NEW POSSIBILITIES OF PHARMACOLOGICAL CARDIOVERSION OF NEWLY DEVELOPED PAROXYSM OF ATRIAL FIBRILLATION


Cite item

Full Text

Open Access Open Access
Restricted Access Access granted
Restricted Access Subscription or Fee Access

Abstract

Atrial fibrillation (AF) is one of the most common cardiac arrhythmias. The review presents the current possibilities of pharmacological cardioversion of AF paroxysm, the mechanisms of action which are applied in practical cardiology antiarrhythmics (AAS) of the various classes are presented. One of these new AAS is vernakalant (drug formulation - solution for intravenous administration), the mechanism of antiarrhythmic action which is associated with selective inhibition of atrial mostly voltage-dependent potassium channels, especially potassium channels delayed rectifier current (IKur) and channels activated by acetylcholine (KAch). Furthermore, vernakalant inhibits frequency-dependent and voltage-dependent sodium channels as well localized in the atria. The data on the pharmacokinetics of vernakalant and the results of its clinical application. Evaluating the results of numerous clinical studies, we can conclude that the new AAS vernakalant is effective and safe in relieving the AF, which lasts from 3 hours to 7 days. The initial dose is 3 mg/kg is administered intravenously over 10 min, with no effect after 15 minutes possible re-introduction in dose of 2 mg/kg. However, the probability of restoring sinus rhythm in the absence of the effect of the first dose is significantly reduced. With a longer period the AF or TA effectiveness of the drug is extremely low. Good clinical effect of vernakalant, and provides for AF, occurred after cardiac surgery. Ability of vernakalant to cause ventricular arrhythmias (ventricular fibrillation, ventricular tachycardia type "feast") appears minimal. In general, the researchers indicate good tolerability of vernakalant.

Full Text

Restricted Access

About the authors

V. V Cheltsov

Russian Peoples' Friendship University

Email: vcheltsov@mail.ru
MD, professor of Department of General and Clinical Pharmacology, Medical Faculty 117198, Moscow, 8 Mikulo-Maklaya St.

Yu. Sh Guschina

Russian Peoples' Friendship University

Email: gushchina@mail.ru
PhD, Associate Professor, Department of General and Clinical Pharmacology, Medical Faculty 117198, Moscow, 8 Mikulo-Maklaya St.

T. S Illarionova

Russian Peoples' Friendship University

Email: illarionova@med.rudn.ru
PhD, Associate Professor, Department of General and Clinical Pharmacology, Medical Faculty 117198, Moscow, 8 Mikulo-Maklaya St.

E. A Korovyakova

Russian Peoples' Friendship University

Email: etinakor@mait.ru
PhD, Associate Professor, Department of General and Clinical Pharmacology, Medical Faculty 117198, Moscow, 8 Mikulo-Maklaya St.

A. I Martynov

A.I. Evdokimov Moscow State Medical and Dental University

Email: mailbox@rnmot.ru
academician of Russian Academy of Sciences, MD, professor of Department of Hospital Therapy № 1, Medical Faculty 127473, Moscow, 2О/1 Delegatskaya St.

