Hulting J, Jansson B
Eur J Clin Pharmacol. 1977 Jan 3;11(2):91-9. doi: 10.1007/BF00562898.
Ten patients with various heart diseases and ventricular arrhythmia received a single oral dose of disopyramide (DE) 200 mg. The ECG was recorded continuously for about 50 h from 2-4 h before drug administration. A statistically significant reduction in the number of ventricular ectopic beats (VEBs) was seen 1.0-3.5 h after drug intake; the average number of VEBs per 30 min decreased from 317 during the control period to 92 by 1.0-3.5 h after treatment and if one patient who did not respond is excluded, the corresponding figures were 272 and 14, respectively. Consecutive VEBs were seen in seven patients before DE was given and decreased significantly (p less than 0.05) 1.5-5.5 h after drug administration. There was no change in the PQ interval, the QRS interval showed a slight increase, whereas the QT interval was prolonged 0.5-4 h after administration of DE. A specific gas chromatographic method was used for DE assay in plasma and urine. Absorption was rapid in all patients. Urinary excretion during the first 48 h after drug intake varied between 35 and 75%. The lowest effective antiarrhythmic concentration estimated in six patients ranged from 1.4 to 7.0 mug/ml. beta-Phase half-life in five patients was between 10.3 and 22.1 h.
10名患有各种心脏病和室性心律失常的患者单次口服200毫克丙吡胺(DE)。在给药前2至4小时开始连续记录心电图约50小时。服药后1.0至3.5小时,室性早搏(VEB)数量出现统计学显著减少;每30分钟的VEB平均数量从对照期的317次降至治疗后1.0至3.5小时的92次,若排除一名无反应的患者,相应数字分别为272次和14次。给药前有7名患者出现连续VEB,给药后1.5至5.5小时显著减少(p小于0.05)。PQ间期无变化,QRS间期略有增加,而给药后0.5至4小时QT间期延长。采用特定的气相色谱法测定血浆和尿液中的DE。所有患者吸收迅速。服药后前48小时的尿排泄率在35%至75%之间。6名患者估计的最低有效抗心律失常浓度范围为1.4至7.0微克/毫升。5名患者的β相半衰期在10.3至22.1小时之间。