Molecular basis for the lack of HERG K+ channel block-related cardiotoxicity by the H1 receptor blocker cetirizine compared with other second-generation antihistamines

Molecular Pharmacology

Volumn 54, Issue 1, 1998, Pages 113-121

  Taglialatela, Maurizio ^a   Pannaccione, Anna ^a   Castaldo, Pasqualina ^a   Giorgio, Giovanna ^a   Zhou, Zhengfeng ^b   January, Craig T ^b   Genovese, Arturo ^a   Marone, Gianni ^a   Annunziato, Lucio ^a  

^a UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^b UNIVERSITY OF WISCONSIN MADISON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIHISTAMINIC AGENT; ASTEMIZOLE; CETIRIZINE; LORATADINE; PIPERAZINE DERIVATIVE; POTASSIUM CHANNEL; TERFENADINE;

ANIMAL CELL; ARTICLE; CARDIOTOXICITY; EXTRACELLULAR SPACE; HEART VENTRICLE ARRHYTHMIA; HUMAN; HUMAN CELL; NEUROBLASTOMA; NONHUMAN; PRIORITY JOURNAL; RECEPTOR BINDING; TORSADE DES POINTES; XENOPUS LAEVIS;

EID: 0031867789     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.54.1.113     Document Type: Article

References (39)

1. + current with a cell cycledependence governs the resting potential of neuroblastoma cells. J Physiol (Lond) 489:455-471.
2. Babe KS and Serafin WE (1996) Goodman and Gilman's The Pharmacological Basis of Therapeutics (Hardman JG, Goodman Gilman A, and Limbird LE, eds) pp. 581-600, IX ed., McGraw-Hill, New York.
3. Berul CI and Morad M (1995) Regulation of potassium channels by nonsedating antihistamines. Circulation 91:2220-2225.
4. + current highly conserved in tumors of different histogenesis: a selective advantage for cancer cells? Cancer Res 58:815-822
5. Brannan MD, Reidenberg P, Radwanski E, Shneyer L, Lin CC, Cayen MN, Affrime MB (1995) Loratadine administered concomitantly with erythromycin: pharmacokinetic and electrocardiographic evaluations. Clin Pharmacol Ther 58:269-278.
6. Craft TM (1986) Torsade de pointes after astemizole overdose. Br Med J 292:660.
7. Crumb WJ, Wible BA, Arnold DJ, Payne JP, and Brown AM (1995) Blockade of multiple human cardiac potassium channels by the antihistamine terfenadine: possible mechanisms for terfenadine-associated cardiotoxicity. Mol Pharmacol 47:181-190.
8. Curran ME, Splawski I, Timothy KW, Vincent GM, Green ED, and Keating MT (1995) A molecular basis for cardiac arrhythmia: HERG mutations cause the long QT syndrome. Cell 80:795-803.
9. Davies AJ, Harinda V, McHewan A, and Ghose RR (1989) Cardiotoxic effect with convulsions in terfenadine overdose. Br Med J 302:1469.
10. Good AP, Rockwood R, and Schad P (1994) Loratadine and ventricular tachycardia. Am J Cardiol 74:1240-1245.
11. Hamill OP, Marty E, Neher E, Sakmann B, and Sigworth FJ (1981) Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflueg Arch Eur J Physiol 391:85-100.
12. Haria M, Fitton A, and Peters DH (1994) Loratadine: a reappraisal of its pharmacodynamic properties and therapeutic use in allergic disorders. Drugs 48:617-638.
13. Hey JA, del Prado M, Egan RW, Sherwood J, and Kreutner W (1995) Loratadine produces antihistamine activity without adverse CNS, ECG or cardiovascular effects in guinea pigs: comparative studies with terfenadine and sedating antihistamines. Int Arch Allergy Immunol 107:418-419.
14. Hey JA, del Prado M, Sherwood J, Kreutner W, and Egan RW (1996) Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects. Arznemittel-Forschung Drug Res 46:153-156.
15. Hoppu K, Tikanoja T, Tapanainen P, Remes M, Saarenpaa-Heikkila O, and Kopuvalainen K (1991) Accidental astemizole overdose in young children. Lancet 338:538-540.
16. Jackman WM, Friday KJ, Anderson JL, Aliot EM, Clark M, and Lazzara R (1988) The long QT syndrome: a critical review, new clinical observations and a unifying hypothesis. Prog Cardiovasc Dis 31:115-172.
17. Kiehn J, Lacerda A, Wible BA, and Brown AM (1996) Molecular physiology and pharmacology of HERG: single channel currents and block by dofetilide. Circulation 94:2575-2579.
18. + channel family by ebastine. J Pharmacol Exp Ther 281:233-244.
19. Lacerda AE, Roy M-L, Lewis EW, and Rampe D (1997) Interaction of the nonsedating antihistamine loratadine with a Kv1.5 type potassium channel cloned from human heart. Mol Pharmacol 52:314-322.
20. Lindquist M and Edwards IR (1997) Risk of non-sedating antihistamines. Lancet 349:1322.
21. + current. Circ Res 81:870-878.
22. Monahan BP, Ferguson CL, Killeavy ES, Lloyd BK, Troy J, and Cantilena LR (1990) Torsade de pointes occurring in association with terfenadine use. JAMA 264:2788-2790.
23. + channel cloned from human heart. J Pharmacol Exp Ther 44:1240-1245.
24. Roy M-L, Dumaíne R, and Brown AM (1996) HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine. Circulation 94:817-823.
25. 1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ Res 76:110-119
26. Sale ME, Barbery JT, Woosley RL, Edwards D, Yeh J, Thakker K, and Chung M (1994) The electrocardiographic effects of cetirizine in normal subjects. Clin Pharmacol Ther 56:295-301.
27. Kr potassium channel. Cell 81:299-307.
28. Singh BN (1993) Arrhythmia control by prolonging repolarization: the concept and its potential therapeutic impact. Eur Heart J 14 (Suppl. H):14-23.
29. + channel: open channel block by methanesulfonanilides. Circ Res 78:499-503.
30. Sorkin EM and Heel RC (1985) Terfenadine: a review of its pharmacodynamic properties and therapeutic efficacy. Drugs 29:34-56.
31. Suessbrich H, Waldegger S, Lang F, and Busch AE (1996) Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole. FEBS Lett 385:77-80.
32. Trudeau MC, Warmke JW, Ganetzky B, and Robertson GA (1995) HERG, a human inward rectifier in the voltage-gated potassium channel family. Science (Washington DC) 269:92-95.
33. Warmke JW and Ganetzky B (1994) A family of potassium channel genes related to eag in Drosofila and mammals. Proc Natl Acad Sci USA 91:3438-3442.
34. Woosley RL (1996) Cardiac actions of antihistamines. Annu Rev Pharmacol Toxicol 36:233-252.
35. Woosley RL and Darrow WR (1994) Analysis of potential adverse drug reactions: a case of mistaken identity. Am J Cardiol 74:208-209.
36. + channel, erg. Circ Res 80:261-268.
37. Yun C, Okerholm RA, and Guengerich FP (1993) Oxidation of the antihistaminic drug terfenadine in human liver microsomes: role of cytochrome P4503A4 in N-dealkylation and C-hydroxylation. Drug Metab Dispos 21:403-409.
38. Zhang M-Q (1997) Chemistry underlying the cardiotoxicity of antihistamines. Curr Med Chem 4:187-200.
39. Zhou Z, Gong Q, Ye B, Fan Z, Makielski JC, Robertson GA, and January CT (1998) Properties of HERG channels stably expressed in HEK 293 cells studied at physiological temperature. Biophys J 74:230-241.