References

  1. Camm A.J., Kirchhof P., Lip G.Y.N., Schotten U., Savelieva I., Ernst S., Van Gelder I.C., Al-Attar N., Hindricks G., Prendergast B., Hei dbuchel H., Alfieri O., Angelini A., Atar D., Colonna P., De Caterina R., De Sutter J., Goette A., Gorenek B., Heldal M., Hohloser S.H., Kolh P., Le Heuzey J.Y., Ponikowski P., Rutten F.H. Guidelines for the management of atrial fibrillation: The Task Force for the Management of Atrial Fibrillation of the European Society of Cardiology (ESC). Eur. Heart J. 2010;31 (19):2369-429.
  2. Fuster V., Rydén L.E., Cannom D.S., Crijns H.J., Curtis A.B., Ellenbogen K.A., Halperin J.L., Le Heuzey J.-V., Kay G.N., Lowe J.E., Olsson S.B., Prystowsky E.N., Tamargo J.L., Wann S. ACC/AHA/ESC 2006 guidelines for the management of patients with atrial fibrillation: full text: 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. Europace. 2006;8(9):651-745.
  3. Naccarelli G.V., Varker H., Lin J., Schulman K.L. Increasing prevalence of atrial fibrillation and flutter in the United States. Am. J. Cardiol. 2009;104:1534-9.
  4. Burashnikov A., Antzelevitch Ch. Novel pharmacological target for the rhythm control management of atrial fibrillation. Pharmacol. Ther. 2011;132:2300м13.
  5. Benjamin E.J., Chen P.S., Bild D.E., Mascette A.M., Albert C.M., Alonso A., Calkins H., Connolly S.J., Curtis A.B., Darbar D., Ellinor P.T., Go A.S., Goldschlager N.F., Heckbert S.R., Jalife J., Kerr C.R., Levy D., Lloyd-Jones D.M., Massie B.M., Nattel S., Olgin J.E., Packer D.L., Po S.S., Tsang T.S., Van Wagoner D.R., Waldo A.L., Wyse D.G. Prevention of atrial fibrillation: report from a national heart, lung, and blood institute workshop. Circulation. 2009;119;606-18.
  6. Rich M.W. Epidemiology of atrial fibrillation. J. Interv. Cardiol. Electrophysiol. 2009;25(1):3-8.
  7. Zaku A., Bendejlid K. Are we contributing to the epidemic? Exp. Clin. Cardiol. 2014;20(1):1949-52.
  8. Amar D.O., Thorvaldsson S., Manolio T.A., Thorgeirsson G., Kristjansson K., Hakonarson H. Familial aggregation of atrial fibrillation in Iceland. Eur. Heart. J. 2006;27(6):708-12.
  9. Watanabe H., Tanabe N., Watanabe T., Darbar D., Roden D.M., Sasaki S., Aizawa Y. Metabolic syndrome and risk of development of atrial fibrillation: the Niigata preventive medicine study. Circulation. 2008;117(10):1255-60.
  10. Rosengren A., Hauptman P.J., Lappas G., Olsson L., Wilhelmsen L., Swedberg K. Big men and atrial fibrillation: effects of body size and weight gain on risk of atrial fibrillation in men. Eur. Heart. J. 2009;30(9):1 113-20.
  11. Gami A.S., Pressman G., Caples S.M., Kanagala R., Gard J.J., Davison D.E., Malouf J.F., Ammash N.M., Friedman P.A., Somers V.K. Association of atrial fibrillation and obstructive sleep apnea. Circulation. 2004;110(4):364-7.
  12. O'Keefe J.H., Patil H.R., Lavie C.J., Magalski A., Vogel R.A., McCullough P.A. Potential adverse cardiovascular effects from excessive endurance exercise. Mayo Clin. Proc. 2012;87( 6):587-95.
  13. Smith M.B., May H.T., Blair T.L., Anderson J.L., Muhlestein J.B., Horne B.D., Lappe D.L., Day J.D., Crandal B.G., Weiss P., Osborn J.S., Bunch T.J. Vitamin D excess is significantly associated with risk of atrial fibrillation. Circulation. 2O1 1;124:A14699.
