Evidence for a crucial modulating role of the sodium channel in the QTc prolongation related to antipsychotics

Journal of Psychopharmacology

Volumn 28, Issue 4, 2014, Pages 330-340

  Silvestre, Jordi S ^a   O'Neill, Michael F ^b   Prous, Josep R ^c  

^a UNIVERSITAT OBERTA DE CATALUNYA   (Spain)

^b Blackrock Co   (Ireland)

^c Prous Institute for Biomedical Research   (Spain)

Author keywords

Antipsychotics; hERG blockade; QTc prolongation; sodium channel; ventricular arrhythmia

Indexed keywords

AMISULPRIDE; AMOXAPINE; ARIPIPRAZOLE; ASENAPINE; BROMPERIDOL; CHLORPROMAZINE; CLOZAPINE; DROPERIDOL; HALOPERIDOL; LEVOMEPROMAZINE; MESORIDAZINE; NEUROLEPTIC AGENT; OLANZAPINE; PALIPERIDONE; PENFLURIDOL; PERICIAZINE; PERPHENAZINE; PIMOZIDE; PIPAMPERONE; PROCHLORPERAZINE; QUETIAPINE; RISPERIDONE; SERTINDOLE; SODIUM CHANNEL NAV1.5; SULPIRIDE; THIORIDAZINE; TRIFLUOPERAZINE; UNINDEXED DRUG; ZIPRASIDONE; ZOTEPINE; ERG1 POTASSIUM CHANNEL; POTASSIUM CHANNEL HERG;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG POTENCY; DRUG TISSUE LEVEL; HEART RATE; HUMAN; IC 50; LINEAR REGRESSION ANALYSIS; MULTIVARIABLE LINEAR REGRESSION ANALYSIS; PRIORITY JOURNAL; QT INTERVAL; QT PROLONGATION; ANTAGONISTS AND INHIBITORS; CHEMICALLY INDUCED; HEK293 CELL LINE; IC50; LONG QT SYNDROME; METABOLISM; PATHOPHYSIOLOGY; STATISTICAL MODEL;

ANTIPSYCHOTIC AGENTS; ETHER-A-GO-GO POTASSIUM CHANNELS; HEK293 CELLS; HUMANS; INHIBITORY CONCENTRATION 50; LINEAR MODELS; LONG QT SYNDROME; NAV1.5 VOLTAGE-GATED SODIUM CHANNEL;

EID: 84896744285     PISSN: 02698811     EISSN: 14617285     Source Type: Journal    
DOI: 10.1177/0269881113515064     Document Type: Article

References (57)

