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Drugs. 1993 Jan;45(1):85-130. doi: 10.2165/00003495-199345010-00008.

Propafenone. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in cardiac arrhythmias.

Drugs

H M Bryson, K J Palmer, H D Langtry, A Fitton

Affiliations

  1. Adis International Limited, Auckland, New Zealand.

PMID: 7680987 DOI: 10.2165/00003495-199345010-00008

Abstract

Propafenone is an orally active sodium channel blocking agent with beta-adrenoceptor antagonist and weak calcium antagonist activity. The pharmacokinetic profile of propafenone is complex, characterised as typically nonlinear, saturable, stereoselective and dependent on both dose and debrisoquin metaboliser phenotype; individualised dosage titration is required. Both placebo- and drug-controlled studies have confirmed the efficacy of propafenone in the treatment of premature ventricular complexes, ventricular couplets and nonsustained ventricular tachycardia; in a large meta-analysis, propafenone together with amiodarone, flecainide and encainide were significantly more effective in the control of ventricular ectopy than other antiarrhythmic agents. However, the use of propafenone in these indications, like that of other antiarrhythmic agents, is likely to be limited to patients with a favourable risk-to-benefit ratio. Propafenone has also demonstrated efficacy in the treatment of malignant ventricular arrhythmias (ventricular fibrillation and sustained ventricular tachycardia); preliminary mortality data obtained with propafenone have been encouraging in this patient group. In addition, propafenone has a favourable noncardiac tolerability profile and beta-adrenoceptor antagonist activity, which may offer advantages in some specific patient groups. The area of research concerning propafenone which has shown the greatest expansion over the past 5 years is in the treatment of supraventricular arrhythmias. Propafenone has marked efficacy in patients with Wolff-Parkinson-White syndrome and has been recommended as a first-line prophylactic agent in those with rapid anterograde conduction. Propafenone is also effective in the conversion of atrial fibrillation to sinus rhythm, although comparative studies are required to determine advantages over more established agents. Propafenone use has been successfully extended to children with limited data demonstrating consistent efficacy in the control of junctional ectopic tachycardia. As with all antiarrhythmic agents, propafenone has the potential to induce arrhythmias. Comparative studies are required to assess in more detail the cardiac tolerability profile of propafenone against other class Ic agents. In conclusion, propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias, although its use in patients with potentially malignant arrhythmias will remain limited for the present. Due to its unique pharmacodynamic profile, propafenone deserves consideration as an individual agent.