  14. Schnabel R.B., Larson M.G., Yamamoto J.F., Sullivan L.M., Pencina M.J., Meigs J.B., Tofler G.H., Selhub J., Jacgues P.F., Wolf P.A., Magnani J.W., Ellinor P.T., Wang T.J., Levy D., Vasan R.S., Benjamin E.J. Relations of biomarkers of distinct pharmacological pathways and atrial fibrillation incidence in the community. Circulation. 2010;121 :200-7.
  15. Patton K.K., Ellinor P.T., Heckbert S.R., Christenson R.H., DeFilippi C., Gottdiener J.S., Kronmal R.A. N-terminal pro-B-type natriuretic peptide is a major predictor of the development of atrial fibrillation: the Cardiovascular Health Study. Circulation. 2009;120:1768-74.
  16. Wijffels M.C., Kirchhof Ch.J., Dorland R., Allessie M.A. Atrial fibrillation begets atrial fibrillation. A Study in Awake Chronically Instrumented Goats. Circulation. 1995;92:1954-68.
  17. Nakajima H., Nakajima H.O., Salcher O., Dittiè A.S., Dembowsky K., Jing S., Field L.J. Atrial but not ventricular fibrosis in mice expressing a mutant transforming growth factor-B1 transgene in the heart. Circ. Res. 2000;86:571-9.
  18. Burashnikov A. Are there atrial selective predominant targets for "upstream" atrial fibrillation. PubMed: 8853021.
  19. Kannel W.B., Wolf P.A., Benjamin E.J., Levy D. Prevalence, incidence, prognosis, and predisposing conditions for atrial fibrillation: population-based estimates. Am. J. Cardiol. 1998;82:2-9.
  20. Curtis A.B., Gersh B.J., Corley S.D., DiMarco J.P., Domanski M.J., Geller N., Greene H.L., Kellen J.C., Mickel M., Nelson J.D., Rosenberg Y., Schron E., Shemanski L., Waldo A.L., Wyse D.G.; AFFIRM Investigators. Clinical factors that influence response to treatment strategies in atrial fibrillation: the Atrial Fibrillation Follow-up Investigation of Rhythm Management (AFFIRM) Study. Am. Heart J. 2005;149:645-9.
  21. Tsai C.T., Lai L.P., Kuo K.T., Hwang J.J., Hsieh C.S., Hsu K.L., Tseng C.D., Tseng Y.Z., Chiang F.T., Lin J.L. Angiotensin II activates signal transducer and activators of transcription З via Racl in atrial myocytes and fibroblasts: implication for the therapeutic effect of statin in atrial structural remodeling. Circulation 2008;117:344-55.
  22. Burstein B., Libby E., Calderone A., Nattel S. Differential behaviors of atrial versus ventricular fibroblasts: a potential role for platelet-derived growth factor in atrial-ventricular remodeling differences. Circulation 2008;117:1630-41.
  23. Mason P.K., DiMarco J.P. New Pharmacological Agents for Arrhythmias. Circ. Arrhythm. Electrophysiol. 2009;2:588-97.
  24. Рекомендации ВНОК и ВНОА. 201 1 :З5
  25. Рекомендации ВНОК и ВНОА. 201 1 :З4
  26. Echt D.S., Liebson P.R., Mitchel L.B., Peters R.W., Obias-Manno D., Barker A.H., Arensberg D., Baker A., Friedman L., Greene H.L. Mortality and morbidity in patients receiving encainide, flecainide or placebo: the Cardiac Arrhythmia Suppression Trial. N. Engl. J. Med. 1991;324:781-8.
  27. Waldo A.L., Camm A.J., de Ruyter H., Friedman P.L., MacNeil D.J., Pauls J.F., Pitt B., Pratt C.M., Schwartz P.J., Veltri E.P. Effect of d-sotalol on mortality in patients with left ventricular dysfunction after recent and remote myocardial infarction. Lancet. 1996;348:7-12.
