Assessment of proarrhythmic activity of chloroquine in in vivo and ex vivo rabbit models

Journal of Pharmacology and Pharmacotherapeutics

Volumn 4, Issue 2, 2013, Pages 116-124

  Khobragade, Shailaja B ^a   Gupta, Pankaj ^b   Gurav, Prashant ^c   Chaudhari, Girish ^c   Gatne, Madhumanjiri M ^c   Shingatgeri, Vyas M ^a  

^a RANBAXY RESEARCH LABORATORIES   (India)

^b Central Research Institute for Homoeopathy   (India)

^c BOMBAY VETERINARY COLLEGE   (India)

Author keywords

1 Adrenoceptor stimulation; chloroquine; clofilium; ex vivo rabbit model; in vivo rabbit model; torsade de pointes

Indexed keywords

ACETYLCHOLINE; ALPHA 1 ADRENERGIC RECEPTOR; CHLORALOSE; CHLOROQUINE; CLOFILIUM; METHOXAMINE; PENTOBARBITAL; PROPRANOLOL; SODIUM CHLORIDE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; ATRIOVENTRICULAR BLOCK; CONTINUOUS INFUSION; CONTROLLED STUDY; DISEASE MODEL; ELECTROCARDIOGRAPHY; EX VIVO STUDY; HEART ARRHYTHMIA; HEART DEPOLARIZATION; HEART RATE; HEART REPOLARIZATION; HEART VENTRICLE EXTRASYSTOLE; HEART VENTRICLE FIBRILLATION; HEART VENTRICLE TACHYCARDIA; IN VIVO STUDY; ISOLATED HEART; MEAN ARTERIAL PRESSURE; NONHUMAN; PR INTERVAL; QT INTERVAL; RABBIT; RECEPTOR UPREGULATION; RR INTERVAL; TORSADE DES POINTES;

EID: 84877139812     PISSN: 0976500X     EISSN: None     Source Type: Journal    
DOI: 10.4103/0976-500X.110892     Document Type: Article

References (30)