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References

  1. J Emerg Med. 1990 Jan-Feb;8(1):15-20 - PubMed
  2. Chest. 1990 Aug;98(2):434-41 - PubMed
  3. J Cardiovasc Pharmacol. 1989 Oct;14 (4):577-84 - PubMed
  4. Am J Cardiol. 1992 Oct 15;70(11):1028-34 - PubMed
  5. JAMA. 1984 Aug 3;252(5):673-6 - PubMed
  6. Am J Cardiol. 1984 Nov 14;54(9):60D-66D - PubMed
  7. Am Heart J. 1985 Jul;110(1 Pt 1):24-9 - PubMed
  8. Eur J Clin Pharmacol. 1978 Mar 17;13(1):17-20 - PubMed
  9. Int J Cardiol. 1991 May;31(2):187-97 - PubMed
  10. Methods Find Exp Clin Pharmacol. 1988 Nov;10(11):717-27 - PubMed
  11. Am Heart J. 1991 Oct;122(4 Pt 1):1022-7 - PubMed
  12. Br J Clin Pharmacol. 1991 Oct;32(4):527-8 - PubMed
  13. J Clin Pharmacol. 1988 Jul;28(7):619-24 - PubMed
  14. Arzneimittelforschung. 1992 Mar;42(3):289-91 - PubMed
  15. Eur J Clin Pharmacol. 1992;42(1):111-4 - PubMed
  16. Can J Cardiol. 1991 May;7(4):175-80 - PubMed
  17. Monatsschr Kinderheilkd. 1983 Nov;131(11):779-83 - PubMed
  18. Angiology. 1989 Jun;40(6):563-8 - PubMed
  19. Ann Intern Med. 1991 Apr 1;114(7):539-44 - PubMed
  20. J Pharmacol Exp Ther. 1984 Feb;228(2):461-6 - PubMed
  21. J Am Coll Cardiol. 1989 Nov 1;14(5):1326-30 - PubMed
  22. Clin Pharmacol Ther. 1984 Aug;36(2):163-8 - PubMed
  23. N Engl J Med. 1989 Aug 10;321(6):406-12 - PubMed
  24. Dtsch Med Wochenschr. 1985 Jul 12;110(28-29):1103-7 - PubMed
  25. Am Heart J. 1985 Apr;109(4):833-40 - PubMed
  26. J Chromatogr. 1985 Jun 14;341(2):305-11 - PubMed
  27. Br J Pharmacol. 1991 Mar;102(3):669-74 - PubMed
  28. Am J Cardiol. 1989 Apr 1;63(12):817-9 - PubMed
  29. Circulation. 1988 Oct;78(4):863-9 - PubMed
  30. J Cardiovasc Pharmacol. 1981 Nov-Dec;3(6):1162-73 - PubMed
  31. Circulation. 1978 Sep;58(3 Pt 1):408-14 - PubMed
  32. Rev Port Cardiol. 1990 Jan;9(1):33-9 - PubMed
  33. Am J Cardiol. 1990 Jun 1;65(20):1328-33 - PubMed
  34. Am J Cardiol. 1990 Aug 1;66(3):366-7 - PubMed
  35. Annu Rev Pharmacol Toxicol. 1991;31:427-55 - PubMed
  36. Am Heart J. 1988 Dec;116(6 Pt 1):1542-51 - PubMed
  37. Cardiovasc Drugs Ther. 1990 Feb;4(1):281-7 - PubMed
  38. Therapie. 1989 Mar-Apr;44(2):79-85 - PubMed
  39. J Chromatogr. 1987 Jul 3;417(2):295-308 - PubMed
  40. Eur Heart J. 1992 Feb;13(2):269-74 - PubMed
  41. Am J Cardiol. 1984 Nov 14;54(9):45D-50D - PubMed
  42. Eur J Pharmacol. 1985 Dec 3;118(3):331-40 - PubMed
  43. J Am Coll Cardiol. 1989 Jul;14(1):219-24 - PubMed
  44. Circulation. 1987 Apr;75(4):785-91 - PubMed
  45. J Cardiovasc Pharmacol. 1987 Nov;10 (5):523-9 - PubMed
  46. Pacing Clin Electrophysiol. 1984 Jul;7(4):649-55 - PubMed
  47. Am Heart J. 1989 Feb;117(2):370-6 - PubMed
