Pharmacological and clinical profile of nifekalant (shinbit injection), a class III antiarrhythmic drug.

• OYABE Akihiro

  Drug Discovery Institute, Nihon Schering K.K.

• SANO Hidetoshi

  Therapeutics CNS/CV Dept./Product Management Hdqrs., Nihon Schering K.K.

Bibliographic Information

Other Title

• ＩＩＩ群抗不整脈薬塩酸ニフェカラント（シンビット注）の薬理作用および臨床効果
• 新薬紹介総説 3群抗不整脈薬塩酸ニフェカラント(シンビット注)の薬理作用および臨床効果
• シンヤク ショウカイ ソウセツ 3グン コウフセイミャクヤク エンサン ニフェカラント シンビット チュウ ノ ヤクリ サヨウ オヨビ リンショウ コウカ

Abstract

Nifekalant (shinbit^®, MS-551) is a pure class III antiarrhythmic drug (Vaughan Williams' classification), which was approved in Japan in June 1999. This drug prolongs the action potential duration (APD) and the effective refractory period (ERP) in cardiac myocytes mainly by blocking the I_Kr (the rapid component of delayed rectifier K⁺ current). The antiarrhythmic efficacy depends on prolongation of ERP. The importance of this drug is to save patients from the life-threatening arrhythmias ventricular tachycardia (VT) and fibrillation (VF). Nifekalant was effective against reentrant arrhythmias such as VT and VF in postinfarction dogs. This drug does not have the negative inotropic effect that has been observed with other antiarrhythmic drugs. In clinical therapy, this drug was remarkably effective on patients who were unresponsive to therapy with other drugs or who were not able to receive other drugs due to decreased cardiac function. There has been no case of drug-induced worsening of the cardiac function. The significant adverse reaction is proarrhythmia such as ventricular tachycardia including TdP. Nifekalant is expected to be a useful drug for patients who could not be rescued from life-threatening arrhythmia by conventional therapies.<br>

Journal

• Folia Pharmacologica Japonica

  Folia Pharmacologica Japonica 119 (2), 103-109, 2002

  The Japanese Pharmacological Society

Keywords

• nifekalant
• class III antiarrhythmic drug
• K⁺ channel
• VT/VF
• reentry

Details

• CRID: 1390282679248018048
• NII Article ID: 10008414799
• NII Book ID: AN00198335
• DOI: 10.1254/fpj.119.103
• COI: 1:STN:280:DC%2BD387islGktA%3D%3D
• ISSN: 13478397
• ISSN: 00155691
• NDL BIB ID: 6054233
• PubMed: 11862758
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I6054233
• Web Site: https://search.jamas.or.jp/link/ui/2002115447
• Text Lang: ja
• Data Source:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• Abstract License Flag: Disallowed