  28. Coplen S.E., Antman E.M., Berlin J.A., Hewitt P., Chalmers T.C. Efficacy and safety of guinidine therapy for maintenance of SR after cardioversion: a meta-analysis of randomized clinical trials. Circulation. 1990;82:1106-16.
  29. Lafuente C., Mouly S., Longas-Tejero M.A., Mahe I., Bergmann J.F. Antiarrhythmic drugs for maintaining sinus rhythm after cardioversion of atrial fibrillation. Arch. Intern. Med. 2006;166:719-28.
  30. Roy D., Talajic M., Dorian P., Connolly S., Eisenberg M.J., Green M., Kus T., Lambert J., Dubuc M., Gagné P., Nattel S., Thibault В. Amiodarone to prevent recurrence of atrial fibrillation. N. Engl. J. Med. 2000;342:913-20.
  31. Morrow J.P., Cannon C.P., Reiffel J.A. New antiarrhythmic drugs for establishing sinus rhythm in atrial fibrillation: what are our therapies likely to be by 2010 and beyond? Am. Heart. J. 2007;154:824-9.
  32. Kobel L., Torp-Pedersen J.J., McMurray J.V., Gøtzsche 0., Lévy S., Crijns H., Amlie J., Carlsen J.; Dronedarone Study Group. Increased mortality after dronedarone therapy for severe heart failure. N. Engl. J. Med. 2008;358(25):2678-87.
  33. Connolly S.J., Camm A.J., Halperin J.L. Dronedarone in high-risk permanent atrial fibrillation. N. Engl. J. Med. 2O11 ;365(24):2268-76.
  34. Sharif M.N., Wyse D.G. Atrial fibrillation: overview of therapeutic trials. Can. J. Cardiol. 1998;14:1241-54.
  35. Nichol G., McAlister F., Pham В., Laupacis A., Shea В., Green M., Tang A., Wells G. Meta-analysis of randomized controlled trials of the effectiveness of antiarrhythmic agents at promoting sinus rhythm in patients with atrial fibrillation, Heart. 2002;87:535-43.
  36. Van Gelderl C., Tuinenburg A.E., Schoonderwoerd B.S., Tieleman R.G., Crijns H.J. Pharmacologic versus direct-current electrical cardioversion of atrial fibrillation. Am. J. Cardiol. 1999;84(suppl 9A):147-51.
  37. Aronov W.S. Etiology, pathophysiology and treatment of atrial fibrillation: part 1. Cardiol. Rev. 2008;16:181-8.
  38. Khaykin Ya, Shamiss Y. Current issues in atrial fibrillation ISRN Cardiol. 2012;376071 :1-10.
  39. Fedida D., Orth P.M.R., Chen J.Y., Lin S., Plouvier B., Jung G., Ezrin A.M., Beatch G.N. The mechanism of atrial antiarrhythmic action of RSD1235. J. Cardiovasc. Electrophysiol. 2005;16(11):1 227-38.
  40. Wang Z.G., Fermini B., Nattel S. Sustained depolarization-induced outward current in human atrial myocytes: evidence for a novel delayed rectifier K+ current similar to Kv1.5 cloned channel currents. Cir. Res. 1993;73:1061-76.
  41. Nattel S. 2006, цит. по Burashnikov A., Antzelevitch Ch. How do atrial-selective drugs differ from antiarrhythmic drugs current used in the treatment of atrial fibrillation? J. Atr. Fibrillation. 2008;1(2):98-107.
  42. Grant A.O. Cardiac ion channels. Circ. Arrhythm. Electrophysiol. 2009;2:185-94.
  43. Cheng J.W.M., Rybak I. Pharmacotherapy options in atrial fibrillation. Clin. Med. Ther. 2009;1 :21 5-30.
  44. Burashnikov A., Antzelevitch A. New pharmacological strategies for the treatment of atrial fibrillation. Ann. Noninvasive Electrocardiol. 2009;14(3):290-300.
  45. Fedida D. Vernakalant (RSD1235): a novel, atrial-selective antifibrillatory agent. Expert. Opin. Investig. Drugs. 2007;16:519-32.
