Cardiac actions of antihistamines

Annual Review of Pharmacology and Toxicology

Volumn 36, Issue , 1996, Pages 233-252

  Woosley, Raymond L ^a  

^a GEORGETOWN UNIVERSITY MEDICAL CENTER   (United States)

Author keywords

arrhythmia; astemizole; potassium channels; terfenadine

Indexed keywords

ANTIARRHYTHMIC AGENT; ANTIHISTAMINIC AGENT; ASTEMIZOLE; AZATADINE; CETIRIZINE; CHLORCYCLIZINE; CHLORPHENIRAMINE; CHLORPHENIRAMINE MALEATE; CLEMASTINE; CYPROHEPTADINE; DIPHENHYDRAMINE; HYDROXYZINE; HYDROXYZINE EMBONATE; LORATADINE; MEPYRAMINE; PHENINDAMINE; POTASSIUM CHANNEL; QUINIDINE; TERFENADINE; TRIPELENNAMINE; TRIPROLIDINE;

CARDIOTOXICITY; HEART VENTRICLE TACHYCARDIA; HUMAN; PRIORITY JOURNAL; QT INTERVAL; REPOLARIZATION; REVIEW; TORSADE DES POINTES;

EID: 0030011760     PISSN: 00664251     EISSN: None     Source Type: Book Series    
DOI: 10.1146/annurev.pharmtox.36.1.233     Document Type: Review

References (73)

