生物活性

• 描述Azimilide dihydrochloride is an antiarrhythmic drug with Vaughn Williams class III properties, which blocks both fast (IKr) and slow (IKs) components of the delayed rectifier cardiac potassium channel. Azimilide does not exhibit reverse-use dependence, that is, its binding characteristics and effectiveness are not related to the heart rate^[3]. Azimilide prolongs cardiac refractory period in a dose-dependent manner, as manifested by increases in action potential duration, QTc interval, and effective refractory period. Azimilide does not affect PR or QRS interval and minimally affects hemodynamic properties such as blood pressure and heart rate. Azimilide has shown excellent efficacy (>85%) in suppressing supraventricular arrhythmias in a variety of dog models. It also suppressed complex ventricular arrhythmias in infarcted dogs and, in a sudden death cardiac model, decreased mortality^[4]. In patients with a history of atrial fibrillation/flutter, oral azimilide controlled arrhythmias more effectively than placebo in a 6-month randomised double-blind study. At a dosage of 125 mg once daily, azimilide significantly increased the time to first symptomatic recurrence of atrial fibrillation/flutter^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01097330	Defibrillators, Implantable ... more >> Tachycardia, Ventricular Collapse <<	Phase 3	Terminated(Anticipated non-fea... more >>sibility of recruitment objectives) Collapse <<	December 2014	United States, Illinois ... more >> Northwestern University Chicago, Illinois, United States, 60611 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, Pennsylvania Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 United States, Texas Texas Cardiac Arrhythmia Research Foundation Austin, Texas, United States, 78705 United States, Virginia University of Virginia Health System Charlottesville, Virginia, United States, 22908 Canada, Ontario Hamilton Health Sciences Hamilton, Ontario, Canada, L8L 2X2 Southlake Regional Health Centre Newmarket, Ontario, Canada, L3Y 2P9 University of Ottawa Heart Institute Ottawa, Ontario, Canada, K1Y 4W7 Canada, Quebec McGill University Health Center Montreal, Quebec, Canada, H3G 1A4 Canada Institut Universitaire de Cardiologie et Pneumologie de Québec Quebec, Canada, G1V 4G5 China Beijng Fuwai Heart Hospital Beijing, China, 100037 Collapse <<
  NCT00035464	Atrial Fibrillation	Phase 3	Completed	-	-
  NCT00035477	Atrial Fibrillation	Phase 3	Completed	-	-

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• 参考文献

• [1] Busch AE, Eigenberger B, et al. Blockade of HERG channels by the class III antiarrhythmic azimilide: mode of action. Br J Pharmacol. 1998 Jan;123(1):23-30.

  [2] Fermini B, Jurkiewicz NK, et al. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: block of delayed rectifier potassium and L-type calcium currents. J Cardiovasc Pharmacol. 1995 Aug;26(2):259-71.

  [3] Carlson M. Azimilide dihydrochloride. Expert Rev Cardiovasc Ther. 2005;3(3):387-391

  [4] Karam R, Marcello S, Brooks RR, Corey AE, Moore A. Azimilide dihydrochloride, a novel antiarrhythmic agent. Am J Cardiol. 1998;81(6A):40D-46D

  [5] Clemett D, Markham A. Azimilide. Drugs. 2000;59(2):271-279

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