Wenger T L, Masterton C E, Abou-Donia M B, Bache R J, Strauss H C
J Cardiovasc Pharmacol. 1979 Jan-Feb;1(1):155-61. doi: 10.1097/00005344-197901000-00015.
The aim of this investigation was to examine the distribution of procainamide in the canine heart. Eight anesthetized open-chest dogs received intravenous infusions of 14C-labeled procainamide at 40 micrograms/kg/min for 4 hr. Just prior to the end of the infusion period, 51Cr-labeled microspheres were injected into the left atrium to measure regional myocardial blood flow. The heart was then excised and dissected into regional myocardial sections from each cardiac chamber. Samples from each section were combusted, and the liberated 14CO2 was trapped and counted to determine regional myocardial procainamide concentration. The remainder of each section was analyzed for 51Cr to determine regional myocardial blood flow. Plasma procainamide concentration (mean +/- SE) at the termination of the infusion was 2.68 +/- 0.14 micrograms/ml. Left ventricular procainamide concentration was 6.09 +/- 0.46 micrograms/g. The right ventricular drug concentration was 94% (NS), the left atrial concentration was 85% (p less than 0.005), and the right atrial concentration was 79% (p less than 0.005) of the left ventricular concentration. Within the myocardium of each cardiac chamber there was no correlation between drug concentration and blood flow. We conclude that these concentration differences are insufficient to explain differences in procainamide efficacy between ventricular and atrial arrhythmias.
本研究的目的是检测普鲁卡因酰胺在犬心脏中的分布情况。八只麻醉开胸犬以40微克/千克/分钟的速度静脉输注14C标记的普鲁卡因酰胺,持续4小时。在输注期结束前,将51Cr标记的微球注入左心房以测量局部心肌血流量。然后切除心脏,并将每个心腔的心肌切成局部心肌切片。每个切片的样本进行燃烧,捕获并计数释放的14CO2以确定局部心肌普鲁卡因酰胺浓度。每个切片的其余部分分析51Cr以确定局部心肌血流量。输注结束时血浆普鲁卡因酰胺浓度(平均值±标准误)为2.68±0.14微克/毫升。左心室普鲁卡因酰胺浓度为6.09±0.46微克/克。右心室药物浓度为左心室浓度的94%(无显著性差异),左心房浓度为85%(p<0.005),右心房浓度为79%(p<0.005)。在每个心腔的心肌内,药物浓度与血流量之间无相关性。我们得出结论,这些浓度差异不足以解释普鲁卡因酰胺对室性和房性心律失常疗效的差异。