  48. J Cardiovasc Pharmacol. 1991 Dec;18(6):911-7 - PubMed
  49. Am J Cardiol. 1990 Jan 1;65(1):40-8 - PubMed
  50. J Am Coll Cardiol. 1987 Jun;9(6):1364-8 - PubMed
  51. Am J Cardiol. 1988 Sep 1;62(7):480-1 - PubMed
  52. Br J Clin Pharmacol. 1988 Oct;26(4):489-90 - PubMed
  53. J Clin Pharmacol. 1991 Feb;31(2):123-35 - PubMed
  54. Int J Cardiol. 1986 Nov;13(2):163-70 - PubMed
  55. Am Heart J. 1989 Feb;117(2):497-8 - PubMed
  56. J Chromatogr. 1990 Apr 27;527(1):79-89 - PubMed
  57. Eur Heart J. 1987 Mar;8 Suppl A:27-32 - PubMed
  58. J Neurol Neurosurg Psychiatry. 1991 Apr;54(4):377 - PubMed
  59. J Clin Psychiatry. 1991 Oct;52(10):432-3 - PubMed
  60. Br J Clin Pharmacol. 1987 Jun;23(6):735-41 - PubMed
  61. N Engl J Med. 1992 May 7;326(19):1264-71 - PubMed
  62. Am J Cardiol. 1988 Apr 15;61(11):914-6 - PubMed
  63. Acta Clin Belg. 1988;43(2):143-5 - PubMed
  64. G Ital Cardiol. 1987 Jul;17(7):605-8 - PubMed
  65. Am J Cardiol. 1990 Jun 15;65(22):1497-503 - PubMed
  66. J Am Coll Cardiol. 1992 May;19(6):1368-9 - PubMed
  67. G Ital Cardiol. 1987 Mar;17(3):233-8 - PubMed
  68. G Ital Cardiol. 1986 Oct;16(10):855-62 - PubMed
  69. Circ Res. 1987 Oct;61(4):492-7 - PubMed
  70. Br J Pharmacol. 1988 Dec;95(4):1039-46 - PubMed
  71. J Cardiovasc Pharmacol. 1990 Jan;15(1):75-81 - PubMed
  72. J Am Coll Cardiol. 1984 May;3(5):1291-7 - PubMed
  73. Eur Heart J. 1984 Feb;5(2):115-25 - PubMed
  74. J Clin Pharmacol. 1989 Feb;29(2):112-3 - PubMed
  75. J Am Coll Cardiol. 1991 Mar 1;17(3):604-12 - PubMed
  76. Am J Cardiol. 1990 Feb 15;65(7):458-62 - PubMed
  77. Circulation. 1987 Jul;76(1):1-5 - PubMed
  78. Eur J Clin Pharmacol. 1986;30(6):665-71 - PubMed
  79. Am Heart J. 1986 Jul;112(1):14-9 - PubMed
  80. Int J Cardiol. 1990 Apr;27(1):63-70 - PubMed
  81. J Cardiovasc Pharmacol. 1992 Apr;19(4):493-502 - PubMed
  82. Clin Pharmacol Ther. 1987 Sep;42(3):305-11 - PubMed
  83. J Clin Pharmacol. 1989 Jan;29(1):46-52 - PubMed
  84. Am J Cardiol. 1989 Jan 1;63(1):114-6 - PubMed
  85. Ann Intern Med. 1986 Apr;104(4):589 - PubMed
  86. Eur Heart J. 1980 Aug;1(4):309-13 - PubMed
  87. Am J Cardiol. 1990 Sep 15;66(7):755-7 - PubMed
  88. Br J Clin Pharmacol. 1989 Apr;27(4):435-44 - PubMed
  89. Br J Pharmacol. 1991 Jun;103(2):1453-7 - PubMed
  90. Clin Pharmacol Ther. 1990 Sep;48(3):245-54 - PubMed
  91. Z Kardiol. 1986 Dec;75(12):764-9 - PubMed
  92. N Engl J Med. 1991 Mar 21;324(12):781-8 - PubMed
  93. Cardiologia. 1989 Jan;34(1):83-5 - PubMed
  94. Am J Cardiol. 1984 Aug 1;54(3):424-9 - PubMed
  95. Am J Cardiol. 1988 Feb 15;61(6):473-4 - PubMed
  96. Lancet. 1990 Apr 21;335(8695):979 - PubMed
