v d Meiracker A, Man in't Veld A J, van Eck H R, Wenting G J, Schalekamp M A
J Hypertens Suppl. 1984 Dec;2(3):S581-3.
The acute haemodynamic effects of the non-selective beta-adrenoceptor antiagonist pindolol which has considerable intrinsic sympathomimetic activity (ISA), were studied in 10 patients with essential hypertension for 24 h. One hour after oral dosing (10 mg), the drug reduced supine arterial pressure significantly. The maximum antihypertensive effect was observed after 3-4 h (-15 +/- 3%, P less than 0.001). The fall in arterial pressure was associated with a 25% reduction of systemic vascular resistance (P less than 0.001) after 24 h. By that time cardiac output was increased by 16 +/- 5% (P less than 0.05). Cardiac filling pressures and pulmonary artery pressure did not change. The vasodilator effect of pindolol cannot easily be explained by suppression of plasma renin activity since changes in arterial pressure and plasma renin were inversely correlated (r = -0.58, P less than 0.001). Despite the antihypertensive and vasodilator effect of pendolol, plasma noradrenaline did not rise. The rapid fall in arterial pressure and systemic vascular resistance may be explained by the absence of an initial reflex vasoconstriction which normally follows blockade of cardiac beta-receptors. This may be related to ISA on cardiac and vascular postsynaptic beta-receptors. Concomitant blockade of central and/or peripheral presynaptic beta-receptors is suggested by the absence of a rise in plasma noradrenaline and may contribute to the vasodilator action of pindolol.
对10例原发性高血压患者进行了24小时研究，以观察具有显著内在拟交感活性（ISA）的非选择性β-肾上腺素能受体拮抗剂吲哚洛尔的急性血流动力学效应。口服给药（10毫克）1小时后，该药显著降低了仰卧位动脉压。3-4小时后观察到最大降压效果（-15±3%，P<0.001）。24小时后，动脉压下降与全身血管阻力降低25%相关（P<0.001）。此时心输出量增加了16±5%（P<0.05）。心脏充盈压和肺动脉压未发生变化。吲哚洛尔的血管舒张作用难以通过抑制血浆肾素活性来解释，因为动脉压变化与血浆肾素呈负相关（r=-0.58，P<0.001）。尽管吲哚洛尔具有降压和血管舒张作用，但血浆去甲肾上腺素并未升高。动脉压和全身血管阻力的快速下降可能是由于缺乏通常在心脏β受体阻断后出现的初始反射性血管收缩。这可能与心脏和血管突触后β受体的ISA有关。血浆去甲肾上腺素未升高提示中枢和/或外周突触前β受体同时被阻断，这可能有助于吲哚洛尔的血管舒张作用。
