Atrial-selective sodium channel block strategy to suppress atrial fibrillation: Ranolazine versus propafenone

Journal of Pharmacology and Experimental Therapeutics

Volumn 340, Issue 1, 2012, Pages 161-168

  Burashnikov, Alexander ^a   Belardinelli, Luiz ^b   Antzelevitch, Charles ^a  

^a MASONIC MEDICAL RESEARCH LABORATORY   (United States)

^b Gilead Sciences   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; PROPAFENONE; RANOLAZINE;

ANIMAL TISSUE; ANTIARRHYTHMIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DOG; DRUG EFFICACY; DRUG SELECTIVITY; HEART ATRIUM; HEART ATRIUM FIBRILLATION; HEART EXCITATION; HEART MUSCLE FIBER MEMBRANE POTENTIAL; HEART MUSCLE REFRACTORY PERIOD; HEART REPOLARIZATION; HEART VENTRICLE; NONHUMAN; PRIORITY JOURNAL;

ACETANILIDES; ACTION POTENTIALS; ANIMALS; ANTI-ARRHYTHMIA AGENTS; ATRIAL FIBRILLATION; DIASTOLE; DOGS; ELECTROPHYSIOLOGICAL PHENOMENA; HEART ATRIA; HEART CONDUCTION SYSTEM; HEART VENTRICLES; KINETICS; PIPERAZINES; PROPAFENONE; REFRACTORY PERIOD, ELECTROPHYSIOLOGICAL; SODIUM CHANNEL BLOCKERS;

EID: 84055178015     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.111.186395     Document Type: Article

References (39)

