Predicting drug-induced slowing of conduction and pro-arrhythmia: Identifying the 'bad' sodium current blockers

British Journal of Pharmacology

Volumn 160, Issue 1, 2010, Pages 60-76

  Lu, Hua Rong ^a   Rohrbacher, Jutta ^a   Vlaminckx, Eddy ^a   Van Ammel, Karel ^a   Yan, Gan Xin ^b   Gallacher, David J ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b Main Line Health Heart Center   (United States)

Author keywords

Conduction time; Drug; I Na; Ventricular fibrillation (VF); Ventricular tachycardia (VT)

Indexed keywords

FLECAINIDE; LIDOCAINE; SODIUM CHANNEL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; ATRIOVENTRICULAR DISSOCIATION; BRADYCARDIA; CHO CELL; CONTROLLED STUDY; DRUG PROTEIN BINDING; DRUG TARGETING; EXPERIMENTAL RABBIT; FEMALE; HEART; HEART ARRHYTHMIA; HEART CONDUCTION; HEART MUSCLE ISCHEMIA; HEART VENTRICLE FIBRILLATION; HEART VENTRICLE TACHYCARDIA; ISOLATED KIDNEY; NONHUMAN; PRACTICE GUIDELINE; PRIORITY JOURNAL; PURKINJE FIBER; QRS COMPLEX; QT PROLONGATION; REPERFUSION; SODIUM CURRENT; TRIANGULATION;

ANIMALS; ANTI-ARRHYTHMIA AGENTS; ARRHYTHMIAS, CARDIAC; CHO CELLS; CRICETINAE; CRICETULUS; DRUG EVALUATION, PRECLINICAL; ELECTRIC CONDUCTIVITY; ETHER-A-GO-GO POTASSIUM CHANNELS; FLECAINIDE; HEART CONDUCTION SYSTEM; LIDOCAINE; MYOCARDIAL REPERFUSION INJURY; PATCH-CLAMP TECHNIQUES; PURKINJE FIBERS; RABBITS; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; TACHYCARDIA, VENTRICULAR; VENTRICULAR FIBRILLATION;

EID: 77950929073     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.00646.x     Document Type: Article

References (43)

