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Chemical Compound Review

Rythmol     1-[2-(2-hydroxy-3- propylamino...

Synonyms: Propafenona, propafenone, Propafenonum, CHEMBL631, GNF-Pf-4594, ...
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Disease relevance of propafenone

  • We randomly assigned patients who had had at least one episode of atrial fibrillation within the previous six months to amiodarone or to sotalol or propafenone, given in an open-label fashion [1].
  • The close time relationship between the administration of the drug and the acute onset of the liver damage, the histological findings, and the reappearance of biochemical signs of liver dysfunction upon rechallenge with the same medication strongly suggest that propafenone was involved in the pathogenesis of this syndrome [2].
  • The recurrence rate of arrhythmia during treatment with propafenone was estimated to be approximately one fifth of the recurrence rate during treatment with placebo [3].
  • Propafenone prolonged refractoriness and slowed conduction of the atrium, the atrioventricular node, and accessory atrioventricular bypass tracts, and these effects provided antiarrhythmic action to halt tachycardia [4].
  • Termination of supraventricular tachycardia occurred in 15 of the 20 patients receiving propafenone but 0 of the 11 patients receiving placebo (p less than 0.01) [4].

Psychiatry related information on propafenone


High impact information on propafenone

  • Adverse events requiring the discontinuation of drug therapy occurred in 18 percent of the patients receiving amiodarone, as compared with 11 percent of those treated with sotalol or propafenone (P=0.06) [1].
  • Nine subjects (with the extensive-metabolizer phenotype) metabolized most of the propafenone to 5-hydroxy propafenone, and five (with the poor-metabolizer phenotype) did not produce this metabolite [7].
  • In this study, we tested the hypothesis that genetically determined variations in the biotransformation of propafenone to its 5-hydroxy metabolite account for variations in the drug's beta-blocking action [7].
  • Propafenone also had a higher affinity for beta 2 receptors in vitro than either of its major metabolites [7].
  • Subgroup analysis showed that among patients without heart disease, 78% of those receiving propafenone and 56% of those receiving placebo converted to sinus rhythm within 8 hours (P = 0.02) [8].

Chemical compound and disease context of propafenone


Biological context of propafenone


Anatomical context of propafenone


Associations of propafenone with other chemical compounds


Gene context of propafenone

  • CONCLUSION: Propafenone is a potent CYP2D6 inhibitor that may cause an increase in plasma concentrations of coadministered CYP2D6 substrates [23].
  • Our data indicate that N-dealkylation of propafenone is mediated via CYP3A4 and CYP1A2 [26].
  • Structural requirements for activity of propafenone-type modulators in P-glycoprotein-mediated multidrug resistance [27].
  • An indirect conclusion from these in vivo data might be that propafenone is not a substrate of the UGT1A1 isoform [28].
  • Two months after discontinuing propafenone, serum aminotransaminase and ALK concentrations had normalized and GGT had decreased and remained only slightly elevated [29].