1. Alboni P, Botto GL, Baldi N, Luzi M, Russo V, Gianfranchi L, Marchi P, Calzolari M, Solano A, Baroffio R, et al. (2004) Outpatient treatment of recent-onset atrial fibrillation with the "pill-in-the-pocket" approach. N Engl J Med 351:2384-2391. (Pubitemid 40485990)
2. Antzelevitch C, Belardinelli L, Zygmunt AC, Burashnikov A, Di Diego JM, Fish JM, Cordeiro JM, and Thomas G (2004) Electrophysiological effects of ranolazine, a novel antianginal agent with antiarrhythmic properties. Circulation 110:904-910. (Pubitemid 39136212)
3. Antzelevitch C, Burashnikov A, Sicouri S, and Belardinelli L (2011) Electrophysiologic basis for the antiarrhythmic actions of ranolazine. Heart Rhythm 8:1281-1290.
4. Burashnikov A and Antzelevitch C (2003) Reinduction of atrial fibrillation immediately after termination of the arrhythmia is mediated by late phase 3 early afterdepolarization-induced triggered activity. Circulation 107:2355-2360. (Pubitemid 36578508)
5. Burashnikov A and Antzelevitch C (2008a) Atrial-selective sodium channel blockers: do they exist? J Cardiovasc Pharmacol 52:121-128.
6. Kur promote atrial fibrillation? Heart Rhythm 5:1304-1309.
7. Burashnikov A and Antzelevitch C (2008c) How do atrial-selective drugs differ from antiarrhythmic drugs currently used in the treatment of atrial fibrillation? J Atr Fibrillation 1:98-107.
8. Burashnikov A and Antzelevitch C (2009) Atrial-selective sodium channel block for the treatment of atrial fibrillation. Expert Opin Emerg Drugs 14:233-249.
9. Burashnikov A and Antzelevitch C (2010) New developments in atrial antiarrhythmic drug therapy. Nat Rev Cardiol 7:139-148.
10. Burashnikov A, Di Diego JM, Sicouri S, Ferreiro M, Carlsson L, and Antzelevitch C (2008) Atrial-selective effects of chronic amiodarone in the management of atrial fibrillation. Heart Rhythm 5:1735-1742.
11. Burashnikov A, Di Diego JM, Zygmunt AC, Belardinelli L, and Antzelevitch C (2007) Atrium-selective sodium channel block as a strategy for suppression of atrial fibrillation: differences in sodium channel inactivation between atria and ventricles and the role of ranolazine. Circulation 116:1449-1457.
12. Kur block. Am J Physiol Heart Circ Physiol 286:H2393-H2400.
13. Burashnikov A, Zygmunt AC, Di Diego JM, Linhardt G, Carlsson L, and Antzelevitch C (2010) AZD1305 exerts atrial predominant electrophysiological actions and is effective in suppressing atrial fibrillation and preventing its reinduction in the dog. J Cardiovasc Pharmacol 56:80-90.
14. Carvas M, Nascimento BC, Acar M, Nearing BD, Belardinelli L, and Verrier RL (2010) Intrapericardial ranolazine prolongs atrial refractory period and markedly reduces atrial fibrillation inducibility in the intact porcine heart. J Cardiovasc Pharmacol 55:286-291.
15. Delgado C, Tamargo J, and Tejerina T (1985) Electrophysiological effects of propafenone in untreated and propafenone-pretreated guinea-pig atrial and ventricular muscle fibres. Br J Pharmacol 86:765-775. (Pubitemid 16211353)
16. Fuster V, Rydén LE, Cannom DS, Crijns HJ, Curtis AB, Ellenbogen KA, Halperin JL, Kay GN, Le Huezey JY, Lowe JE, et al. (2011) 2011 ACCF/AHA/HRS focused updates incorporated into the ACC/AHA/ESC 2006 guidelines for the management of patients with atrial fibrillation: a report of the American College of Cardiology Foundation/American Heart Association Task Force on Practice Guidelines developed in partnership with the European Society of Cardiology and in collaboration with the European Heart Rhythm Association and the Heart Rhythm Society. J Am Coll Cardiol 57:e101-e198.
17. Grant AO (1996) Propafenone: an effective agent for the management of supraventricular arrhythmias. J Cardiovasc Electrophysiol 7:353-364.
18. Gross GJ and Castle NA (1998) Propafenone inhibition of human atrial myocyte repolarizing currents. J Mol Cell Cardiol 30:783-793. (Pubitemid 28190722)
19. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals 7th ed. Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington DC.
20. Koren MJ, Crager MR, and Sweeney M (2007) Long-term safety of a novel antianginal agent in patients with severe chronic stable angina: the Ranolazine Open Label Experience (ROLE). J Am Coll Cardiol 49:1027-1034. (Pubitemid 46349506)
21. Kumar K, Nearing BD, Carvas M, Nascimento BC, Acar M, Belardinelli L, and Verrier RL (2009) Ranolazine exerts potent effects on atrial electrical properties and abbreviates atrial fibrillation duration in the intact porcine heart. J Cardiovasc Electrophysiol 20:796-802.
22. Lemmens-Gruber R, Marei H, and Heistracher P (1997) Electrophysiological properties of the propafenone-analogue GE 68 (1-[3-(phenylethyl)-2-benzofuryl]- 2- (propylamino)-ethanol) in isolated preparations and ventricular myocytes of guinea- pig hearts. Naunyn Schmiedebergs Arch Pharmacol 355:230-238. (Pubitemid 27065313)