  46. Dorian P., Pinter A., Mangat I., Korley V., Cvitkovic S.S., Beatch G.N. The effect of vernakalant (RSD1235), an investigational antiarrhythmic agent, on atrial electrophysiology in human. J. Cardiovasc. Pharmacol. 2007;50(1):35-40.
  47. Burashnikov A., Pourrier M., Gibson J.K., Lynch J.J., Antzelevitch C. Rate-dependent effects of vernakalant in the isolated nonremodeled canine left atrial are primarily due to block of the sodium channel. Comparison with ranolazine and dl-sotalol. Circ. Arrhythm. Electrophysiol. 2012;5:400-8.
  48. Orth P.M.R., Hesketh J.C., Mak C.K.H., Yang Y., Lin S., Beatch G.N., Ezrin A.M., Fedida D. RSD1235 blocks late INa and supresses early afterdepolarization and torsades de pointes induced by class III agents. Cardiovasc. Res. 2006;70:486-96.
  49. Dorian P., Mangat I., Korley V. Electrophysiological properties of an atrial selective antiarrhythmic agent, RSD1235, in humans. Can. J. Cardiol. 2004;20:198D.
  50. Ezrin A.M. цит. по Finnin M. Vernakalant: a novel agent for the termination of atrial fibrillation. Am. J. Health Syst. Pharm. 2010;67(14):1157-64.
  51. Mao Z.L., Wheeler J.J., Clohs L., Beatch G.N., Keirns J. Pharmacokinetics of novel atrial-selective antiarrhythmic agent vernakalant hydrochloride injection (RSD1235): influence of CYP2D6 expression and other factors. J. Clin. Pharmacol. 2009;49(1):17-29.
  52. Roy D., Rowe B.H., Steill I.G., Coutu B., Ip J.H., Phaneuf D., Lee J., Vidaillet H., Dickinson G., Grant S., Ezrin A.M., Beatch G.N.; CRAFT Investigators. A randomized controlled trial of RSD1235, a novel antiarrhythmic agent in the treatment of recent onset atrial fibrillation. JACC. 2004;44:2355-61.
  53. http://www.fda.gov/ohrms/dockets/ac/07/briefing/2007-4327b1-01-astellas-backgrounder.pdf.
  54. Roy D., Pratt C.M., Torp-Pedersen Ch., Wyse D.G., Toft E., Juul-Moller S., Nielsen T., Rasmussen S.L., Stiell I.G., Coutu B., Ip J.H., Pritchett E.L., Camm A.J.; Atrial Arrhythmia Conversion Trial Investigators. Vernakalant hydrochloride for rapid conversion of atrial fibrillation. A phase 3, randomized, placebo-controlled trial. Circulation. 2008;117:1 518-25.
  55. Roy D., Rowe B.H., Stiell I.G., Coutu B., Ip J.H., Phaneuf D., Lee J., Vidaillet H., Dickinson G. Grant S., Ezrin A.M., Beatch G.N.; CRAFT Investigators. A randomized, controlled trial of RSD1235, a novel anti-arrhythmic agent in the treatment of recent onset atrial fibrillation. J. Am. Coll. Cardiol. 2004;44:2355-61.
  56. Hravnak M., Hoffman L.A., Saul M.I., Zullo T.G., Whitman G.R., Griffith B.P. Predictors and impact of atrial fibrillation after isolated coronary artery bypass grafting. Crit. Care. Med. 2002;30(2):33-7.
  57. Longnarangsin K. Postoperative atrial fibrillation. Med. Clin. North Am. 2008;92(1):87-99.
  58. Kowey P.R., Dorian P., Mitchel L.B., Pratt C.M., Roy D., Schwartz P.J., Sadowski J., Sobczyk D., Bochenek A., Toft E; Atrial Arrhyth mia Conversion Trial Investigators. Vernakalant hydrochloride for the rapid conversion of atrial fibrillation after cardiac surgery: a randomized, double-blind, placebo-controlled trial. Circ. Arrhythmia Electrophysiol. 2009;2(6):652-9.

Supplementary files

Supplementary Files
Action
1. JATS XML

Copyright (c) 2015 Bionika Media

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies