propafenone

Summary

Summary: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.

Top Publications

  1. Gorenek B, Cavusoglu Y, Goktekin O, Birdane A, Kudaiberdieva G, Ata N, et al. Amiodarone versus Sotalol and Propafenone for prevention of immediate recurrence of atrial fibrillation after internal cardioversion: importance of P wave analysis. Int J Cardiol. 2006;106:268-9 pubmed
  2. Morike K, Kivistö K, Schaeffeler E, Jägle C, Igel S, Drescher S, et al. Propafenone for the prevention of atrial tachyarrhythmias after cardiac surgery: a randomized, double-blind placebo-controlled trial. Clin Pharmacol Ther. 2008;84:104-10 pubmed publisher
    We studied the efficacy of propafenone in preventing atrial tachyarrhythmias after cardiac surgery, and the possible relationships between CYP2D6 polymorphism and the efficacy, pharmacokinetics, and tolerability of propafenone...
  3. Dilger K, Hofmann U, Klotz U. Enzyme induction in the elderly: effect of rifampin on the pharmacokinetics and pharmacodynamics of propafenone. Clin Pharmacol Ther. 2000;67:512-20 pubmed
    ..induction in elderly subjects was performed by investigation of the effect of rifampin (INN, rifampicin) on propafenone disposition...
  4. Jazwinska Tarnawska E, Orzechowska Juzwenko K, Niewinski P, Rzemislawska Z, Loboz Grudzien K, Dmochowska Perz M, et al. The influence of CYP2D6 polymorphism on the antiarrhythmic efficacy of propafenone in patients with paroxysmal atrial fibrillation during 3 months propafenone prophylactic treatment. Int J Clin Pharmacol Ther. 2001;39:288-92 pubmed
    b>Propafenone (PPF) is an antiarrhythmic, Class Ic agent. Its metabolism is genetically controlled by a cytochrome P450 isoenzyme named CYP2D6, which shows polymorphism in human population...
  5. Kowey P, Yannicelli D, Amsterdam E. Effectiveness of oral propafenone for the prevention of atrial fibrillation after coronary artery bypass grafting. Am J Cardiol. 2004;94:663-5 pubmed
    The efficacy and safety of oral propafenone for the prevention of atrial fibrillation (AF) were tested in a group of 293 patients who underwent coronary artery bypass grafting...
  6. Alfonsi E, Merlo I, Tonini M, Ravaglia S, Brugnoni R, Gozzini A, et al. Efficacy of propafenone in paramyotonia congenita. Neurology. 2007;68:1080-1 pubmed
  7. Gareri P, De Fazio P, Gallelli L, De Fazio S, Davoli A, Seminara G, et al. Venlafaxine-propafenone interaction resulting in hallucinations and psychomotor agitation. Ann Pharmacother. 2008;42:434-8 pubmed publisher
    To report a case of visual hallucinations and psychomotor agitation probably induced by an interaction between venlafaxine and propafenone.
  8. Xu L, Huang C, Chen J, Jiang X, Li X, Bett G, et al. Effect of amiodarone on Kv1.4 channel C-type inactivation: comparison of its effects with those induced by propafenone and verapamil. Pharmazie. 2008;63:475-9 pubmed
    ..4 C-type inactivation and compare amiodarone's effects on Kv1.4 with propafenone and verapamil. Our data show that those three antiarrhythmic drugs blocked fKv1...
  9. Amit G, Rosen A, Wagshal A, Bonneh D, Liss T, Grosbard A, et al. Efficacy of substituting innovator propafenone for its generic formulation in patients with atrial fibrillation. Am J Cardiol. 2004;93:1558-60 pubmed
    The clinical outcomes of 114 patients with atrial fibrillation who had been treated with the innovator propafenone, and in whom the drug was then replaced with generic propafenone because of cost containment, were compared...

More Information

Publications62

  1. Langer T, Eder M, Hoffmann R, Chiba P, Ecker G. Lead identification for modulators of multidrug resistance based on in silico screening with a pharmacophoric feature model. Arch Pharm (Weinheim). 2004;337:317-27 pubmed
    ..Comparative molecular field analysis (CoMFA) led to distinct 3D-QSAR models for propafenone and phenothiazine analogs...
  2. Pintaric H, Manola S, Nossan J, Pavlovic N, Delic Brkljacic D, Radeljic V. Electrophysiological effects, efficacy and safety of intravenous propafenone in termination of atrioventricular nodal reentrant tachycardia and atrioventricular reentrant tachycardia: a prospective non-randomized interventional study. Acta Clin Croat. 2010;49:25-31 pubmed
    ..interventional study was to assess electrophysiological effects, efficacy and safety of intravenous propafenone in termination of atrioventricular nodal reentrant tachycardia (AVNRT) and orthodromic atrioventricular ..
  3. Freemantle N, Lafuente Lafuente C, Mitchell S, Eckert L, Reynolds M. Mixed treatment comparison of dronedarone, amiodarone, sotalol, flecainide, and propafenone, for the management of atrial fibrillation. Europace. 2011;13:329-45 pubmed publisher
    ..Mixed treatment comparisons (MTC) were performed to assess the relative efficacy and tolerability of the main anti-arrhythmic drugs used for the treatment of atrial fibrillation (AF)/flutter...
  4. Lappin G, Shishikura Y, Jochemsen R, Weaver R, Gesson C, Brian Houston J, et al. Comparative pharmacokinetics between a microdose and therapeutic dose for clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen), and phenobarbital in human volunteers. Eur J Pharm Sci. 2011;43:141-50 pubmed publisher
    ..g) to predict the human pharmacokinetics (PK) following a therapeutic dose of clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen) and phenobarbital, both within the study and by reference to the existing ..
  5. Sestito A, Molina E. Atrial fibrillation and the pharmacological treatment: the role of propafenone. Eur Rev Med Pharmacol Sci. 2012;16:242-53 pubmed
    ..Among antiarrhythmic agents, drugs that inhibit early sodium current (as propafenone) are proven effective in atrial fibrillation...
  6. Hoppe U, Beuckelmann D. Modulation of the hyperpolarization-activated inward current (If) by antiarrhythmic agents in isolated human atrial myocytes. Naunyn Schmiedebergs Arch Pharmacol. 1998;358:635-40 pubmed
    ..However, propafenone (10(-5) mol/l) was found to reversibly reduce If current size (9/13 cells) by shifting the activation curve by -..
  7. Azpitarte J, Alvarez M, Baun O, Garcia R, Moreno E, Martin F, et al. Value of single oral loading dose of propafenone in converting recent-onset atrial fibrillation. Results of a randomized, double-blind, controlled study. Eur Heart J. 1997;18:1649-54 pubmed
    To evaluate the efficacy and safety of a single loading oral dose of propafenone in the interruption of recent-onset atrial fibrillation...
  8. Anzenbacherova E, Anzenbacher P, Svoboda Z, Ulrichova J, Kvetina J, Zoulová J, et al. Minipig as a model for drug metabolism in man: comparison of in vitro and in vivo metabolism of propafenone. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2003;147:155-9 pubmed
    ..suitability of minipigs as experimental animal in modeling of the drug metabolism and pharmacokine-tics in man, propafenone metabolism in vitro at the microsomal level as well as propafenone pharmacokinetics in the minipig was studied...
  9. Younan L, Barada K, Faraj W, Tawil A, Jabbour M, Khoury M, et al. Propafenone hepatotoxicity: report of a new case and review of the literature. Saudi J Gastroenterol. 2013;19:235-7 pubmed publisher
    b>Propafenone is a class Ic antiarrhythmic drug. It is a beta-adrenergic blocker that causes bradycardia and bronchospasm. It is metabolized primarily in the liver...
  10. Kosior D, Kochanowski J, Scisło P, Piatkowski R, Postuła M, Rabczenko D, et al. Efficacy and tolerability of oral propafenone versus quinidine in the treatment of recent onset atrial fibrillation: A randomized, prospective study. Cardiol J. 2009;16:521-7 pubmed
    A prospective, randomized study was conducted to evaluate the efficacy and tolerability of oral propafenone and quinidine for the conversion of paroxysmal atrial fibrillation (AF)...
  11. Huh S, Jung E, Lee J, Roh K, Kim J, Lee J, et al. Mechanisms of melanogenesis inhibition by propafenone. Arch Dermatol Res. 2010;302:561-5 pubmed publisher
    ..The present study was conducted to determine the inhibitory effects of propafenone on melanogenesis and to elucidate the molecular events involved in the inhibition of melanogenesis by ..
  12. Windisch A, Timin E, Schwarz T, Stork Riedler D, Erker T, Ecker G, et al. Trapping and dissociation of propafenone derivatives in HERG channels. Br J Pharmacol. 2011;162:1542-52 pubmed publisher
    ..A small molecule-like propafenone is efficiently trapped in the closed HERG channel conformation...
  13. Meinertz T, Lip G, Lombardi F, Sadowski Z, Kalsch B, Camez A, et al. Efficacy and safety of propafenone sustained release in the prophylaxis of symptomatic paroxysmal atrial fibrillation (The European Rythmol/Rytmonorm Atrial Fibrillation Trial [ERAFT] Study). Am J Cardiol. 2002;90:1300-6 pubmed
    ..placebo-controlled, and well-controlled trial to prove that the sustained-release (SR) formulation of propafenone is superior to placebo in preventing symptoms of paroxysmal atrial fibrillation (AF)...
  14. Paul A, Witchel H, Hancox J. Inhibition of the current of heterologously expressed HERG potassium channels by flecainide and comparison with quinidine, propafenone and lignocaine. Br J Pharmacol. 2002;136:717-29 pubmed
    ..potency of FLEC with other Class I agents: quinidine (QUIN, Class Ia); lignocaine (LIG, Class Ib) and propafenone (PROPAF, Class Ic). 2...
  15. Cahill S, Gross G. Propafenone and its metabolites preferentially inhibit IKr in rabbit ventricular myocytes. J Pharmacol Exp Ther. 2004;308:59-65 pubmed
    b>Propafenone is an antiarrhythmic agent with recognized cardiac myocyte repolarizing K+ current inhibitory effects...
  16. Khan I. Single oral loading dose of propafenone for pharmacological cardioversion of recent-onset atrial fibrillation. J Am Coll Cardiol. 2001;37:542-7 pubmed
    The efficacy and safety of the single dose oral loading regimen of propafenone for pharmacological cardioversion of recent-onset atrial fibrillation (AFib) was evaluated by analyzing the trials on the subject identified through a ..
  17. Chiba P, Ecker G, Schmid D, Drach J, Tell B, Goldenberg S, et al. Structural requirements for activity of propafenone-type modulators in P-glycoprotein-mediated multidrug resistance. Mol Pharmacol. 1996;49:1122-30 pubmed
    The sodium channel blocker propafenone and a series of analogs have been identified as effective modulators of P-glyco-protein-mediated multidrug resistance in human tumor cells...
  18. Reder Hilz B, Ullrich M, Ringel M, Hewitt N, Utesch D, Oesch F, et al. Metabolism of propafenone and verapamil by cryopreserved human, rat, mouse and dog hepatocytes: comparison with metabolism in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2004;369:408-17 pubmed
    In the present study we examined the metabolism of [(14)C]propafenone (P) and [(14)C]verapamil (V) using cryopreserved human, dog (Beagle), rat (Sprague-Dawley) and mouse (NMRI) hepatocytes...
  19. Fleischer R, Wiese M. Three-dimensional quantitative structure-activity relationship analysis of propafenone-type multidrug resistance modulators: influence of variable selection on test set predictivity. J Med Chem. 2003;46:4988-5004 pubmed
    An extended set of multidrug-resistance modulators of the propafenone type were investigated using CoMFA and CoMSIA. A number of 3D-QSAR models were derived from steric, electrostatic, and hydrophobic fields and their combinations...
  20. Hong Y, Tang Y, Zeng S. Enantioselective plasma protein binding of propafenone: mechanism, drug interaction, and species difference. Chirality. 2009;21:692-8 pubmed publisher
    The interaction of propafenone (PPF) enantiomers with human plasma, human serum albumin (HSA), alpha(1)-acid glycoprotein (AGP), as well as with plasma from rat, rabbit, and cow was investigated using indirect chiral high performance ..
  21. Zhang D, Wang S, Chen H, Jiang X, Chao S. Effects of diltiazem and propafenone on the inactivation and recovery kinetics of fKv1.4 channel currents expressed in Xenopus oocytes. Acta Pharmacol Sin. 2011;32:465-77 pubmed publisher
    To investigate the effects of diltiazem, an L-type calcium channel blocker, and propafenone, a sodium channel blocker, on the inactivation and recovery kinetics of fKv1...
  22. Mergenthaler J, Haverkamp W, Huttenhofer A, Skryabin B, Musshoff U, Borggrefe M, et al. Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel. Naunyn Schmiedebergs Arch Pharmacol. 2001;363:472-80 pubmed
    b>Propafenone has been shown to affect the delayed-rectifier potassium currents in cardiomyocytes of different animal models...
  23. Chiladakis J, Kalogeropoulos A, Patsouras N, Manolis A. Ibutilide added to propafenone for the conversion of atrial fibrillation and atrial flutter. J Am Coll Cardiol. 2004;44:859-63 pubmed
    We evaluated the safety and efficacy of ibutilide when added to propafenone in treating both paroxysmal and chronic atrial fibrillation (AF) and atrial flutter (AFL)...
  24. Cocozzella D, Curciarello J, Corallini O, Olivera A, Alburquerque M, Fraquelli E, et al. Propafenone hepatotoxicity: report of two new cases. Dig Dis Sci. 2003;48:354-7 pubmed
    Two patients developed acute cholestatic hepatitis during treatment with propafenone. Viral infections, alcohol abuse, hepatotoxicity by other drugs, and biliary obstruction were excluded as causes...
  25. Witchel H, Dempsey C, Sessions R, Perry M, Milnes J, Hancox J, et al. The low-potency, voltage-dependent HERG blocker propafenone--molecular determinants and drug trapping. Mol Pharmacol. 2004;66:1201-12 pubmed
    ..in Xenopus laevis oocytes and were used to characterize the HERG channel binding site of the antiarrhythmic propafenone. Propafenone's blockade of HERG was strongly dependent on residue Phe656 but was insensitive or weakly ..
  26. Klepsch F, Chiba P, Ecker G. Exhaustive sampling of docking poses reveals binding hypotheses for propafenone type inhibitors of P-glycoprotein. PLoS Comput Biol. 2011;7:e1002036 pubmed publisher
    ..In order to identify binding hypotheses for propafenone-type P-gp inhibitors, five different propafenone derivatives with known structure-activity relationship (SAR) ..
  27. Tai C, Chiang C, Lee S, Chen Y, Yu W, Feng A, et al. Persistent atrial flutter in patients treated for atrial fibrillation with amiodarone and propafenone: electrophysiologic characteristics, radiofrequency catheter ablation, and risk prediction. J Cardiovasc Electrophysiol. 1999;10:1180-7 pubmed
    ..Among the 136 patients treated for atrial fibrillation with amiodarone (n = 96) or propafenone (n = 40), 15 (11%, mean age 65.5 +/- 12...
  28. Martínez Marcos F, Garcia Garmendia J, Ortega Carpio A, Fernandez Gomez J, Santos J, Camacho C. Comparison of intravenous flecainide, propafenone, and amiodarone for conversion of acute atrial fibrillation to sinus rhythm. Am J Cardiol. 2000;86:950-3 pubmed
    ..patients with acute (< or = 48 hours' duration) atrial fibrillation to receive intravenous flecainide, propafenone, or amiodarone. Flecainide and propafenone were administered as a bolus dose of 2 mg/kg in 20 minutes...
  29. Klopman G, Zhu H, Ecker G, Chiba P. MCASE study of the multidrug resistance reversal activity of propafenone analogs. J Comput Aided Mol Des. 2003;17:291-7 pubmed
    A database containing 130 propafenone type chemicals which have been tested for their multidrug resistance (MDR) reversal activity was compiled...
  30. Madeja M, Steffen W, Mesic I, Garic B, Zhorov B. Overlapping binding sites of structurally different antiarrhythmics flecainide and propafenone in the subunit interface of potassium channel Kv2.1. J Biol Chem. 2010;285:33898-905 pubmed publisher
    ..Flecainide and propafenone are known to block Kv2.1 channels more potently than other Kv channels...
  31. Bauer A, Becker R, Freigang K, Senges J, Voss F, Hansen A, et al. Rate- and site-dependent effects of propafenone, dofetilide, and the new I(Ks)-blocking agent chromanol 293b on individual muscle layers of the intact canine heart. Circulation. 1999;100:2184-90 pubmed
    ..Effective refractory periods (ERPs) were determined at baseline and after application of propafenone (2 mg/kg), dofetilide (30 microg/kg), or chromanol 293b (10 mg/kg) by the extrastimulus technique (BCL 300 and ..
  32. Madeja M, Leicher T, Friederich P, Punke M, Haverkamp W, Musshoff U, et al. Molecular site of action of the antiarrhythmic drug propafenone at the voltage-operated potassium channel Kv2.1. Mol Pharmacol. 2003;63:547-56 pubmed
    The effects of the antiarrhythmic drug propafenone at Kv2.1 channels were studied with wild-type and mutated channels expressed in Xenopus laevis oocytes. Propafenone decreased the Kv2...
  33. Arias C, Gonzalez T, Moreno I, Caballero R, Delpón E, Tamargo J, et al. Effects of propafenone and its main metabolite, 5-hydroxypropafenone, on HERG channels. Cardiovasc Res. 2003;57:660-9 pubmed
    b>Propafenone is a class Ic antiarrhythmic drug used to maintain sinus rhythm in patients with atrial fibrillation. During chronic therapy, it undergoes extensive first-pass hepatic metabolism to 5-hydroxypropafenone...
  34. Kochiadakis G, Igoumenidis N, Hamilos M, Tzerakis P, Klapsinos N, Chlouverakis G, et al. Sotalol versus propafenone for long-term maintenance of normal sinus rhythm in patients with recurrent symptomatic atrial fibrillation. Am J Cardiol. 2004;94:1563-6 pubmed
    ..randomized, single-blinded, placebo-controlled study compared the efficacy and safety of sotalol and propafenone when used for long-term prevention of atrial fibrillation...
  35. Kaiser D, Smiesko M, Kopp S, Chiba P, Ecker G. Interaction field based and hologram based QSAR analysis of propafenone-type modulators of multidrug resistance. Med Chem. 2005;1:431-44 pubmed
    ..Within this paper, a set of propafenone-type inhibitors of P-gp were analyzed using both interaction field based methods such as CoMFA and CoMSIA and ..
  36. Kochiadakis G, Igoumenidis N, Hamilos M, Tzerakis P, Klapsinos N, Zacharis E, et al. Long-term maintenance of normal sinus rhythm in patients with current symptomatic atrial fibrillation: amiodarone vs propafenone, both in low doses. Chest. 2004;125:377-83 pubmed
    To compare the efficacy and safety of amiodarone and propafenone when used for the prevention of atrial fibrillation (AF) and maintenance of normal sinus rhythm in patients with refractory AF. Prospective, randomized, single-blind trial...
  37. Pasek M, Simurda J. Quantitative modelling of interaction of propafenone with sodium channels in cardiac cells. Med Biol Eng Comput. 2004;42:151-7 pubmed
    A mathematical model of the interaction of propafenone with cardiac sodium channels is based on experimental data that demonstrate use-dependent effects of the drug...
  38. Pleban K, Hoffer C, Kopp S, Peer M, Chiba P, Ecker G. Intramolecular distribution of hydrophobicity influences pharmacological activity of propafenone-type MDR modulators. Arch Pharm (Weinheim). 2004;337:328-34 pubmed
    ..In the present study, a series of propafenone-type P-gp inhibitors with systematically varying hydrophobicity distribution within the molecules were ..
  39. Pritchett E, Page R, Carlson M, Undesser K, Fava G. Efficacy and safety of sustained-release propafenone (propafenone SR) for patients with atrial fibrillation. Am J Cardiol. 2003;92:941-6 pubmed
    ..trial was to test the efficacy and safety of a new sustained-release preparation of the antiarrhythmic drug propafenone (propafenone SR) in reducing the frequency of symptomatic arrhythmia recurrences in patients with atrial ..