  97. J Pharm Sci. 1987 Jun;76(6):437-40 - PubMed
  98. Clin Pharmacol Ther. 1992 Mar;51(3):353-5 - PubMed
  99. Am J Cardiol. 1988 May 1;61(13):1127-30 - PubMed
  100. Am J Cardiol. 1983 Sep 22;52(6):47C-54C - PubMed
  101. Eur Heart J. 1992 Apr;13(4):517-25 - PubMed
  102. Am Heart J. 1987 Sep;114(3):551-8 - PubMed
  103. Am J Cardiol. 1990 Jan 16;65(4):36B-42B - PubMed
  104. J Am Coll Cardiol. 1987 Jun;9(6):1357-63 - PubMed
  105. Pediatr Res. 1987 Jul;22(1):50-4 - PubMed
  106. Lancet. 1989 Dec 23-30;2(8678-8679):1490-1 - PubMed
  107. Ann Cardiol Angeiol (Paris). 1992 Apr;41(4):225-34 - PubMed
  108. J Pharmacol Exp Ther. 1993 Mar;264(3):1113-23 - PubMed
  109. J Cardiovasc Pharmacol. 1992 Aug;20(2):324-31 - PubMed
  110. Am J Cardiol. 1987 Aug 31;60(6):21D-26D - PubMed
  111. Circulation. 1989 Jun;79(6):1354-60 - PubMed
  112. Arch Mal Coeur Vaiss. 1987 Aug;80(9):1385-93 - PubMed
  113. J Am Coll Cardiol. 1990 Nov;16(6):1408-14 - PubMed
  114. Am J Cardiol. 1989 Aug 1;64(5):335-8 - PubMed
  115. Arch Pharm (Weinheim). 1991 Jan;324(1):39-44 - PubMed
  116. Am J Med Sci. 1992 Feb;303(2):123-8 - PubMed
  117. Acta Cardiol. 1990;45(5):359-63 - PubMed
  118. Circulation. 1983 Sep;68(3):589-96 - PubMed
  119. J Cardiovasc Pharmacol. 1990 Jun;15(6):998-1009 - PubMed
  120. Am Heart J. 1987 Aug;114(2):397-406 - PubMed
  121. Arch Toxicol. 1990;64(3):218-30 - PubMed
  122. Methods Find Exp Clin Pharmacol. 1985 Aug;7(8):435-8 - PubMed
  123. Am Heart J. 1986 May;111(5):852-60 - PubMed
  124. J Am Coll Cardiol. 1990 Dec;16(7):1722-7 - PubMed
  125. Biopharm Drug Dispos. 1991 May;12(4):299-310 - PubMed
  126. Am Heart J. 1985 Oct;110(4):794-9 - PubMed
  127. Am Heart J. 1988 Jan;115(1 Pt 1):92-6 - PubMed
  128. Eur Heart J. 1985 Feb;6(2):123-9 - PubMed
  129. Eur J Nucl Med. 1988;13(11):568-71 - PubMed
  130. J Chromatogr. 1991 Nov 1;585(2):329-32 - PubMed
  131. Am Heart J. 1984 Aug;108(2):285-9 - PubMed
  132. J Clin Pharmacol. 1989 Jun;29(6):512-7 - PubMed
  133. J Clin Pharmacol. 1987 May-Jun;27(5):384-9 - PubMed
  134. G Ital Cardiol. 1992 Mar;22(3):257-65 - PubMed
  135. Eur Heart J. 1991 Apr;12 (4):526-32 - PubMed
  136. Klin Wochenschr. 1990 Sep 3;68(17):872 - PubMed
  137. Am Heart J. 1991 Nov;122(5):1355-60 - PubMed
  138. Am J Cardiol. 1989 Sep 15;64(10):671-4 - PubMed
  139. Clin Pharmacokinet. 1991 Jul;21(1):1-10 - PubMed
  140. N Engl J Med. 1990 Feb 22;322(8):518-25 - PubMed
  141. Am J Cardiol. 1991 Sep 15;68(8):741-4 - PubMed
  142. Am Heart J. 1991 Apr;121(4 Pt 1):1178-84 - PubMed
  143. Naunyn Schmiedebergs Arch Pharmacol. 1980;315(1):55-62 - PubMed
  144. J Cardiovasc Pharmacol. 1989 Sep;14(3):444-53 - PubMed