1. Agelink MW, Majewski T, Wurthmann C, et al. Effects of newer atypical antipsychotics on autonomic neurocardiac function: A comparison between amisulpride, olanzapine, sertindole, and clozapine. J Clin Psychopharmacol. 2001 ; 21: 8-13
2. Antzelevitch C. Ionic, molecular, and cellular bases of QT-interval prolongation and torsade de pointes. Europace. 2007 ; 9: iv4 - iv15
3. Antzelevitch C, Belardinelli L. The role of sodium channel current in modulating transmural dispersion of repolarization and arrhythmogenesis. J Cardiovasc Electrophysiol. 2006 ; 17: S79 - S85
4. Belardinelli L, Antzelevitch C, Fraser H. Inhibition of late (sustained/persistent) sodium current: A potential drug target to reduce intracellular sodium-dependent calcium overload and its detrimental effects on cardiomyocyte function. Eur Heart J Suppl. 2004 ; 6: 13-17
5. Belardinelli L, Antzelevitch C, Vos MA. Assessing predictors of drug-induced torsade de pointes. Trends Pharmacol Sci. 2003 ; 24: 619-625
6. Belardinelli L, Shryock JC, Fraser H. Inhibition of the late sodium current as a potential cardioprotective principle: Effects of the late sodium current inhibitor ranolazine. Heart. 2006 ; 92: iv6 - iv14
7. Cavero I, Mestre M, Guillon JM, et al. Drugs that prolong QT interval as an unwanted effect: Assessing their likelihood of inducing hazardous cardiac dysrhythmias. Expert Opin Pharmacother. 2000 ; 1: 947-973
8. Chiladakis J, Kalogeropoulos A, Arvanitis P, et al. Preferred QT correction formula for the assessment of drug-induced QT interval prolongation. J Cardiovasc Electrophysiol. 2010 ; 21: 905-913
9. Chiu PJ, Marcoe KF, Bounds SE, et al. Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels. J Pharmacol Sci. 2004 ; 95: 311-319
10. Creese I, Burt DR, Snyder SH. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science. 1976 ; 192: 481-483
11. Crumb WJ, Ekins S, Sarazan RD, et al. Effects of antipsychotic drugs on I(to), I (Na), I (sus), I (K1), and hERG: QT prolongation, structure activity relationship, and network analysis. Pharm Res. 2006 ; 23: 1133-1143
12. Curtis LH, Ostbye T, Sendersky V, et al. Prescription of QT-prolonging drugs in a cohort of about 5 million outpatients. Am J Med. 2003 ; 114: 135-141
13. De Bruin ML, Pettersson M, Meyboom RH, et al. Anti-HERG activity and the risk of drug-induced arrhythmias and sudden death. Eur Heart J. 2005 ; 26: 590-597
14. De Ponti F, Poluzzi E, Montanaro N. Organising evidence on QT prolongation and occurrence of Torsades de Pointes with non-antiarrhythmic drugs: A call for consensus. Eur J Clin Pharmacol. 2001 ; 57: 185-209
15. Desai M, Li L, Desta Z, et al. Variability of heart rate correction methods for the QT interval. Br J Clin Pharmacol. 2003 ; 55: 511-517
16. Echt DS, Liebson PR, Mitchell LB, et al. Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial. N Engl J Med. 1991 ; 324: 781-788
17. Ekins S, Crumb WJ, Sarazan RD, et al. Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel. J Pharmacol Exp Ther. 2002 ; 301: 427-434
18. Fossa AA. The impact of varying autonomic states on the dynamic beat-to-beat QT-RR and QT-TQ interval relationships. Br J Pharmacol. 2008 ; 154: 1508-1515
19. Gintant G. An evaluation of hERG current assay performance: Translating preclinical safety studies to clinical QT prolongation. Pharmacol Ther. 2011 ; 129: 109-119
20. Gintant GA, Gallacher DJ, Pugsley MK. The 'overly-sensitive' heart: Sodium channel block and QRS interval prolongation. Br J Pharmacol. 2011 ; 164: 254-259
21. Gintant GA, Su Z, Martin RL, et al. Utility of hERG assays as surrogate markers of delayed cardiac repolarization and QT safety. Toxicol Pathol. 2006 ; 34: 81-90
22. Glassman AH. Schizophrenia, antipsychotic drugs, and cardiovascular disease. J Clin Psychiatry. 2005 ; 66: 5-10
23. Gupta A, Lawrence AT, Krishnan K, et al. Current concepts in the mechanisms and management of drug-induced QT prolongation and torsade de pointes. Am Heart J. 2007 ; 153: 891-899
24. Haddad PM, Anderson IM. Antipsychotic-related QTc prolongation, torsade de pointes and sudden death. Drugs. 2002 ; 62: 1649-1671
25. Harmer AR, Valentin JP, Pollard CE. On the relationship between block of the cardiac Na channel and drug-induced prolongation of the QRS complex. Br J Pharmacol. 2011 ; 164: 260-273
26. Heist EK, Ruskin JN. Drug-induced arrhythmia. Circulation. 2010 ; 122: 1426-1435
27. Jia S, Lian J, Guo D, et al. Modulation of the late sodium current by ATX-II and ranolazine affects the reverse use-dependence and proarrhythmic liability of IKr blockade. Br J Pharmacol. 2011 ; 164: 308-316
28. Jordan D. Vagal control of the heart: central serotonergic (5-HT) mechanisms. Exp Physiol. 2005 ; 90: 175-181
