Jaillon P, Heckle J, Jais J M, Poveda-Sierra J, Cheymol G
J Cardiovasc Pharmacol. 1982 May-Jun;4(3):486-92. doi: 10.1097/00005344-198205000-00021.
We compared the acute electrophysiologic properties of prifuroline (P), a new aminopyrroline derivative, to those of amiodarone (A) in pentobarbital-anesthetized dogs using His bundle recordings and programmed stimulation. Ten dogs received in randomized order four cumulative doses of P (2.5-20 mg/kg) and of A (1.25-10 mg/kg) with a 14-day interval between drug administrations. In a control group of four dogs receiving the diluent of the drugs, no significant changes occurred in cardiac automaticity, conduction, and refractoriness except for the atrioventricular (AV) nodal functional refractory period (RP), which increased with time (p less than 0.05). P and A produced a significant dose-related decrease in heart rate and in sinus node recovery time, with A being 3.7-3.1 times more potent than P. While atrionodal conduction time increased with both drugs, only P resulted in a significant dose-related increase in the His-Purkinje system conduction time. Prifuroline was 2.9 times more potent than A in increasing the atrial effective refractory period, while A was 2.5 times more potent than P in increasing the ventricular effective refractory period. Both drugs increased the AV nodal refractoriness in a dose-dependent way. These results suggest that the new compound prifuroline possesses some properties similar to intravenous amiodarone on sinus automaticity, atrionodal conduction, and atrial and ventricular refractoriness. However, its effects on the His-Purkinje System are typical of those of a class I quinidine-like agent.
我们使用希氏束记录和程控刺激,在戊巴比妥麻醉的犬中比较了新型氨基吡咯啉衍生物普呋罗林(P)与胺碘酮(A)的急性电生理特性。10只犬按随机顺序接受4个累积剂量的P(2.5 - 20mg/kg)和A(1.25 - 10mg/kg),两次给药间隔14天。在接受药物稀释剂的4只犬的对照组中,除房室(AV)结功能不应期(RP)随时间增加(p < 0.05)外,心脏自律性、传导和不应期无显著变化。P和A均使心率和窦房结恢复时间显著剂量依赖性降低,A的效力比P高3.7 - 3.1倍。虽然两种药物均使房结传导时间增加,但只有P导致希氏 - 浦肯野系统传导时间显著剂量依赖性增加。普呋罗林在增加心房有效不应期方面的效力比A高2.9倍,而A在增加心室有效不应期方面的效力比P高2.5倍。两种药物均以剂量依赖性方式增加AV结不应期。这些结果表明,新化合物普呋罗林在窦房自律性、房结传导以及心房和心室不应期方面具有一些与静脉注射胺碘酮相似的特性。然而,其对希氏 - 浦肯野系统的作用是典型的I类奎尼丁样药物的作用。