van den Meiracker A H, Man in 't Veld A J, Ritsema van Eck H J, Schalekamp M A
Am Heart J. 1986 Aug;112(2):368-74. doi: 10.1016/0002-8703(86)90277-2.
Pindolol, a beta blocker with considerable partial agonist activity (PAA), was studied in 10 hypertensive subjects. The maximal fall in mean arterial pressure (MAP) was seen 3 to 4 hours after oral dosing with 10 mg of pindolol (-15 +/- 3%, mean +/- SEM). This was caused by a reduction in total peripheral resistance (TPR), which amounted to 25 +/- 4% after 24 hours. Cardiac output increased by 16 +/- 5%. Cardiac filling pressures and pulmonary artery pressure did not change. Increasing the dose of pindolol, from 5 mg twice a day to 15 mg twice a day over a 3-week period, caused no further change in MAP. After 3 weeks, the fall in MAP (-11 +/- 2%) was maintained by reduced TPR (-26 +/- 6%), whereas cardiac output and stroke volume were increased by 16 +/- 6% and 26 +/- 6%. Renal blood flow and glomerular filtration rate did not change. Beta blockers devoid of PAA lower cardiac output, whereas the elevated TPR in hypertension is unchanged. The hemodynamic profile of pindolol essentially differs from that of beta blockers devoid of PAA.
吲哚洛尔是一种具有显著部分激动剂活性(PAA)的β受体阻滞剂,对10名高血压患者进行了研究。口服10mg吲哚洛尔后3至4小时,平均动脉压(MAP)出现最大降幅(-15±3%,平均值±标准误)。这是由于总外周阻力(TPR)降低所致,24小时后TPR降低了25±4%。心输出量增加了16±5%。心脏充盈压和肺动脉压未发生变化。在3周内将吲哚洛尔剂量从每日两次5mg增加至每日两次15mg,MAP未出现进一步变化。3周后,MAP降幅(-11±2%)通过TPR降低(-26±6%)得以维持,而心输出量和每搏输出量分别增加了16±6%和26±6%。肾血流量和肾小球滤过率未发生变化。缺乏PAA的β受体阻滞剂会降低心输出量,而高血压患者升高的TPR则无变化。吲哚洛尔的血流动力学特征与缺乏PAA的β受体阻滞剂基本不同。