23. Miles RH, Passman R, and Murdock DK (2011) Comparison of effectiveness and safety of ranolazine versus amiodarone for preventing atrial fibrillation after coronary artery bypass grafting. Am J Cardiol 108:673-676.
24. Murdock DK, Kersten M, Kaliebe J, and Larrain G (2009) The use of oral ranolazine to convert new or paroxysmal atrial fibrillation: a review of experience with implications for possible "pill in the pocket" approach to atrial fibrillation. Indian Pacing Electrophysiol J 9:260-267.
25. Murdock DK, Overton N, Kersten M, Kaliebe J, and Devecchi F (2008) The effect of ranolazine on maintaining sinus rhythm in patients with resistant atrial fibrillation. Indian Pacing Electrophysiol J 8:175-181.
26. Murdock DK, Reiffel JA, Kaliebe JW, and Larrian G (2010) The conversion of paroxysmal of initial onset of atrial fibrillation with oral ranolazine: implications for "pill in the pocket" approach in structural heart disease. J Am Coll Cardiol 55:A6.E58.
27. Pandit SV, Zlochiver S, Filgueiras-Rama D, Mironov S, Yamazaki M, Ennis SR, Noujaim SF, Workman AJ, Berenfeld O, Kalifa J, et al. (2011) Targeting atrioventricular differences in ion channel properties for terminating acute atrial fibrillation in pigs. Cardiovasc Res 89:843-851.
28. Ravens U and Wettwer E (2011) Ultra-rapid delayed rectifier channels: molecular basis and therapeutic implications. Cardiovasc Res 89:776-785.
29. Scirica BM, Morrow DA, Hod H, Murphy SA, Belardinelli L, Hedgepeth CM, Molhoek P, Verheugt FW, Gersh BJ, McCabe CH, et al. (2007) Effect of ranolazine, an antianginal agent with novel electrophysiological properties, on the incidence of arrhythmias in patients with non ST-segment elevation acute coronary syndrome: results from the Metabolic Efficiency With Ranolazine for Less Ischemia in Non ST-Elevation Acute Coronary Syndrome Thrombolysis in Myocardial Infarction 36 (MERLIN-TIMI 36) randomized controlled trial. Circulation 116:1647-1652. (Pubitemid 47537839)
30. Sicouri S, Belardinelli L, Carlsson L, and Antzelevitch C (2009) Potent antiarrhythmic effects of chronic amiodarone in canine pulmonary vein sleeve preparations. J Cardiovasc Electrophysiol 20:803-810.
31. Spinelli W, Parsons RW, and Colatsky TJ (1992) Effects of WAY-123,398, a new class III antiarrhythmic agent, on cardiac refractoriness and ventricular fibrillation threshold in anesthetized dogs: a comparison with UK-68798, E-4031, and dlsotalol. J Cardiovasc Pharmacol 20:913-922. (Pubitemid 23001457)
32. Szél T, Koncz I, Jost N, Baczkó I, Husti Z, Virág L, Bussek A, Wettwer E, Ravens U, Papp JG, et al. (2011) Class I/B antiarrhythmic property of ranolazine, a novel antianginal agent, in dog and human cardiac preparations. Eur J Pharmacol 662:31-39.
33. Wang GK, Calderon J, and Wang SY (2008) State- and use-dependent block of muscle Nav1.4 and neuronal Nav1.7 voltage-gated Na channel isoforms by ranolazine. Mol Pharmacol 73:940-948. (Pubitemid 351397898)
34. Wettwer E, Hála O, Christ T, Heubach JF, Dobrev D, Knaut M, Varró A, and Ravens U (2004) Role of IKur in controlling action potential shape and contractility in the human atrium: influence of chronic atrial fibrillation. Circulation 110:2299-2306. (Pubitemid 39407330)
35. Whalley DW, Wendt DJ, and Grant AO (1995) Basic concepts in cellular cardiac electrophysiology: Part II: Block of ion channels by antiarrhythmic drugs. PACE 18:1686-1704.
36. Wiesfeld AC, De Langen CD, Crijns HJ, Bel KJ, Hillege HL, Wesseling H, and Lie KI (1996) Rate-dependent effects of the class III antiarrhythmic drug almokalant on refractoriness in the pig. J Cardiovasc Pharmacol 27:594-600.
37. Wilson SR, Scirica BM, Braunwald E, Murphy SA, Karwatowska-Prokopczuk E, Buros JL, Chaitman BR, and Morrow DA (2009) Efficacy of ranolazine in patients with chronic angina observations from the randomized, double-blind, placebocontrolled MERLIN-TIMI (Metabolic Efficiency With Ranolazine for Less Ischemia in Non-ST-Segment Elevation Acute Coronary Syndromes) 36 Trial. J Am Coll Cardiol 53:1510-1516.
38. Wu L, Shryock JC, Song Y, Li Y, Antzelevitch C, and Belardinelli L (2004) Antiarrhythmic effects of ranolazine in a guinea pig in vitro model of long-QT syndrome. J Pharmacol Exp Ther 310:599-605. (Pubitemid 38992327)
39. Zygmunt AC, Nesterenko VV, Rajamani S, Hu D, Barajas-Martinez H, Belardinelli L, and Antzelevitch C (2011) Mechanisms of atrial-selective block of Na channel by ranolazine I. Experimental analysis of the use-dependent block. Am J Physiol Heart Circ Physiol 301:H1606-H1614.