  40. Pleban K, Kopp S, Csaszar E, Peer M, Hrebicek T, Rizzi A, et al. P-glycoprotein substrate binding domains are located at the transmembrane domain/transmembrane domain interfaces: a combined photoaffinity labeling-protein homology modeling approach. Mol Pharmacol. 2005;67:365-74 pubmed
    ..Available data on LmrA and AcrB, two bacterial multidrug efflux pumps, suggest that binding at domain interfaces may be a general feature of polyspecific drug efflux pumps. ..
  41. Pfeffer F, Grube M. An organic psychosis due to a venlafaxine-propafenone interaction. Int J Psychiatry Med. 2001;31:427-32 pubmed
    ..A significant interaction between venlafaxine and propafenone causes markedly increased serum levels of venlafaxine correlating with unexpected psychopathological changes...
  42. Sant S, Nadeau V, Hildgen P. Effect of porosity on the release kinetics of propafenone-loaded PEG-g-PLA nanoparticles. J Control Release. 2005;107:203-14 pubmed
    ..b>Propafenone hydrochloride (Prop...
  43. Hasdemir C, Olukman M, Ulucan C, Roden D. Brugada-type ECG pattern and extreme QRS complex widening with propafenone overdose. J Cardiovasc Electrophysiol. 2006;17:565-6 pubmed
  44. Walsh K. A real-time screening assay for GIRK1/4 channel blockers. J Biomol Screen. 2010;15:1229-37 pubmed publisher
    ..Analogues of amiloride and propafenone were identified as channel blockers at concentrations less than 1 µM...
  45. Wittkowsky A. The "pill-in-the-pocket" approach to atrial fibrillation. N Engl J Med. 2005;352:1150-1; author reply 1150-1 pubmed
  46. Wyse D. Can recent-onset atrial fibrillation be safely and successfully treated with self-administered antiarrhythmic drugs?. Nat Clin Pract Cardiovasc Med. 2005;2:132-3 pubmed
  47. Wongcharoen W, Tai C, Lin Y, Chang S, Chen S. "Pseudosinus rhythm": what is the mechanism?. J Cardiovasc Electrophysiol. 2005;16:1384-5 pubmed
  48. Kanjwal Y, Imran N, Grubb B. Deglutition induced atrial tachycardia and atrial fibrillation. Pacing Clin Electrophysiol. 2007;30:1575-8 pubmed
    ..She was successfully treated with propafenone with no induction of swallowing-induced tachycardia after treatment...
  49. Akdemir I, Davutoglu V, Aksoy M. Intermittent Brugada syndrome misdiagnosed as acute myocardial infarction and unmasked with propafenone. Heart. 2002;87:543 pubmed
  50. Barranco Garduño L, Flores Pérez J, Juárez Olguín H, Bobadilla Chávez J, Osnaya H, Flores Pérez C. Clinical evidence of the antiarrhythmic effect of a magistral suspension of propafenone: a case report. Arch Cardiol Mex. 2009;79:132-4 pubmed
    b>Propafenone is an antiarrhythmic that has been used for the treatment of tachiarrytmias in both adults and children...
  51. Woo H, Northen T, Yanes O, Siuzdak G. Nanostructure-initiator mass spectrometry: a protocol for preparing and applying NIMS surfaces for high-sensitivity mass analysis. Nat Protoc. 2008;3:1341-9 pubmed publisher
    ..Typically, NIMS surface preparation can be completed in less than 2 h. Subsequent sample preparation requires 1-5 min, depending on sample deposition method. Mass spectrometric data acquisition typically takes 1-30 s per sample. ..
  52. Cabrera Duro A, Rodrigo Carbonero D, Galdeano Miranda J, Martínez Corrales P, Pastor Menchaca E, Macua Biurrun P, et al. [The treatment of postoperative junctional ectopic tachycardia]. An Esp Pediatr. 2002;56:505-9 pubmed
    ..Finally, intravenous propafenone was administered to 5 patients...
  53. Lee J, Klein G, Krahn A, Yee R, Zarnke K, Simpson C, et al. Rate-control versus conversion strategy in postoperative atrial fibrillation: trial design and pilot study results. Card Electrophysiol Rev. 2003;7:178-84 pubmed
    ..Regardless of the strategy, majority of patients will be in sinus rhythm after two months. A larger randomized, controlled study is needed to assess the impact of restoration of sinus rhythm on length of stay. ..