Analytical, diagnostic and therapeutic context of propafenone


  1. Amiodarone to prevent recurrence of atrial fibrillation. Canadian Trial of Atrial Fibrillation Investigators. Roy, D., Talajic, M., Dorian, P., Connolly, S., Eisenberg, M.J., Green, M., Kus, T., Lambert, J., Dubuc, M., Gagné, P., Nattel, S., Thibault, B. N. Engl. J. Med. (2000) [Pubmed]
  2. Propafenone-induced liver injury: report of a case and review of the literature. Mondardini, A., Pasquino, P., Bernardi, P., Aluffi, E., Tartaglino, B., Mazzucco, G., Bonino, F., Verme, G., Negro, F. Gastroenterology (1993) [Pubmed]
  3. Propafenone treatment of symptomatic paroxysmal supraventricular arrhythmias. A randomized, placebo-controlled, crossover trial in patients tolerating oral therapy. Pritchett, E.L., McCarthy, E.A., Wilkinson, W.E. Ann. Intern. Med. (1991) [Pubmed]
  4. Intravenous propafenone for termination of reentrant supraventricular tachycardia. A placebo-controlled, randomized, double-blind, crossover study. Shen, E.N., Keung, E., Huycke, E., Dohrmann, M.L., Nguyen, N., Morady, F., Sung, R.J. Ann. Intern. Med. (1986) [Pubmed]
  5. Probable propafenone-induced transient global amnesia. Jones, R.J., Brace, S.R., Vander Tuin, E.L. The Annals of pharmacotherapy. (1995) [Pubmed]
  6. Effects of propafenone on directly measured sinoatrial conduction time. Monizzi, D., Padeletti, L., Michelucci, A., Giovannini, T., Romano, S., Montanari, P., Pozzoni, L. Arzneimittel-Forschung. (1988) [Pubmed]
  7. The role of genetically determined polymorphic drug metabolism in the beta-blockade produced by propafenone. Lee, J.T., Kroemer, H.K., Silberstein, D.J., Funck-Brentano, C., Lineberry, M.D., Wood, A.J., Roden, D.M., Woosley, R.L. N. Engl. J. Med. (1990) [Pubmed]
  8. Oral propafenone to convert recent-onset atrial fibrillation in patients with and without underlying heart disease. A randomized, controlled trial. Boriani, G., Biffi, M., Capucci, A., Botto, G.L., Broffoni, T., Rubino, I., Della Casa, S., Sanguinetti, M., Magnani, B. Ann. Intern. Med. (1997) [Pubmed]
  9. Low-dose amiodarone for atrial fibrillation: time for a prospective study? Middlekauff, H.R., Wiener, I., Saxon, L.A., Stevenson, W.G. Ann. Intern. Med. (1992) [Pubmed]
  10. Postrepolarization refractoriness versus conduction slowing caused by class I antiarrhythmic drugs: antiarrhythmic and proarrhythmic effects. Kirchhof, P.F., Fabritz, C.L., Franz, M.R. Circulation (1998) [Pubmed]
  11. Electropharmacologic effects of class I and class III antiarrhythmia drugs on typical atrial flutter: insights into the mechanism of termination. Tai, C.T., Chen, S.A., Feng, A.N., Yu, W.C., Chen, Y.J., Chang, M.S. Circulation (1998) [Pubmed]
  12. Polymorphism of propafenone metabolism and disposition in man: clinical and pharmacokinetic consequences. Siddoway, L.A., Thompson, K.A., McAllister, C.B., Wang, T., Wilkinson, G.R., Roden, D.M., Woosley, R.L. Circulation (1987) [Pubmed]
  13. Effects of antiarrhythmic drugs on canine atrial flutter due to reentry: role of prolongation of refractory period and depression of conduction to excitable gap. Inoue, H., Yamashita, T., Nozaki, A., Sugimoto, T. J. Am. Coll. Cardiol. (1991) [Pubmed]
  14. Clinical pharmacology of propafenone. Connolly, S.J., Kates, R.E., Lebsack, C.S., Harrison, D.C., Winkle, R.A. Circulation (1983) [Pubmed]
  15. Double-blind study of intravenous propafenone for paroxysmal supraventricular reentrant tachycardia. Hammill, S.C., McLaran, C.J., Wood, D.L., Osborn, M.J., Gersh, B.J., Holmes, D.R. J. Am. Coll. Cardiol. (1987) [Pubmed]
  16. Randomized placebo-controlled trial of propafenone for treatment of atrial tachyarrhythmias after cardiac surgery. Connolly, S.J., Mulji, A.S., Hoffert, D.L., Davis, C., Shragge, B.W. J. Am. Coll. Cardiol. (1987) [Pubmed]
