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吲哚洛尔与普萘洛尔降压作用起效时间的比较。一项24小时血流动力学研究。

Comparison of the onset of the antihypertensive action of pindolol and propranolol. A 24 h haemodynamic study.

作者信息

van den Meiracker A H, Man in't Veld A J, Schalekamp M A

机构信息

Department of Internal Medicine I, University Hospital Dijkzigt, Erasmus University Rotterdam, The Netherlands.

出版信息

Br J Clin Pharmacol. 1987;24 Suppl 1(Suppl 1):39S-44S. doi: 10.1111/j.1365-2125.1987.tb03267.x.

Abstract
  1. Haemodynamic changes during the onset of the antihypertensive action of pindolol, 10 mg twice daily, and propranolol, 80 mg three times daily, were studied for 24 h in two groups of 10 patients with uncomplicated essential hypertension. 2. Baseline haemodynamics were not different between the two groups. 3. Pindolol, with considerable intrinsic sympathomimetic activity (ISA) exerted its maximal antihypertensive efficacy within 3-4 after dosing (-15 +/- 3%, mean +/- s.e. mean, P less than 0.001). This effect was maintained for 24 h. 4. After propranolol, which is devoid of ISA, arterial pressure fell more gradually, but after 24 h the two drugs shared an equal antihypertensive effect. 5. Cardiac output rose after pindolol by 16 +/- 5% (P less than 0.01). It decreased transiently by 16 +/- 6% (P less than 0.01) 1-4 h after propranolol. At that time vascular resistance had risen by 18 +/- 5% (P less than 0.001). 6. The onset of the antihypertensive action of the two drugs was associated with reductions in vascular resistance. Since reflex vasoconstriction did not occur after pindolol, vascular resistance was always lower on this drug than on propranolol (-29 +/- 4%, P less than 0.001 vs -15 +/- 5%, P less than 0.01). 7. Cardiac filling pressures, pulmonary artery pressure and pulmonary vascular resistance did not change after pindolol but they rose after propranolol. 8. During the onset of the vasodilator and antihypertensive effects of the two beta-adrenoceptor blockers heart rate, stroke volume and cardiac output rose, despite cardiac beta-adrenoceptor blockade, suggesting a reduction of parasympathetic tone and an increase in venous return.(ABSTRACT TRUNCATED AT 250 WORDS)
摘要
  1. 在两组各10例无并发症的原发性高血压患者中,对每日两次服用10 mg吲哚洛尔和每日三次服用80 mg普萘洛尔的降压作用起效期间的血流动力学变化进行了24小时研究。2. 两组的基线血流动力学无差异。3. 具有相当内在拟交感活性(ISA)的吲哚洛尔在给药后3 - 4小时内发挥其最大降压效力(-15 +/- 3%,平均值 +/- 标准误平均值,P小于0.001)。该效应维持24小时。4. 无ISA的普萘洛尔给药后动脉压下降较为缓慢,但24小时后两种药物的降压效果相同。5. 吲哚洛尔给药后心输出量增加16 +/- 5%(P小于0.01)。普萘洛尔给药后1 - 4小时心输出量短暂下降16 +/- 6%(P小于0.01)。此时血管阻力增加18 +/- 5%(P小于0.001)。6. 两种药物降压作用的起效均与血管阻力降低有关。由于吲哚洛尔给药后未发生反射性血管收缩,该药物作用时的血管阻力始终低于普萘洛尔(-29 +/- 4%,P小于0.001对比 -15 +/- 5%,P小于0.01)。7. 吲哚洛尔给药后心脏充盈压、肺动脉压和肺血管阻力未改变,但普萘洛尔给药后升高。8. 在两种β - 肾上腺素受体阻滞剂的血管舒张和降压作用起效期间,尽管存在心脏β - 肾上腺素受体阻滞,但心率、每搏量和心输出量增加,提示副交感神经张力降低和静脉回流增加。(摘要截断于250字)

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Is the ISA of pindolol beta 2-adrenoceptor selective?吲哚洛尔对β2肾上腺素能受体有选择性吗?
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