nach oben

Drugs

Erschienen in:

01.03.2010 | Adis Drug Profile

Pilsicainide

verfasst von: Greg L. Plosker

Erschienen in: Drugs | Ausgabe 4/2010

Einloggen, um Zugang zu erhalten

Abstract

Pilsicainide is a class Ic antiarrhythmic agent used for the treatment of supraventricular and ventricular tachycardia. The pharmacodynamic effects of pilsicainide are achieved via selective sodium channel blockade.

In randomized, multicentre trials in patients with atrial fibrillation, restoration of sinus rhythm was achieved in significantly more patients treated with a single oral dose of pilsicainide than those who received placebo, and in a numerically higher proportion of oral pilsicainide than intravenous dis-opyramide recipients.

In another well designed trial in patients with persistent atrial fibrillation, the proportion of patients whose arrhythmia converted to normal sinus rhythm was significantly higher among those randomized to receive 2 weeks of oral pilsicainide therapy than among patients who received placebo.

Over a 1-year period, both pilsicainide and cibenzoline (another class Ic agent) were effective in preventing recurrence of atrial fibrillation in a substantial proportion of patients in a single-centre crossover trial. There were no between-group differences in the subgroup of patients with shorter-duration atrial fibrillation, but actuarial results over 1 year significantly favoured cibenzoline over pilsicainide in patients with longer-duration atrial fibrillation.

Both oral and intravenous pilsicainide have demonstrated efficacy in ventricular tachyar-rhythmias, including ventricular extrasystole.

Clinical trial and postmarketing surveillance data indicate that pilsicainide is generally well tolerated in most patients.

Tachycardia: diagnosis and treatment at Mayo Clinic [online]. Available from URL: http://www.mayoclinic.org/tachycardia/[Accessed 2010 Jan 14]

Fox DJ, Tischenko A, Krahn AD, et al. Supraventricular tachycardia: diagnosis and management. Mayo Clin Proc 2008 Dec; 83(12): 1400–11PubMedCrossRef

Clarke JM, Hamer J, Shelton JR. The rhythm of the normal human heart. Lancet 1976; 1(7984): 508–12PubMedCrossRef

Hinkle Jr LE, Carver ST, Stevens M. The frequency of asymptomatic disturbances of cardiac rhythm and conduction in middle-aged men. Am J Cardiol 1969; 24(5): 629–50PubMedCrossRef

Fuster V, Rydén LE, Crijns HJ, et al. ACC/AHA/ESC 2006 guidelines for the management of patients with atrial fibrillation: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines and the European Society of Cardiology Committee for Practice Guidelines (Writing Committee to Revise the 2001 Guidelines for the Management of Patients With Atrial Fibrillation). Circulation 2006; 114: e257–354PubMedCrossRef

Ehrlich JR, Nattel S. Novel approaches for pharmacological management of atrial fibrillation. Drugs 2009; 69(7): 757–74PubMedCrossRef

Hancox JC, Patel KCR, Jones JV. Antiarrhythmics-from cell to clinic: past, present, and future. Heart 2000; 84: 14–24PubMedCrossRef

Walker MJA. Antiarrhythmic drug research. Br J Pharmacol 2006; 147: S222–31PubMedCrossRef

Hattori Y, Hidaka T, Aisaka K, et al. Effect of SUN 1165, a new potent antiarrhythmic agent, on the kinetics of rate-dependent block of Na channels and ventricular conduction of extrasystoles. JCardiovasc Pharmacol 1988 Apr; 11(4): 407–12CrossRef

10.

Sunrythm® (pilsicainide 25 mg and 50 mg capsules): Japanese prescribing information [in Japanese]. Tokyo: Daiichi Sankyo, 2007

11.

Hattori Y, Inomata N, Aisaka K, et al. Electrophysiological actions of N-(2,6-dimethylphenyl)8-pyrrolizidine-acetamide hydrochloride hemihydrate (SUN 1165), a new antiarrhythmic agent. J Cardiovasc Pharmacol 1986; 8(5): 998–1002PubMedCrossRef

12.

Inomata N, Ishihara T, Akaike N. SUN 1165: a new antiarrhythmic Na current blocker in ventricular myocytes of guinea-pig. Comp Biochem Physiol C 1987; 87(2): 237–43PubMedCrossRef

13.

Sakai R, Inoue D, Ishibashi K, et al. Kinetics of frequency-dependent conduction delay by class I antiarrhythmic drugs in human atrium. J Cardiovasc Pharmacol 1995; 25(6): 953–60PubMedCrossRef

14.

Hattori Y, Inomata N. Modes of the Na channel blocking action of pilsicainide, a new antiarrhythmic agent, in cardiac cells. Jpn J Pharmacol 1992 Apr; 58(4): 365–73PubMedCrossRef

15.

Aisaka K, Hidaka T, Inomata N, et al. N-(2,6-dimethylphenyl)-8-pyrrolizidineacetamide hydrochloride hemihydrate (SUN 1165): a new potent and long-acting antiarrhythmic agent. Arzneimittelforschung 1985; 35(8): 1239–45PubMed

16.