  17. Propafenone: a new agent for ventricular arrhythmia. Podrid, P.J., Lown, B. J. Am. Coll. Cardiol. (1984) [Pubmed]
  18. Propafenone preferentially blocks the rapidly activating component of delayed rectifier K+ current in guinea pig ventricular myocytes. Voltage-independent and time-dependent block of the slowly activating component. Delpón, E., Valenzuela, C., Pérez, O., Casis, O., Tamargo, J. Circ. Res. (1995) [Pubmed]
  19. Electrophysiologic and hemodynamic effects of intravenous propafenone in patients with recurrent ventricular tachycardia. Shen, E.N., Sung, R.J., Morady, F., Schwartz, A.B., Scheinman, M.M., DiCarlo, L., Shapiro, W. J. Am. Coll. Cardiol. (1984) [Pubmed]
  20. Molecular site of action of the antiarrhythmic drug propafenone at the voltage-operated potassium channel Kv2.1. Madeja, M., Leicher, T., Friederich, P., Punke, M.A., Haverkamp, W., Musshoff, U., Breithardt, G., Speckmann, E.J. Mol. Pharmacol. (2003) [Pubmed]
  21. Enantiomer/enantiomer interaction of (S)- and (R)-propafenone for cytochrome P450IID6-catalyzed 5-hydroxylation: in vitro evaluation of the mechanism. Kroemer, H.K., Fischer, C., Meese, C.O., Eichelbaum, M. Mol. Pharmacol. (1991) [Pubmed]
  22. Therapy of refractory symptomatic atrial fibrillation and atrial flutter: a staged care approach with new antiarrhythmic drugs. Antman, E.M., Beamer, A.D., Cantillon, C., McGowan, N., Friedman, P.L. J. Am. Coll. Cardiol. (1990) [Pubmed]
  23. Pharmacokinetic and pharmacodynamic interaction between mexiletine and propafenone in human beings. Labbé, L., O'Hara, G., Lefebvre, M., Lessard, E., Gilbert, M., Adedoyin, A., Champagne, J., Hamelin, B., Turgeon, J. Clin. Pharmacol. Ther. (2000) [Pubmed]
  24. The pharmacokinetic and pharmacodynamic interaction between propafenone and lidocaine. Ujhelyi, M.R., O'Rangers, E.A., Fan, C., Kluger, J., Pharand, C., Chow, M.S. Clin. Pharmacol. Ther. (1993) [Pubmed]
  25. Disposition kinetics and dynamics of nicainoprol, a new antiarrhythmic agent, in humans. Ishizaki, T., Horai, Y., Kubota, K., Minegishi, A., Echizen, H., Chiba, K. Clin. Pharmacol. Ther. (1987) [Pubmed]
  26. Identification and characterization of the cytochrome P450 enzymes involved in N-dealkylation of propafenone: molecular base for interaction potential and variable disposition of active metabolites. Botsch, S., Gautier, J.C., Beaune, P., Eichelbaum, M., Kroemer, H.K. Mol. Pharmacol. (1993) [Pubmed]
  27. Structural requirements for activity of propafenone-type modulators in P-glycoprotein-mediated multidrug resistance. Chiba, P., Ecker, G., Schmid, D., Drach, J., Tell, B., Goldenberg, S., Gekeler, V. Mol. Pharmacol. (1996) [Pubmed]
  28. Disposition of propafenone in a poor metabolizer of CYP2D6 with Gilbert's syndrome. Dilger, K., Meisel, P., Hofmann, U., Eichelbaum, M. Therapeutic drug monitoring. (2000) [Pubmed]
  29. Propafenone-induced liver injury. Spinler, S.A., Elder, C.A., Kindwall, K.E. The Annals of pharmacotherapy. (1992) [Pubmed]
  30. Influence of dietary fat on the pharmacodynamics of propafenone in isolated, perfused rabbit hearts. Gillis, A.M., Keashly, R., Watson, P.A., Mathison, H.J., Parsons, H.G. Circulation (1992) [Pubmed]
  31. Effects of oral propafenone administration before electrical cardioversion of chronic atrial fibrillation: a placebo-controlled study. Bianconi, L., Mennuni, M., Lukic, V., Castro, A., Chieffi, M., Santini, M. J. Am. Coll. Cardiol. (1996) [Pubmed]
  32. Effects of oral propafenone on defibrillation and pacing thresholds in patients receiving implantable cardioverter-defibrillators. Propafenone Defibrillation Threshold Investigators. Stevens, S.K., Haffajee, C.I., Naccarelli, G.V., Schwartz, K.M., Luceri, R.M., Packer, D.L., Rubin, A.M., Kowey, P.R. J. Am. Coll. Cardiol. (1996) [Pubmed]
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