Preclinical Pharmacology of Diprafenone

  • Mark E. Sullivan
  • H. J. Reiser
Conference paper


The development of antiarrhythmic agents and their eventual clinical success depend predominantly on two aspects: efficacy and safety. In the setting of drug development, these data are acquired from a variety of pre-clinical studies conducted in animal models intended to mimic the clinical setting. Diprafenone, a dimethyl analog of propafenone (Fig. 1), is undergoing extensive clinical development in Europe and the United States. A limited number of studies have reported on the cellular electrophysiological properties of the drug [20, 36], as well as its antiarrhythmic efficacy in animal models [13, 36, 29]. Results of recent clinical testing of diprafenone in patients have correlated reasonably well with the pre-clinical arrhythmia models. Manz et al. [23] studied the effects of diprafenone in 31 patients and reported that the drug increased refractoriness throughout the heart (atria, ventricle, A-V node). In addition, these authors reported that diprafenone (1.5 mg/kg, i.v.) was also effective in suppressing programmed electrical stimulation (PES)-induced supraventricular tachycardia in 12 of 17 patients and PES-induced ventricular tachycardia in seven of 10 patients. Heur et al. [16] reported that diprafenone was effective in 21 of 27 patients for controlling ventricular arrhythmias in patients that were refractory to other antiarrhythmic drug therapies. Kunze and Kuck [21] have shown that oral diprafenone (100 mg, t.i.d.) was effective in 13/15 patients in preventing recurrences of supraventricular tachycardia (WPW syndrome) during 10 months of follow-up.


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Copyright information

© Dr. Dietrich Steinkopff Verlag, GmbH & Co. KG, Darmstadt 1990

Authors and Affiliations

  • Mark E. Sullivan
    • 1
  • H. J. Reiser
    • 1
  1. 1.Department of PharmacologyBerlex Laboratories, Inc.Cedar KnollsUSA

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