Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes

Journal of Pharmacy and Pharmacology

Volumn 51, Issue 9, 1999, Pages 1059-1063

  Ohtani, Hisakazu ^a   Hanada, Erika ^a   Hirota, Michiko ^a   Sato, Hitoshi ^a   Kotaki, Hajime ^b   Sawada, Yasufumi ^c   Uemura, Hiroko ^d   Nakaya, Haruaki ^d   Iga, Tatsuji ^a  

^a UNIVERSITY OF TOKYO HOSPITAL   (Japan)

^b UNIVERSITY OF TOKYO   (Japan)

^c KYUSHU UNIVERSITY   (Japan)

^d CHIBA UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIHISTAMINIC AGENT; EBASTINE; EPINASTINE; POTASSIUM ION; TERFENADINE;

ANIMAL CELL; ARRHYTHMOGENESIS; ARTICLE; HEART MUSCLE CELL; MALE; NONHUMAN; PATCH CLAMP; POTASSIUM CURRENT; QT INTERVAL; RAT;

ANIMALS; BUTYROPHENONES; DIBENZAZEPINES; ELECTROPHYSIOLOGY; HEART VENTRICLES; HISTAMINE H1 ANTAGONISTS; IMIDAZOLES; MALE; PATCH-CLAMP TECHNIQUES; PIPERIDINES; POTASSIUM CHANNELS; RATS; RATS, SPRAGUE-DAWLEY; TERFENADINE;

EID: 0032874010     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357991773393     Document Type: Article

References (23)

1. + currents in isolated adult rat ventricular myocytes. J. Gen. Physiol. 97: 973-1011
2. Arky, R. (1998) Physicians' Desk Reference (PDR). 52nd edn, Medical Economics Company, pp 1238-1241
3. Azuma, J., Yoshida, H., Seto, Y., Fukui, K., Konishi, K., Otani, M., Tarui, S., Nagakura, A., Kohei, H. (1992) Phase I study of WAL801CL. Rinsho-Iyaku 8 (Suppl. 1): 3-24
4. Crumb, W. J., Brown, A. M. (1993) Terfenadine blockade of a potassium current in human atrial myocytes. Circulation 88 (Suppl. I): 1-230
5. Davies, A. J., Harindra, V., McEwan, A., Ghose R. R. (1989) Cardiotoxic effect with convulsions in terfenadine overdose. Br. Med. J. 298: 325
6. Deal, K. R., England, S. K., Tamkun, M. M. (1996) Molecular physiology of cardiac potassium channels. Physiol. Rev. 76: 49-67
7. + channels. J. Cardiovasc. Pharmacol. 30: 42-45
8. Fabiato, A., Fabiato, F. (1979) Calculator programs for computing the composition of solutions containing multiple metal and ligands used for skinned muscle cells. J. Physiol. (Paris) 75: 463-505
9. Garteiz, D. A., Hook, R. H., Walker, B. J., Okerholm, R. A. (1982) Pharmacokinetics and biotransformation studies of terfenadine in man. Arzn. Forsch. 32: 1185-1190
10. Hey, J. A., Del Prado, M., Sherwood, J., Kreutner, W., Egan, R. W. (1996) Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects. Arzn. Forsch. 46: 153-158
11. Kamisako, T., Adachi, Y., Nakagawa, H., Yamamoto, T. (1995) Torsades de pointes associated with terfenadine in a case of liver cirrhosis and hepatocellular carcinoma. Intern. Med. 34: 92-95
12. + channel family by ebastine. J. Pharmacol. Exp. Ther. 281: 233-244
13. Mathews, D. R., McNutt, B., Okerholm, R., Flicker, M., McBride, G. (1991) Torsades de pointes occurring in association with terfenadine use. J. Am. Med. Assoc. 266: 2375-2376
14. Monahan, B. P., Ferguson, C. L., Killeavy, E. S., Lloyd, B. K., Troy, J., Cantilena, L. R. (1991) Torsades de pointes occurring in association with terfenadine use. J. Am. Med. Assoc. 264: 2788-2790
15. Ohtani, H., Kotaki, H., Sawada, Y., Iga, T. (1997) A comparative pharmacokinetic-pharmacodynamic study of the electrocardiographic effects of epinastine and terfenadine in rats. J. Pharm. Pharmacol. 49: 458-462
16. Ohtani, H., Sato, H., Iga, T., Kotaki, H., Sawada, Y. (1999) A pharmacokinetic-pharmacodynamic analysis of the arrhythmogenic potency of a novel antiallergic agent, ebastine, in rats. Biopharm. Drug Dispos. In press
17. + channel cloned from human heart. Mol. Pharmacol. 44: 1240-1245
18. 1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ. Res. 76: 110-119
19. + channel blocking actions of flecainide compared with those of propafenone and quinidine in adult rat ventricular myocytes. J. Pharmacol. Exp. Ther. 269: 66-74
20. Tsien, R. Y., Rink, T. J. (1980) Neutral carrier ion-selective microelectrodes for measurement of intracellular free calcium. Biophys. Acta 599: 623-638
21. Watanabe, Y., Hara, Y., Tamagawa, M., Nakaya, H. (1996) Inhibitory effect of amiodarone on the muscarinic acetylcholine receptor-operated potassium current in guinea pig atrial cells. J. Pharmacol. Exp. Ther. 279: 617-624
22. Woosley, R. L., Chen, Y., Frieman, J. P., Gillis, R. A. (1993) Mechanism of the cardiotoxic actions of terfenadine. J. Am. Med. Assoc. 269: 1532-1536
23. Zehender, M., Hohnloser, S., Just, H. (1991) QT-interval prolonging drugs: mechanisms and clinical relevance of their arrhythmogenic hazards. Cardiovasc. Drugs Ther. 5: 515-530