1. Aidonidis I, Brachmann J, Rizos I, Toutouzas P, Kubler W (1994). Lidocaine converts inducible ventricular fibrillation into sustained ventricular tachycardia in conscious dogs with recent myocardial infarction. Cardiology 85 : 378 387.
2. Akar FG, Spragg DD, Tunin RS, Kass DA, Tomaselli GF (2004). Mechanisms underlying conduction slowing and arrhythmogenesis in nonischemic dilated cardiomyopathy. Circ Res 95 : 717 725.
3. Alexander SPH, Mathie A, Peters JA (2009). Guide to Receptors and Channels (GRAC), 4th edn. Br J Pharmacol 158 (Suppl. 1 S1 S254.
4. Amitzur G, Shenkar N, Mueller M, Kraft P, Noviko I, Eldar M et al. (2003). Refractoriness and conduction interaction during modulation of non-ischemic ventricular fibrillation by flecainide. Cardiovasc Drugs Ther 17 : 237 247. (Pubitemid 37421741)
5. Anno T, Hondeghem LM (1990). Interactions of flecainide with guinea-pig cardiac sodium channels. Importance of activation unblocking to the voltage dependence of recovery. Circ Res 66 : 789 803. (Pubitemid 20086917)
6. Antzelevitch C (2006). Brugada syndrome. Pacing Clin Electrophysiol 29 : 1130 1159. (Pubitemid 44581402)
7. Antzelevitch C, Yan GX, Shimizu W (1999). Transmural dispersion of repolarization and arrhythmogenicity: the Brugada syndrome versus the long QT syndrome. J Electrocardiol 32 (Suppl. 158 165. (Pubitemid 30100122)
8. Bean BP, Cohen CJ, Tsien RW (1983). Lidocaine block of cardiac sodium channels. J Gen Physiol 81 : 613 642. (Pubitemid 13062306)
9. Bellemin-Baurreau J, Poizot A, Hicks PE, Armstrong JM (1994). An in vitro method for the evaluation of antiarrhythmic and antiischemic agents by using programmed electrical stimulation of rabbit heart. J Pharmacol Toxicol Methods 31 : 31 40. (Pubitemid 24093428)
10. Bezanilla F, Armstrong CM (1977). Inactivation of the sodium channel. I. Sodium current experiments. J Gen Physiol 70 : 549 566. (Pubitemid 8239321)
11. Brugada J, Boersma L, Kirchhof C, Allessie M (1991). Proarrhythmic effects of flecainide: experimental evidence for increased susceptibility to reentrant arrhythmias. Circulation 84 : 1808 1818.
12. Carmeliet E, Mubagwa K (1998). Antiarrhythmic drugs and cardiac ion channels: mechanisms of action. Prog Biophys Mol Biol 70 : 1 72. (Pubitemid 28425790)
13. Clements-Jewery H, Kanaganaygam GS, Kabra R, Curtis MJ (2006). Actions of flecainide on susceptibility to phase-2 ventricular arrhythmias during infarct evolution in rat isolated perfused hearts. Br J Pharmacol 147 : 468 475. (Pubitemid 43355044)
14. Cubeddu LX (2003). QT prolongation and fatal arrhythmias: a review of clinical implications and effects of drugs. Am J Ther 10 : 452 457.
15. Darpo B, Nebout T, Sager PT (2006). Clinical evaluation of QT/QTc interval prolongation and proarrhythmic potential for non-antiarrhythmic drugs: the International Conference on Harmonization of Technical Requirement for Registration of Pharmaceuticals for Human Use E14 guidance. J Clin Pharmacol 46 : 498 507.
16. Dubin AE, Nasser N, Rohrbacher J, Hermans AN, Marrannes R, Grantham C et al. (2005). Identifying modulators of hERG channel activity using the PatchXpress planar patch clamp. J Biomol Screen 10 : 168 181. (Pubitemid 40503503)
17. Echt DS, Liebson PR, Mitchell LB, Peters RW, Obias-Manno D, Barker AH et al. (1991). Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmias Suppression Trial. N Engl J Med 324 : 781 788.
18. Food and Drug Administration (2005). HRS: International Conference on Harmonisation; guidance on S7B nonclinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals; availability. Fed Regist 70 : 61133 61134.
19. Gellens ME, George Al, Chen L, Chahine M, Horn R, Barchi RL et al. (1992). Primary structure and functional expression of the human cardiac tetrodotoxin-insensitive voltage-dependent sodium channel. Proc Natl Acad Sci USA 89 : 554 558.
20. Greenberg HM, Dwyer EMJ, Hochman JS, Steinberg JS, Echt DS, Peters RW (1995). Interaction of ischemia and encainide/flecainide treatment: a proposed mechanism for the increased mortality in CAST I. Br Heart J 74 : 631 635.
21. Gutstein DE, Morley GE, Tamaddon H, Vaidya D, Schneider MD, Chen J et al. (2001). Conduction slowing and sudden arrhythmic death in mice with cardiac-restricted inactivation of connexin43. Circ Res 88 : 333 339. (Pubitemid 32173758)