Hashimoto K, Ishii M, Komori S, et al. Canine digitalis arrhythmia as a model for detecting Na-channel blocking antiarrhythmic drugs: a comparative study using other canine arrhythmia models and the new antiarrhythmic drugs, propafenone, tocainide, and SUN 1165. Heart Vessels 1985 Feb; 1(1): 29–35PubMedCrossRef

17.

Iwasa A, Okumura K, Tabuchi T, et al. Effects of pilsicainide and propafenone on vagally induced atrial fibrillation: role of suppressant effect in conductivity. Eur J Pharmacol 1998 Aug 28; 356(1): 31–40PubMedCrossRef

18.

Kojima J, Niwano S, Moriguchi M, et al. Effect of pilsicainide on atrial electrophysiologic properties in the canine rapid atrial stimulation model. Circ J 2003 Apr; 67(4): 340–6PubMedCrossRef

19.

Kawase A, Ikeda T, Nakazawa K, et al. Widening of the excitable gap and enlargement of the core of reentry during atrial fibrillation with a pure sodium channel blocker in canine atria. Circulation 2003; 107: 905–10PubMedCrossRef

20.

Ino T, Atarashi H, Kuruma A, et al. Electrophysiologic and hemodynamic effects of a single oral dose of pilsicainide hydrochloride, a new class 1c antiarrhythmic agent. J Cardiovasc Pharmacol 1998 Jan; 31(1): 157–64PubMedCrossRef

21.

Terazawa T, Suzuki M, Goto T, et al. Suppressive effect of SUN1165 on supraventricular tachycardia. Am Heart J 1991 May; 121(5): 1437–44PubMedCrossRef

22.

Kanemoto M, Shimizu A, Yamagata T, et al. Differentiation of the electrophysiological effects on the atrial myocardium between the pure Na channel blocker, pilsicainide, and flecainide. Cardiovasc Drugs Ther 2004 Jul; 18(4): 295–303PubMedCrossRef

23.

Sadanaga T, Ogawa S. Ischemia enhances use-dependent sodium channel blockade by pilsicainide, a class IC antiarrhythmic agent. J Am Coll Cardiol 1994 May; 23(6): 1378–81PubMedCrossRef

24.

Hirose M, Ohkubo Y, Takano M, et al. Mechanisms of the preventive effect of pilsicainide on atrial fibrillation originating from the pulmonary vein. Circ J 2007 Nov; 71(11): 1805–14PubMedCrossRef

25.

Horiuchi D, Iwasa A, Sasaki K, et al. Effect of pilsicainide on dominant frequency in the right and left atria and pulmonary veins during atrial fibrillation: association with its atrial fibrillation terminating effect. Eur J Pharmacol 2009 Apr 17; 608: 54–61PubMedCrossRef

26.

Kumagai K, Tojo H, Noguchi H, et al. Effects of the Na+ channel blocker pilsicainide on the electrophysiologic properties of pulmonary veins in patients with atrial fibrillation. J Cardiovasc Electrophysiol 2004 Dec; 15(12): 1396–401PubMedCrossRef

27.

Kumagai K, Nakashima H, Tojo H, et al. Pilsicainide for atrial fibrillation. Drugs 2006; 66(16): 2067–73PubMedCrossRef

28.

Sunrythm® (pilsicainide 50 mg injection): Japanese prescribing information [in Japanese]. Tokyo: Daiichi Sankyo, 2007

29.

Tsuruoka S, Ioka T, Wakaumi M, et al. Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: first case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2. Clin Pharmacol Ther 2006 Apr; 79(4): 389–96PubMedCrossRef

30.

Kim BH, Kim JR, Lim KS, et al. An open-label, single-dose, parallel-group, dose-increasing study comparing the pharmacokinetics and tolerability of pilsicainide hydrochloride in healthy Korean and Japanese male subjects. Clin Ther 2009 Mar; 31(3): 609–18PubMedCrossRef

31.

Fukumoto K, Tanemura M, Tsuchishita Y, et al. Effect of protein binding of pilsicainide on the pharmacokinetics. Drug Metab Pharmacokinet 2005 Jun; 20(3): 183–6PubMedCrossRef

32.

Ogawa R, Kishi R, Mihara K, et al. Population pharm-acokinetic and pharmacodynamic analysis of a class IC antiarrhythmic, pilsicainide, in patients with cardiac arrhythmias. J Clin Pharmacol 2006 Jan; 46(1): 59–68PubMedCrossRef

33.

Matsumoto M, Fujii Z, Kawata Y, et al. Appropriate dosing of pilsicainide hydrochloride in patients on hemodialysis. Nephron 2001 Jun; 88(2): 134–7PubMedCrossRef

34.

Atarashi H, Inoue H, Hiejima K, et al. Conversion of recent-onset atrial fibrillation by a single oral dose of pilsicainide (Pilsicainide Suppression Trial on Atrial Fibrillation): the PSTAF Investigators. Am J Cardiol 1996 Sep 15; 78(6): 694–7PubMedCrossRef

35.