1. Woosley RL: Drugs that prolong the QT interval and/or induce Torsades de pointes (Arizon CERT web site) Available from: http://www.azcert.org/medical- pros/drug-lists/browse-drug-list.cfm. [Last accessed on 2012 March 02].
2. Haverkamp W, Breithardt G, Camm AJ, Janse MJ, Rosen MR, Antzelevitch C, et al. The potential for QT prolongation and proarrhythmia by non-antiarrhythmic drug: Clinical and regulatory implications. Report on a conference of the European society of cardiology. Eur Heart J 2000;21:1216-31.
3. The non-clinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals ICH Topic S7B guideline. (CPMP/ICH/423/02). Nov 2005.
4. Morganroth J. Comparative efficacy of oral mexiletine and quinidine in benign or potentially lethal ventricular arrhythmia. Am J Cardiol 1987;60:1276-81.
5. Lawrence CL, Pollard CE, Hammond TG, Valentine JP. Non-clinical proarrhythmia models: Predicting torsades de pointes. J Pharmacol Toxicol Methods 2005;52:46-59.
6. Crumb WJ, Wible B, Arnold DJ, Payne PJ, Brown AM. Blockade of multiple human cardiac potassium currents by the antihistamine terfenadine: Possible mechanism for terfenadine-associated cardiotoxicity. Mol Pharmacol 1995;47:181-90.
7. Castot A, Rapoport P, Coz PL, Monlun E, Pillet O, Cochard JF, et al. Prolonged QT-interval with halofantrine. Lancet 1993;341:1541-2.
8. Nosten F, Terkuile FO, Luxemburger C, Woodrow C, Chongsuphajaisiddhi T, White NJ, et al. Cardiac effects of antimalarial treatment with halofantrine. Lancet 1993;341:1054-6.
9. Lu HR, Vlaminckx E, Van de water A, Rohrbacher J, Herman A, Gallacher DJ. In vitro experimental models for the risk assessment of antibiotic-induced QT prolongation. Eur J Pharmacol 2006;553:229-39.
10. Sanchez-Chapula JA, Salinas-Stefanon E, Torres-Jacome J, Banavides-Haro DE, Navarro-Polanco RA. Blockade of currents by antimalarial drug chloroquine in feline ventricular myocytes. J Pharmacol Exp Ther 2001;297:437-45.
11. Carlsson L, Almgren O, Duker G. QTU-prolongation and Torsade de pointes induced by putative class III antiarrhythmic agents in the rabbit-etiology and interventions. J Cardiovasc Pharmacol 1990;16:276-85.
12. Farkas A, Lepran I, Papp JG. Comparison of antiarrhythmic and the proarrhythmic effect of almokalant in anesthetized rabbits. Eur J Pharmacol 1998;346:245-53.
13. Buchanan LV, Kabell G, Brunden MN, Gibson JK. Comparative assessment of ibutilide, D-sotalol, clofilium, E-4031 and UK-68, 798 in a rabbit model of proarrhythmia. J Cardiovasc Pharmacol 1993;220:540-9.
14. D'Alonzo AJ, Zhu JL, Darbenzio RB. Effects of class III antiarrhythmic agents in an in vitro rabbit model of spontaneous torsades de pointe. Eur J Pharmacol 1999;369:57-64.
15. Farkas A, Batey AJ, Coker SJ. How to measure electrocardiograph QT interval in the anaesthetized rabbit. J Pharmacol Toxicol Methods 2004;50:175-85.
16. Farkas A, Lepran I, Papp JG. Proarrhythmic effects of intravenous quinidine, amidarone, D-sotalol and almokalant in the anaesthetized rabbit model of Torsades de pointes. J Cardiovasc Pharmacol 2002;39:287-97.
17. Harris L, Downar E, Shaikh NA, Chen T. Antiarrhythmic potential of chloroquine: New use for an old drug. Can J Cardiol 1988;4:295-300.
18. Vincze D, Farkas AS, Rudas L, Makra P, Csýk N, Lepran I, et al. Relevance of anesthesia for dofetilide-induced torsades de pointes in α1-adrenoceptor stimulated rabbits. Br J Pharmacol 2008;153:75-89.
19. White CM, Xie J, Chow MS, Kluger J. Prophylactic magnesium to decrease the arrhythmogenic potential of class III antiarrhythmic agents in a rabbit model. Pharmacotherapy 1999;19:635-40.
20. Orth PM, Hesketh JC, Mak CK, Yang Y, Lin S, Beatch GN, et al. RSD 1235 blocks late INa and suppresses early after depolarizations and torsade de pointes induced by class III agents. Cardiovasc Res 2006;70:486-96.
21. Shimizu W, McMahon B, Antzelevitch C. Sodium pentobarbital reduces transmural dispersion of repolarization and prevent. J Cardiovasc Electrophysiol 1999;10:154-64.
22. Westfall TC, Westfall David P. Adrenergic agonists and antagonists. In: Brunton LL, Chabner BA, Knollmann BC, editors. Goodman and Gilman's manual of pharmacology and therapeutics. 12 th ed. USA: McGraw-Hill companies; 2008. p. 277-334.
23. Braun AP, Fedida D, Clark RB, Giles WR. Intracellular mechanisms for α1-adrenergic regulation of the transient outward current in rabbit atrial myocytes. J Physiol 1990;431:689-712.
24. Choi BR, Burton F, Salama G. Cystolic Ca 2+ triggers early after depolarization and torsode de pointes in rabbit hearts with type 2 long QT syndrome. J Physiol 2002;543:615-31.
25. Farkas AS, Acsai K, Toth A, Dezsi L, Orosz O, Forster T, et al. Importance of extracardiac α1-adrenoceptor stimulation in assisting dofetilide to induce torsade de pointes in rabbit hearts. Eur J Pharmacol 2006;537:118-25.
26. Bustos MD, Gay F, Diquet B, Thomare P, Warot D. The pharmacokinetics and electrocardiographic effects of chloroquine in healthy subjects. Trop Med Parasitol 1994;45:83-6.
27. Anigbogu CN, Adigun SA, Inyang I, Adegunloye BJ. Chloroquine reduces blood pressure and forearm vascular resistance and increases forearm blood flow in healthy young adults. Clin Physiol 1993;13:209-16.
28. Ghigo D, Aldieri E, Todde R, Costamagna C, Garbarino G, Pescarmona G, et al. Chloroquine stimulates Nitric Oxide synthesis in murine, porcine, and human endothelial Cells. J Clin Invest 1998;102:595-605.
29. Guedira N, Hajjaj-Hassouni N, Srairi JE, el Hassani S, Fellat R, Benomar M. Third-degree atrioventricular block in a patient under chloroquine therapy. Rev Rhum Engl 1998;65:58-62.
30. Li Q, Himmel HM, Ravens U. Selectivity of class-III antiarrhythmic action of clofilium in guinea pig ventricular myocytes. J Cardiovasc Pharmacol 1996;27:401-10.