Touboul P, Atallah G, Kirkorian G
Eur J Pharmacol. 1980 Jun 27;64(4):297-306. doi: 10.1016/0014-2999(80)90237-x.
The effects of L 9394, a new compound closely related to amiodarone, were investigated in 44 patients by electrophysiological studies. Thirty two patients were given an intravenous injection of one of the following doses: 0.5, 1, 1.5 or 2 mg/kg. Conduction times of the A-V node (A-H interval) and of the His-Purkinje system (H-V interval) were measured by recording the His bundle potential. Refractory periods were determined by the extrastimulus technique. In the remaining 12 subjects, the action of L 9394 on sinus node was assessed. Sinus node recovery time was measured by rapid atrial stimulation and estimated atrial-sinoatrial conduction time deduced from the effects of atrial premature stimulation on sinus node activity. Results were as follows: (1) A-V nodal conduction was depressed after L9394. The A-H interval increased in direct proportion to the dose. Similarly, the effective and functional refractory periods of the A-V node were prolonged, more markedly after higher doses. (2) No change was shown in the His-Purkinje system. The H-V interval was unaltered. (3) L 9394 had no significant effects on the atrial or ventricular muscle. (4) Sinus cycle length as well as sinus node recovery time did not change significantly. In 7/12 patients, results of premature atrial stimulation suggested the formation of a sinoatrial block.
对44例患者进行电生理研究,以调查与胺碘酮密切相关的新化合物L 9394的作用。32例患者静脉注射以下剂量之一:0.5、1、1.5或2mg/kg。通过记录希氏束电位来测量房室结(A-H间期)和希氏-浦肯野系统(H-V间期)的传导时间。采用额外刺激技术测定不应期。在其余12名受试者中,评估L 9394对窦房结的作用。通过快速心房刺激测量窦房结恢复时间,并根据房性早搏刺激对窦房结活动的影响推断估计的房-窦房传导时间。结果如下:(1)L 9394后房室结传导受到抑制。A-H间期与剂量成正比增加。同样,房室结的有效和功能不应期延长,高剂量后更明显。(2)希氏-浦肯野系统未显示变化。H-V间期未改变。(3)L 9394对心房或心室肌无显著影响。(4)窦性周期长度以及窦房结恢复时间无显著变化。在12例患者中的7例中,房性早搏刺激结果提示形成窦房阻滞。