1. Simonsen L. 1991. What are pharmacists dispensing most often? Pharm. Times April:57-70
2. IMS America Ltd. 1992. 1991 National Prescription Audit. IMS America Ltd, Plymouth Meeting, PA
3. Craft TM. 1986. Torsade de pointes after astemizole overdose. Br. Med. J. 292:660
4. Snook J, Coothman-Burrell D, Watkins J, Colin-Jones D. 1988. Torsade de pointes ventricular tachycardia associated with astemizole overdose. Br. J. Clin. Pract. 42:257-59
5. Wiley JF, Gelber ML, Henretig FM, Wiley CC, Sandhu S, Loiselle J. 1992. Cardiotoxic effects of astemizole overdose in children. J. Pediatr. 120:799-802
6. Hoppu K, Tikanoja T, Tapanainen P, Remes M, Saarenpaa-Heikkila O, Kouvalainen K. 1991. Accidental astemizole overdose in young children. Lancet 338: 538-40
7. Davies AJ, Harindra V, McEwan A, Ghose RR. 1989. Cardiotoxic effect with convulsions in terfenadine overdose. Br. Med. J. 298:325
8. MacConnell TJ, Stanners AJ. 1991. Torsades de pointes complicating treatment with terfenadine. Br. Med. J. 302:1469
9. Monahan BP, Ferguson CL, Killeavy ES, Lloyd BK, Troy J, Cantilena LR. 1990 Torsades de pointes occurring in association with terfenadine use. JAMA 264:2788-90
10. Douglas WW. 1970. Histamines and antihistamines. In Pharmacologic Basis of Therapeutics, ed. L Goodman, A Gilman, pp. 621-62. New York: Macmillan
11. Landau SW, Nelson WA, Gay LN. 1948. Antihistaminic properties of local anesthetics and anesthetic properties of antihistaminic compounds. J. Allergy 20: 19-30
12. Meyer RA, Jakubowski W. 1964. Use of tripelennamine and diphenhydramine as local anesthetics. J. Am. Dent Assoc. 69:112-17
13. Singh KP, Pendse VK, Bhandari DS. 1975. Cyproheptadine in ventricular arrhythmias. Indian Heart J. 27:120-26
14. Abaza A, Delattre G, Germain G. 1967. Treatment of cardiac arrhythmia by a tranquilizing antihistamine. Coeur Med. Interne 6(3):373-78
15. Jackman WM, Friday KJ, Anderson JL, Aliot EM, Clark M, Lazzara R. 1988. The long QT syndromes: a critical review, new clinical observations and a unifying hypothesis. Prog. Cardiovasc. Dis. 31:115-72
16. Roden D, Woosley R, Primm R. 1986. Incidence and clinical features of the quinidine-associated long-QT syndrome, implications for patient care. Am. Heart J. 111(6): 1088-93
17. Carlsson L, Almgren O, Duker G. 1990. QTU-prolongation and torsade de pointes induced by putative class III antiarrhythmic agents in the rabbit: etiology and interventions. J. Cardiovasc. Pharmacol. 16:276-85
18. Takahashi N, Ito M, Ishida S, Fujino T, Saikawa T, Arita M. 1992. Effects of vagal stimulation on cesium-induced early afterdepolarizations and ventricular arrhythmias in rabbits. Circulation 86:1987-92
19. Thompson KA, Murray JJ, Blair IA, Woosley RL, Roden DM. 1988. Plasma concentrations of quinidine, major metabolites, and dihydroquinidine in patients with torsades de pointes. Clin. Pharmacol. Ther. 43:636-42
20. Thompson KA, Blair IA, Woosley RL, Roden DM. 1987. Comparative in vitro electrophysiology of quinidine, its major metabolites and dihydroxyquinidine. J. Pharmacol. Exp. Ther. 241:84-90
21. Colatsky TJ, Follmer CH, Starmer CF. 1990. Channel specificity in antiarrhythmic drug action: mechanism of potassium channel block, and its role in suppressing and aggravating cardiac arrhythmias. Circulation 82(6):2235-42
22. El-Sherif N, Bekheit SS, Henkin R. 1989. Quinidine-induced long QTU interval and torsade de pointes: role of bradycardia-dependent early afterdepolarizations. J. Am. Coll. Cardiol. 14: 252-57
23. Antzelevitch C, Sicouri S. 1994. Clinical relevance of cardiac arrhythmias generated by afterdepolarizations: role of M cells in the generation of U waves, triggered activity and torsades de pointes. J. Am. Coll. Cardiol. 23: 259-77
24. Zehender M, Hohnloser SH, Just H. 1991. QT-interval prolonging drugs: mechanisms and clinical relevance of their arrhythmogenic hazards. Cardiovasc. Drugs Ther. 5:515-30
25. Surawicz B. 1992. Bradycardia-dependent long QT syndrome, sudden death and late potentials. Am. J. Cardiol. 19 (3):550-51
26. Jackman WM, Szabo B, Friday KJ, Margolis PD, Moulton K, et al. 1990. Ventricular tachyarrhythmias related to early afterdepolarizations and triggered firing: relationship to QT interval prolongation and potential therapeutic role for calcium channel blocking agents. J. Cardiovasc. Pharmacol 1(2):170-95
27. Napolitano C, Priori SG, Schwartz PJ. 1994. Torsade de pointes: mechanisms and management. Drugs 47:51-65
28. Berul CI, Morad M. 1995. Regulation of potassium channels by non-sedating antihistamines. Circulation 91: 2220-25
29. Salata JJ, Jurkiewicz NK, Wallace AA, Stupienski RF 3rd, Guinosso PJ Jr, Lynch JJ Jr. 1995. Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ. Res. 76: 110-19
30. K1 blockade is a potentially useful antiarrhythmic mechanism. Cardiovasc. Res. 28:421
31. Botstein P. 1993. Is QT interval prolongation harmful? A regulatory perspective. Am. J. Cardiol. 72:50B-52B
32. Woosley RL, Chen Y, Freiman JP, Gillis RA, 1993. Mechanism of the cardiotoxic actions of terfenadine. JAMA 269(12): 1532-36
33. Crumb WJ Jr, Wible B, Arnold DJ, Payne JP, Brown AM. 1993. Blockade of multiple human cardiac potassium currents by the antihistamine terfenadine: possible mechanism for terfenadine-associated cardiotoxicity. Mol. Pharmacol. 47:181-90
34. + channel cloned from human heart. Mol. Pharmacol. 44:1240-45
35. Good AP, Rockwood R, Schad P. 1994. Loratadine and ventricular tachycardia. Am. J. Cardiol. 74:207-9
36. Sale ME, Barbey JT, Woosley RL, Edwards D, Yeh J, et al. 1994. The electrocardiographic effects of cetirizine in normal subjects. Clin. Pharmacol. Ther. 56:295-301