Nagai S, Takeishi Y, Kubota I. Low-dose flecainide infusion followed by oral pilsicainide is highly effective and safe for paroxysmal atrial fibrillation [letter]. Cardiovasc Drugs Ther 2003 Jan; 17(1): 95–7PubMedCrossRef

36.

Okishige K, Fukunami M, Kumagai K, et al. Pharmacological conversion of persistent atrial fibrillation into sinus rhythm with oral pilsicainide: pilsicainide suppression trial for persistent atrial fibrillation II [published erratum appears in Circ J 2006 Jul; 70 (7): 945]. Circ J 2006 Jun; 70(6): 657–61PubMedCrossRef

37.

Komatsu T, Tachibana H, Sato Y, et al. A randomized study on the efficacy of intravenous cibenzoline and pilsicainide administered prior to electrical cardioversion in patients with lone paroxysmal and persistent atrial fibrillation. J Cardiol 2009 Feb; 53(1): 35–42PubMedCrossRef

38.

Kohno K, Takeuchi Y, Gomi A, et al. Efficacy and safety of a single oral dose of pilsicainide in supraventricular arrhythmia after coronary artery bypass grafting [in Japanese]. Jpn J Thorac Cardiovasc Surg 1998; 46(4): 361–7PubMedCrossRef

39.

Kumagai K, Abe H, Hiraki T, et al. Single oral administration of pilsicainide versus infusion of disopyramide for termination of paroxysmal atrial fibrillation: a multicenter trial. Pacing Clin Electrophysiol 2000 Nov; 23 (11 Pt 2): 1880–2PubMed

40.

Komatsu T, Sato Y, Tachibana H, et al. Randomized crossover study of the long-term effects of pilsicainide and cibenzoline in preventing recurrence of symptomatic paroxysmal atrial fibrillation: influence of the duration of arrhythmia before therapy. Circ J 2006 Jun; 70(6): 667–72PubMedCrossRef

41.

Tojo H, Kumagai K, Noguchi H, et al. Hybrid therapy with pilsicainide and pulmonary vein isolation for atrial fibrillation. Circ J 2005 Dec; 69(12): 1503–7PubMedCrossRef

42.

Hirao K, Okishige K, Yamamoto N, et al. Long-term efficacy of hybrid pharmacologic and ablation therapy in patients with pilsicainide-induced atrial flutter. Clin Cardiol 2005 Jul; 28(7): 338–42PubMedCrossRef

43.

Ikeda K, Kanaya T, Yamaki M, et al. Clinical efficacy of pilsicainide (Sunrythm) in patients with non-sustained ventricular tachycardia or repetitive ventricular premature contractions [in Japanese]. Ther Res 2000; 21(3): 645–52

44.

Matsumoto K, Takabatake Y, Matsuo H, et al. Efficacy and safety of antiarrhythmic agent pilsicainide hydrochloride on ventricular arrhythmias: Saitama multi center study [in Japanese]. Ther Res 1995; 16(10): 407–15

45.

Niitani H, Katoh K, Sugimoto T, et al. Clinical evaluation of pilsicainide hydrochloride (SUN 1165) in patients with supraventricular premature contractions: a multicenter double-blind dose finding study [in Japanese]. Jpn J Clin Pharmacol Ther 1992; 23(3): 557–72CrossRef

46.

Okishige K, Nishizaki M, Azegami K, et al. Pilsicainide for conversion and maintenance of sinus rhythm in chronic atrial fibrillation: a placebo-controlled, multicenter study [abstract]. Am Heart J 2000 Sep; 140(3): e1 3CrossRef

47.

Chinushi M, Komura S, Izumi D, et al. Incidence and initial characteristics of pilsicainide-induced ventricular arrhythmias in patients with Brugada syndrome. Pacing Clin Electrophysiol 2007 May; 30(5): 662–71PubMedCrossRef

48.

Haghi D, Schumacher B. Current management of symptomatic atrial fibrillation. Am J Cardiovasc Drugs 2001; 1(2): 127–39PubMedCrossRef

49.

Cardiac Arrhythmia Suppression Trial (CAST) Investigators. Preliminary report: effect of encainide and flecainide on mortality in a randomized trial of arrhythmia suppression after myocardial infarction. N Engl J Med 1989 Aug 10; 321(6): 406–12CrossRef

Titel: Pilsicainide
verfasst von: Greg L. Plosker
Publikationsdatum: 01.03.2010
Verlag: Springer International Publishing
Erschienen in: Drugs / Ausgabe 4/2010
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI: https://doi.org/10.2165/11204960-000000000-00000

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Pilsicainide

Abstract

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Abstract

Bitte loggen Sie sich ein, um Zugang zu diesem Inhalt zu erhalten

Weitere Artikel der Ausgabe 4/2010

Sodium-Glucose Co-Transport Inhibitors

Tolvaptan

Fospropofol

Pharmacotherapy Options for Locally Advanced and Advanced Cervical Cancer

Atypical Antipsychotics for Acute Manic and Mixed Episodes in Children and Adolescents with Bipolar Disorder

Pharmacological Management of Low Back Pain