = Ahmmed | first1 = G. U. | last2 = Hisatome | first2 = I. | last3 = Kurata | first3 = Y. | last4 = Makita | first4 = N. | last5 = Tanaka | first5 = Y. | last6 = Tanaka | first6 = H. | last7 = Okamura | first7 = T. | last8 = Sonoyama | first8 = K. | last9 = Furuse | first9 = Y. | last10 = Kato | first10 = M. | last11 = Yamamoto | first11 = Y. | last12 = Ogura | first12 = K. | last13 = Shimoyama | first13 = M. | last14 = Miake | first14 = J. | last15 = Sasaki | first15 = N. | last16 = Ogino | first16 = K. | last17 = Igawa | first17 = O. | last18 = Yoshida | first18 = A. | last19 = Shigemasa | first19 = C. | title = Analysis of moricizine block of sodium current in isolated guinea-pig atrial myocytes. Atrioventricular difference of moricizine block | journal = Vascular Pharmacology | volume = 38 | issue = 3 | pages = 131–141 | year = 2002 | pmid = 12402511}}
3. ^{{cite book|title=British National Formulary|edition=59th|publisher=British Medical Journal Publishing Group, Pharmaceutical Press|year=2010|title-link=British National Formulary}}
4. ^{{cite news|url=http://www.hrsonline.org/policy/devicesdrugsfda/drugs/ethmozine_discontinued.cfm|title=Shire Announces Ethmozine will be Available until December 31, 2007|publisher=Heart Rhythm Society}}
5. ^{{Cite journal | doi = 10.1056/NEJM199207233270403 | title = Effect of the Antiarrhythmic Agent Moricizine on Survival after Myocardial Infarction | journal = New England Journal of Medicine | volume = 327 | issue = 4 | pages = 227–233 | year = 1992 | pmid = 1377359 | pmc = | author1 = Cardiac Arrhythmia Suppression Trial II Investigators }}
{{Antiarrhythmic agents}}{{cardiovascular-drug-stub}}

6 : Antiarrhythmic agents|Sodium channel blockers|Phenothiazines|Morpholines|Carbamates|Abandoned drugs

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