Antifibrillatory effects of BRL-32872 in anesthetized Yucatan minipigs with regional myocardial ischemia

J Cardiovasc Pharmacol. 1995 Oct;26(4):636-44. doi: 10.1097/00005344-199510000-00020.

Abstract

The antifibrillatory potential of BRL-32872, a novel antiarrhythmic compound with K+ and Ca2+ channel blocking activities, was examined in a minipig model of ischemia-induced arrhythmia. The effects of intravenous (i.v.) BRL-32872 (0.3 and 1.0 mg/kg, n = 8), dofetilide (0.3 mg/kg, n = 8), and flecainide (2.0 mg/kg, n = 8), were investigated on the incidence of ventricular fibrillation (VF) during a 20-min occlusion of the left anterior descending coronary artery (LAD). Ischemia-induced VF occurred in 6 of 9 vehicle-treated pigs. BRL-32872 reduced the incidence of ischemic VF to 13% at 0.3 mg/kg (p < 0.05) and to 0% at 1.0 mg/kg (p < 0.01). Dofetilide also prevented the occurrence of VF (0%, p < 0.01) In contrast, flecainide did not reduce the incidence of VF (63%). Indeed, flecainide shortened the time to onset of VF from 17 +/- 1 min in the vehicle group to 10 +/- 1 min (p < 0.001). The antifibrillatory effects of BRL-32872 and dofetilide were associated with a prolongation of QT interval on ECG. Flecainide did not prolong repolarization, but slowed the ventricular conduction velocity, as shown by significant increases in PR and QRS intervals. During early reperfusion, 1 of 8 surviving pigs in each group treated with BRL-32872 and 4 of 8 in the dofetilide group developed VF. This study demonstrated an antifibrillatory effect of BRL-32872 associated with prolonged ventricular repolarization and showed enhanced efficacy over dofetilide on reperfusion arrhythmias which is most likely a consequence of its Ca2+ blocking activity.

MeSH terms

  • Analysis of Variance
  • Animals
  • Anti-Arrhythmia Agents / administration & dosage
  • Anti-Arrhythmia Agents / pharmacology
  • Anti-Arrhythmia Agents / therapeutic use*
  • Benzamides / administration & dosage
  • Benzamides / pharmacology
  • Benzamides / therapeutic use*
  • Disease Models, Animal
  • Flecainide / administration & dosage
  • Flecainide / pharmacology
  • Flecainide / therapeutic use
  • Injections, Intravenous
  • Myocardial Ischemia / complications*
  • Myocardial Ischemia / drug therapy
  • Myocardial Reperfusion Injury / complications
  • Phenethylamines / administration & dosage
  • Phenethylamines / pharmacology
  • Phenethylamines / therapeutic use
  • Sulfonamides / administration & dosage
  • Sulfonamides / pharmacology
  • Sulfonamides / therapeutic use
  • Swine
  • Swine, Miniature
  • Ventricular Fibrillation / drug therapy*
  • Ventricular Fibrillation / etiology

Substances

  • Anti-Arrhythmia Agents
  • Benzamides
  • Phenethylamines
  • Sulfonamides
  • BRL 32872
  • Flecainide
  • dofetilide