22. Hamill OP, Marty A, Neher E, Sakmann B, Sigworth FJ (1981). Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 391 : 85 100. (Pubitemid 11012976)
23. Haverkamp W, Breithardt G, Camm AJ, Janse MJ, Rosen MR, Antzelevitch C et al. (2000). The potential for QT prolongation and pro-arrhythmia by non-anti-arrhythmic drugs: clinical and regulatory implications: report on a Policy Conference on the European Society of Cardiology. Cardiovasc Res 47 : 219 233. (Pubitemid 30625285)
24. Kou WH, Nelson SD, Lynch JJ, Montgomery DG, DiCarlo L, Lucchesi BR (1987). Effect of flecainide acetate on prevention of electrical induction of ventricular tachycardia and occurrence of ischemic ventricular fibrillation during the early postmyocardial infarction period: evaluation in a conscious canine model of sudden death. J Am Coll Cardiol 9 : 359 365.
25. Lathers CM, Schraeder PL (2002). Clinical pharmacology: drugs as a benefit and/or risk in sudden unexpected death in epilepsy? J Clin Pharmacol 42 : 123 136.
26. Levine JH, Morganroth J, Kadish AH (1989). Mechanisms and risk factors for proarrhythmias with type Ia compared with Ic antiarrhythmic drug therapy. Circulation 80 : 1063 1069. (Pubitemid 19261654)
27. Lu HR, Mariën R, Saels A, De Clerck F (2001). Species plays an important role in drug-induced prolongation of action potential duration and early afterdepolarizations in isolated Purkinje fibers. J Cardiovasc Electrophysiol 12 : 93 102. (Pubitemid 32099490)
28. Lu HR, Vlaminckx E, Hermans AN, Rohrbacher J, Van Ammel K, Towart R et al. (2008). Predicting drug-induced changes in QT interval and arrhythmias: QT-shortening drugs point to gaps in the ICHS7B guidelines. Br J Pharmacol 154 : 1427 1438.
29. Patterson E, Gibson JK, Lucchesi BR (1988). Antiarrhythmic and arrhythmogenic actions of methyl lidocaine during the recovery phase after canine myocardial infarction. Pharmacology 36 : 73 83. (Pubitemid 18037575)
30. + channels. Proc Natl Acad Sci USA 93 : 9270 9275. (Pubitemid 26282053)
31. Ranger S, Nattel S (1995). Determinants and mechanisms of flecainide-induced promotion of ventricular tachycardia in anesthetized dogs. Circulation 92 : 1300 1311.
32. Ranger S, Talajic M, Lemery R, Roy D, Nattel S (1989). Amplification flecainide-induced ventricular conduction slowing by exercise. A potentially significant clinical consequence of use-dependent sodium channel blockade. Circulation 79 : 1000 1006. (Pubitemid 19129180)
33. Roden DM (2008). Long-QT syndrome. N Engl J Med 358 : 169 176.
34. Sakai T, Ogawa S, Hosokawa M, Miyazaki T, Sakurai K, Nakamura Y (1989). Electrophysiological effects of flecainide in a canine 7 day old myocardial infarction model. Cardiovas Res 23 : 177 183. (Pubitemid 19084603)
35. Sellers TD, DiMarco JP (1984). Sinusoidal ventricular tachycardia associated with flecainide acetate. Chest 85 : 647 649. (Pubitemid 14147913)
36. Shah RR (2004). Pharmacogenetic aspects of drug-induced torsade de pointes. Drug Saf 27 : 145 172.
37. The CAST Investigators (1989). Preliminary report: effect of encainide and flecainide on mortality in a randomized trial of arrhythmia suppression after myocardial infarction. N Engl J Med 321 : 406 412.
38. Walczak T (2003). Do antiepileptic drugs play a role in sudden unexpected death in epilepsy? Drug Saf 26 : 673 683. (Pubitemid 36976129)
39. Wang D, Patel C, Cui C, Yan G-X (2008). Preclinical assessment of drug-induced proarrhythmias: role of the arterially perfused rabbit left ventricular wedge preparation. Pharmacol Ther 119 : 141 151.
40. Wyman MG, Wyman RM, Cannom DS, Criley JM (2004). Prevention of primary fibrillation in acute myocardial infarction with prophylactic lidocaine. Am J Cardiol 94 : 545 551. (Pubitemid 39165830)
41. Yan GX, Antzelevitch C (1999). Cellular basis for the Brugada syndrome and other mechanisms of arrhythmogenesis associated with ST-segment elevation. Circulation 100 : 1660 1666. (Pubitemid 29477277)
42. Yan GX, Wu Y, Liu T, Wang J, Marinchak RA, Kowey PR (2001). Phase 2 early afterdepolarization as a trigger of polymorphic ventricular tachycardia in acquired long-QT syndrome: direct evidence from intracellular recordings in the intact left ventricular wall. Circulation 103 : 2851 2856. (Pubitemid 32550076)
43. Zehender M, Kasper W, Just H (1990). Lidocaine in the early phase of acute myocardial infarction: the controversy over prophylactic or selective use. Clin Cardiol 13 : 534 539. (Pubitemid 20256069)