Matsumoto N, Hayasaki K
Department of Cardiovascular Medicine, Saiseikai Kumamoto Hospital.
Kokyu To Junkan. 1990 Apr;38(4):383-9.
The effects of aprindine, 100 mg iv, on hemodynamics, and the relationship between its inhibitory effect on PVC and its levels in the blood were determined in patients with diminished cardiac function. PVC was inhibited in 7 of 13 patients (54%), compared with a 50% inhibition rate in controls. The levels of aprindine in the blood after intravenous administration, rapidly decreased from 1.78 +/- 1.09 micrograms/ml immediately after administration, to 0.80 +/- 0.25 micrograms/ml after 15 min, to 0.65 +/- 0.23 micrograms/ml after 30 min and to 0.56 +/- 0.19 micrograms/ml after 1 hour. The duration of blood levels of 0.55 +/- 0.35 micrograms/ml, which are the levels presumed to be effective, was one hour after administration. The mean elimination half-life of aprindine was 18.9 +/- 8.4 hours. Aprindine produced relatively little effect on hemodynamics in patients with moderate to severe heart failure, but when its effects in individual cases were studied, it was found that aprindine elicited such changes as reduction in cardiac index, stroke volume index and stroke work index, and elevation in pulmonary arterial diastolic pressure. These findings suggest that care should be exercised in aprindine therapy in patients with diminished cardiac function. At least there should be monitoring of blood pressure and heart rate at appropriate times after intravenous administration.
在心脏功能减退的患者中，测定了静脉注射100毫克安搏律定对血流动力学的影响，以及其对室性早搏（PVC）的抑制作用与其血药浓度之间的关系。13例患者中有7例（54%）的PVC受到抑制，而对照组的抑制率为50%。静脉给药后，安搏律定的血药浓度迅速下降，给药后即刻从1.78±1.09微克/毫升降至15分钟后的0.80±0.25微克/毫升，30分钟后降至0.65±0.23微克/毫升，1小时后降至0.56±0.19微克/毫升。假定有效的血药浓度0.55±0.35微克/毫升的持续时间为给药后1小时。安搏律定的平均消除半衰期为18.9±8.4小时。安搏律定对中重度心力衰竭患者的血流动力学影响相对较小，但在研究其对个别病例的影响时发现，安搏律定可引起心脏指数、每搏量指数和每搏功指数降低，以及肺动脉舒张压升高。这些发现提示，对心脏功能减退的患者进行安搏律定治疗时应谨慎。至少在静脉给药后的适当时间应监测血压和心率。