  145. Methods Find Exp Clin Pharmacol. 1988 May;10 (5):319-29 - PubMed
  146. G Ital Cardiol. 1987 Nov;17(11):975-82 - PubMed
  147. J Am Coll Cardiol. 1991 Oct;18(4):1098-104 - PubMed
  148. Br J Pharmacol. 1991 Dec;104(4):853-8 - PubMed
  149. Ther Drug Monit. 1989;11(1):10-5 - PubMed
  150. Clin Pharmacol Ther. 1989 May;45(5):535-41 - PubMed
  151. Am Heart J. 1987 Apr;113(4):941-52 - PubMed
  152. Am Heart J. 1992 May;123(5):1225-8 - PubMed
  153. J Perinat Med. 1988;16(1):39-44 - PubMed
  154. Br J Clin Pharmacol. 1987 Aug;24(2):213-20 - PubMed
  155. J Am Coll Cardiol. 1988 Oct;12(4):1005-11 - PubMed
  156. Clin Pharm. 1991 Mar;10(3):195-205 - PubMed
  157. J Pediatr. 1990 Feb;116(2):310-2 - PubMed
  158. Pflugers Arch. 1983 Mar 1;396(3):199-209 - PubMed
  159. Herz. 1985 Feb;10(1):44-52 - PubMed
  160. Drug Metab Dispos. 1990 Nov-Dec;18(6):987-91 - PubMed
  161. J Pharmacol Exp Ther. 1991 Aug;258(2):722-7 - PubMed
  162. Pharmacotherapy. 1989;9(5):331-3 - PubMed
  163. J Clin Pharmacol. 1991 Jun;31(6):521-6 - PubMed
  164. Eur Heart J. 1987 Aug;8 Suppl D:95-8 - PubMed
  165. Am J Cardiol. 1991 Sep 1;68(6):681-4 - PubMed
  166. Eur J Clin Pharmacol. 1989;36(5):495-9 - PubMed
  167. Am J Cardiol. 1984 Nov 14;54(9):29D-39D - PubMed
  168. Am Heart J. 1990 Aug;120(2):340-53 - PubMed
  169. Drugs. 1992 Feb;43(2):185-200 - PubMed
  170. Br J Clin Pharmacol. 1990 Jul;30(1):155-6 - PubMed
  171. Chest. 1986 Nov;90(5):698-702 - PubMed
  172. Am J Cardiol. 1986 Jan 1;57(1):96-101 - PubMed
  173. Arzneimittelforschung. 1991 Feb;41(2):119-24 - PubMed
  174. Drugs. 1987 Dec;34(6):617-47 - PubMed
  175. J Cardiovasc Pharmacol. 1992 Mar;19(3):341-8 - PubMed
  176. Arch Mal Coeur Vaiss. 1986 Sep;79(10):1495-505 - PubMed
  177. Am J Cardiol. 1984 Jan 1;53(1):77-83 - PubMed
  178. J Am Coll Cardiol. 1989 Jul;14(1):209-15; discussion 216-7 - PubMed
  179. Am J Cardiol. 1987 Jun 1;59(15):1422-4 - PubMed
  180. Jpn Circ J. 1988 Mar;52(3):254-61 - PubMed
  181. Am J Cardiol. 1984 Nov 14;54(9):26D-28D - PubMed
  182. Wien Klin Wochenschr. 1990 Sep 14;102(17):510-3 - PubMed
  183. Pacing Clin Electrophysiol. 1992 Apr;15(4 Pt 1):387-90 - PubMed
  184. Clin Pharmacol Ther. 1990 Jun;47(6):740-6 - PubMed
  185. J Cardiovasc Pharmacol. 1991 Aug;18(2):254-60 - PubMed
  186. Am J Cardiol. 1984 Nov 14;54(9):53D-59D - PubMed
  187. Chest. 1988 Oct;94(4):853-4 - PubMed
  188. Ann Cardiol Angeiol (Paris). 1988 Mar;37(3):133-6 - PubMed
  189. Eur Heart J. 1988 Nov;9(11):1188-93 - PubMed
  190. Ann Cardiol Angeiol (Paris). 1986 Mar;35(3):173-9 - PubMed
  191. Acta Med Scand. 1988;223(6):515-23 - PubMed
  192. Am J Cardiol. 1984 Nov 14;54(9):40D-44D - PubMed