37. Brannan M, Reidenberg P, Radwanski E, Shneyer L, Lin C, et al. 1995. Loratadine administered concomilantly with erythromycin: pharmacokinetic and electrocardiographic evaluations. Clin. Pharmacol. Ther. 58(3):269-78
38. Hey J, del Prado M, Egan RW, Sherwood J, 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. 107:418-19
39. Nightingale SL. 1992. Warnings issued on nonsedating antihistamines terfenadine and astemizole. JAMA 268(6): 705
40. Yun C, Okerholm RA, Guengerich FP. 1993. Oxidation of the antihistaminic drug terfenadine in human liver microsomes Role of cytochrome P450 3A4 in N-dealkylation and C-hydroxylation. Drug Metab. Dispos. 21(3):403-9
41. Coutant JE, Westmark PA, Nardella PA, Walter SM, Okerholm RA. 1991. Determination of terfenadine and terfenadine acid metabolite in plasma using solid-phase extraction and high-performance liquid chromatography with fluorescence detection. J. Chromatogr. 570:139-48
42. 1992. Seldane. In Physician's Desk Reference, pp. 1349-50. Montvale, NJ: Med. Econ. Data
43. Garteiz DA, Hook RH, Walker BJ, Okerholm RA. 1982. Pharmacokinetics and biotransformation studies of terfenadine in man. Arzneim. Forschung 32(II): 1185-90
44. Lang DG, Wang CM, Wenger TL. 1993. Terfenadine alters action potentials in isolated canine purkinje fibers more than acrivastine. J. Cardiovasc. Pharmacol. 22:438-42
45. Pinney SP, Koller BS, Franz MR, Woosley RL. 1995. Terfenadine increases the QT interval in isolated guinea pig heart. J. Cardiovasc. Pharmacol. 25(1):30-34
46. Woosley RL, Chen Y. 1994. Synergistic effects of ketoconazole and terfenadine on cardiac repolarizalion. Clin. Res. 42 (2):329A (Abstr.)
47. Carmeliet E. 1995. Block of the delayed K current in cardiac cells by antihistamines: a comparison of cetirizine and terfenadine. Circ. Res. In press
48. + current. J. Gen. Physiol. 96: 195-215
49. Honig PK, Woosley RL, Zamani K, Conner DP, Cantilena LR. 1992. Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine with concomitant administration of erythromycin. Clin. Pharmacol. Ther. 52(3):231-38
50. Larrey D, Funck-Brentano C, Breil P, Vitaux J, Theodore C, et al. 1982. Effects of erythromycin on hepatic drug-metabolizing enzymes in humans. Biochem. Pharmacol. 32:1063-68
51. Honig PK, Wortham DC, Zamani K, Conner DP, Mullin JC, Cantilena LR. 1993. Terfenadine-ketoconazole interaction, pharmacokinetic and electrocardiographic consequences. JAMA 269: 1513-18
52. Honig PK, Wortham DC, Hull R, Zamani K, Smith JE, Cantilena LR. 1993. Itraconazole affects single-dose terfenadine pharmacokinetics and cardiac repolarization pharmacodynamics. J. Clin. Pharmacol. 33:1201-6
53. Honig PK, Wortham DC, Zamani K, Conner DP, Mullin JC, Cantilena LR. 1993. Effect of concomitant administration of cimetidine and ranitidine on the pharmacokinetics and electrocardiographic effects of terfenadine. Eur. J. Clin. Pharmacol. 45:41-46
54. Honig PK, Wortham DC, Zamani K, Mulin JC, Conner DP, Cantilena LR. 1993. The effect of fluconazole on the steady-state pharmacokinetics and electrocardiographic pharmacodymanics of terfenadine in humans. Clin. Pharmacol. Ther. 53(6):630-36
55. Cantilena L, Sorrels S, Wiley T, Wortham D. 1995. Fluconazole alters terfenadine pharmacokinetics and electrocardiographic pharmacodynamics. Clin. Pharmacol. Ther. 57:(2)185 (Abstr.)
56. Simons FE, Simons KJ, Chung M, Yeh J. 1987. The comparative pharmacokinetics of H1-receptor antagonists. Ann. Allergy 59:20-24
57. Pratt CM, Hertz RP, Ellis BE, Crowell SP, Louv W, Moye L. 1994. Risk of developing life-threatening ventricular arrhythmia associated with terfenadine in comparison with over-the-counter anuhistamines, ibuprofen and clemastine. Am. J. Cardiol. 73:346-52
58. Zechnich AD, Hedges JR, Eiselt-Proteau D, Haxby D. 1994. Possible interactions with terfenadine or astemizole. West. J. Med. 160:321-25
59. Cavuto J, Woosley R, Sale M. 1995. Effectiveness of community pharmacies in detection of prescription errors. JAMA. In press
60. Benton R, Honig P, Zamani K, Hewett J, Cantilena LR, et al. 1995. Grapefruit juice alters terfenadine pharmacokinetics resulting in prolongation of QTc. Clin. Pharamacol. Ther. In press
61. Chen Y, Woosley RL. 1994. Electrophysiologic actions of astemizole. Clin. Pharmacol. Ther. 55:(2)146 (Abstr.)
62. Brewer N, Cruise L. 1995. The guinea pig heart - some comparative aspects. Contemp. Top. 33(6):64-67
63. Woosley RL, Darrow WR. 1994. Analysis of potential adverse drug reactions-a case of mistaken identity. Am. J. Cardiol. 74(2):208-9
64. 1994. Diphenhydramine. In Physician's Desk Reference, pp. 1719-20. Montvale, NJ: Med. Econ. Data
65. Burkhart GA, Freiman J. 1995. The risk of life-threatening cardiovascular events with terfenadine. Am. J. Cardiol 75: 213-14
66. Simons KJ, Watson WT, Martin TJ, Chen XY, Simons FE. 1990. Diphenhydramine: pharmacokinetics and pharmacodynamics in elderly adults, young adults, and children. J. Clin. Pharmacol. 30:665-71
67. Hollister LE. 1975. Hydroxyzine hydrochloride: possible adverse cardiac interactions. Psychopharmacol. Commun. 1: 61-65
68. Burton BT, Rice M, Schmertzler LE. 1985. Atrioventricular block following overdose of decongestant cold medication. J. Emerg. Med. 2:415-19
69. Deleted in proof
70. ++ entry into GH3 and chromaffin cells by imidazole antimycotics and other cytochrome P450 blockers. FASEB J. 6:2742-47
71. Chen Y, Woosley RL. 1993. Ketoconazole blocks potassium currents in feline heart. Circulation 88:1-38 (Abstr.)
72. Paserchia LA, Hewett J, Woosley RL. 1994. Effects of ketoconazole on QTc. Clin. Pharmacol. Ther. 55(2):146
73. Carlsson L, Abrahamsson C, Drews L, Duker G. 1992. Antiarrhythmic effects of potassium channel openers in rhythm abnormalities related to delayed repolarization. Circulation 85:1491-500