29. Kannankeril PJ, Roden DM. Drug-induced long QT and torsade de pointes: Recent advances. Curr Opin Cardiol. 2007 ; 22: 39-43
30. Kellett DO, Ramage AG, Jordan D. Central 5-HT7 receptors are critical for reflex activation of cardiac vagal drive in anaesthetized rats. J Physiol. 2005 ; 563: 319-331
31. Killeen MJ. Antipsychotic-induced sudden cardiac death: Examination of an atypical reaction. Expert Opin Drug Saf. 2009a ; 8: 249-252
32. Killeen MJ. Drug-induced arrhythmias and sudden cardiac death: Implications for the pharmaceutical industry. Drug Discov Today. 2009b ; 14: 589-597
33. Kongsamut S, Kang J, Chen XL, et al. A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs. Eur J Pharmacol. 2002 ; 450: 37-41
34. Kroeze WK, Hufeisen SJ, Popadak BA, et al. H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology. 2003 ; 28: 519-526
35. Lasser KE, Allen PD, Woolhandler SJ, et al. Timing of new black box warnings and withdrawals for prescription medications. JAMA. 2002 ; 287: 2215-2220
36. Leucht S, Cipriani A, Spineli L, et al. Comparative efficacy and tolerability of 15 antipsychotic drugs in schizophrenia: A multiple-treatments meta-analysis. Lancet. 2013 ; 382: 951-962
37. Martin RL, McDermott JS, Salmen HJ, et al. The utility of hERG and repolarization assays in evaluating delayed cardiac repolarization: Influence of multi-channel block. J Cardiovasc Pharmacol. 2004 ; 43: 369-379
38. Mason JW, Ramseth DJ, Chanter DO, et al. Electrocardiographic reference ranges derived from 79,743 ambulatory subjects. J Electrocardiol. 2007 ; 40: 228-234
39. Moss AJ. The QT interval and torsade de pointes. Drug Saf. 1999 ; 21: 5-10
40. Nielsen J, Graff C, Kanters JK, et al. Assessing QT interval prolongation and its associated risks with antipsychotics. CNS Drugs. 2011 ; 25: 473-490
41. Paulussen AD, Gilissen RA, Armstrong M, et al. Genetic variations of KCNQ1, KCNH2, SCN5A, KCNE1, and KCNE2 in drug-induced long QT syndrome patients. J Mol Med. 2004 ; 82: 182-188
42. Redfern WS, Carlsson L, Davis AS, et al. Relationships between preclinical cardiac electrophysiology, clinical QT interval prolongation and torsade de pointes for a broad range of drugs: Evidence for a provisional safety margin in drug development. Cardiovasc Res. 2003 ; 58: 32-45
43. Roden DM. Drug-induced prolongation of the QT interval. N Engl J Med. 2004 ; 350: 1013-1022
44. Sager PT. Key clinical considerations for demonstrating the utility of preclinical models to predict clinical drug-induced torsades de pointes. Br J Pharmacol. 2008 ; 154: 1544-1549
45. Salvi V, Karnad DR, Panicker GK, et al. Update on the evaluation of a new drug for effects on cardiac repolarization in humans: Issues in early drug development. Br J Pharmacol. 2010 ; 159: 34-48
46. Sampson KJ, Kass RS. Molecular mechanisms of adrenergic stimulation in the heart. Heart Rhythm. 2010 ; 7: 1151-1153
47. Seeman P, Lee T, Chau-Wong M, et al. Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976 ; 261: 717-719
48. Shimizu W, Aiba T, Antzelevitch C. Specific therapy based on the genotype and cellular mechanism in inherited cardiac arrhythmias. Long QT syndrome and Brugada syndrome. Curr Pharm Des. 2005 ; 11: 1561-1572
49. Silvestre JS, Prous J. Research on adverse drug events. I. Muscarinic M3 receptor binding affinity could predict the risk of antipsychotics to induce type 2 diabetes. Methods Find Exp Clin Pharmacol. 2005 ; 27: 289-304
50. Silvestre JS, Prous JR. Comparative evaluation of hERG potassium channel blockade by antipsychotics. Methods Find Exp Clin Pharmacol. 2007 ; 29: 457-465
51. Stahl SM. Describing an atypical antipsychotic: Receptor binding and its role in pathophysiology. Prim Care Companion J Clin Psychiatry. 2003 ; 5: 9-13
52. Taggart P, Sutton P, Chalabi Z, et al. Effect of adrenergic stimulation on action potential duration restitution in humans. Circulation. 2003 ; 107: 285-289
53. Tisdale JE, Wroblewski HA, Overholser BR, et al. Prevalence of QT interval prolongation in patients admitted to cardiac care units and frequency of subsequent administration of QT interval-prolonging drugs: A prospective, observational study in a large urban academic medical center in the US. Drug Saf. 2012 ; 35: 459-470
54. Titier K, Girodet PO, Verdoux H, et al. Atypical antipsychotics: From potassium channels to torsade de pointes and sudden death. Drug Saf. 2005 ; 28: 35-51
55. Viskin S. Long QT syndromes and torsade de pointes. Lancet. 1999 ; 354: 1625-1633
56. Webster R, Leishman D, Walker D. Towards a drug concentration effect relationship for QT prolongation and torsades de pointes. Curr Opin Drug Discov Devel. 2002 ; 5: 116-126
57. Witchel HJ, Hancox JC, Nutt DJ. Psychotropic drugs, cardiac arrhythmia, and sudden death.. J Clin Psychopharmacol. 2003 ; 23: 58-77