  193. Ann Cardiol Angeiol (Paris). 1989 Jan;38(1):37-42 - PubMed
  194. Circ Res. 1989 Dec;65(6):1565-79 - PubMed
  195. Am J Cardiol. 1984 Nov 14;54(9):13D-19D - PubMed
  196. Am Heart J. 1991 Dec;122(6):1788-90 - PubMed
  197. Circulation. 1989 May;79(5):1068-76 - PubMed
  198. Br J Pharmacol. 1989 Jul;97(3):731-8 - PubMed
  199. Clin Pharmacol Ther. 1989 Jan;45(1):28-33 - PubMed
  200. J Chromatogr. 1989 Oct 27;495 :349-53 - PubMed
  201. Eur Heart J. 1991 Oct;12(10):1112-31 - PubMed
  202. Eur Heart J. 1991 Jul;12(7):796-9 - PubMed
  203. J Am Coll Cardiol. 1990 Nov;16(5):1229-37 - PubMed
  204. Mol Pharmacol. 1991 Jul;40(1):135-42 - PubMed
  205. G Ital Cardiol. 1991 May;21(5):517-26 - PubMed
  206. Eur J Clin Pharmacol. 1990;38(5):509-13 - PubMed
  207. J Cardiovasc Pharmacol. 1989 Aug;14(2):205-12 - PubMed
  208. Ann Emerg Med. 1987 Apr;16(4):437-40 - PubMed
  209. Clin Cardiol. 1987 Jul;10(7):405-10 - PubMed
  210. J Toxicol Clin Toxicol. 1990;28(4):433-44 - PubMed
  211. Arzneimittelforschung. 1988 Sep;38(9):1345-6 - PubMed
  212. J Am Coll Cardiol. 1992 Oct;20(4):911-4 - PubMed
  213. J Clin Pharmacol. 1990 Mar;30(3):226-34 - PubMed
  214. Am J Cardiol. 1989 Dec 5;64(20):37J-40J - PubMed
  215. Am J Cardiol. 1989 May 15;63(17):1275-8 - PubMed
  216. Am Heart J. 1992 Jul;124(1):104-9 - PubMed
  217. Am J Cardiol. 1985 Jun 1;55(13 Pt 1):1520-4 - PubMed
  218. Ther Drug Monit. 1991 Mar;13(2):157-65 - PubMed
  219. Eur J Clin Pharmacol. 1988;34(2):187-94 - PubMed
  220. J Cardiovasc Pharmacol. 1989 Sep;14(3):351-7 - PubMed
  221. Ann Cardiol Angeiol (Paris). 1989 Nov;38(9):555-60 - PubMed
  222. J Am Coll Cardiol. 1992 Sep;20(3):547-51 - PubMed
  223. Therapie. 1991 May-Jun;46(3):254-5 - PubMed
  224. Am J Cardiol. 1983 Dec 1;52(10):1208-13 - PubMed
  225. Cardiologia. 1990 Apr;35(4):291-4 - PubMed
  226. Biol Mass Spectrom. 1991 Jun;20(6):382-8 - PubMed
  227. J Am Coll Cardiol. 1987 Nov;10(5):1145-8 - PubMed
  228. Br Heart J. 1992 Jun;67(6):491-7 - PubMed
  229. Dev Pharmacol Ther. 1991;17 (1-2):24-34 - PubMed
  230. Z Kardiol. 1988 Jul;77(7):464-9 - PubMed
  231. Arzneimittelforschung. 1983;33(5):763-70 - PubMed
  232. Eur Heart J. 1992 Sep;13(9):1251-8 - PubMed
  233. Pacing Clin Electrophysiol. 1991 Nov;14(11 Pt 2):2028-34 - PubMed
  234. Can J Cardiol. 1991 Nov;7(9):407-9 - PubMed
  235. N Engl J Med. 1990 Jun 21;322(25):1764-8 - PubMed
  236. J Pharmacol Exp Ther. 1988 Mar;244(3):950-5 - PubMed
  237. Can J Physiol Pharmacol. 1990 Jul;68(7):851-5 - PubMed
  238. J Pharmacol Exp Ther. 1988 Aug;246(2):419-26 - PubMed

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