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β-肾上腺素能受体阻断药的中心血流动力学:β1选择性与内在拟交感活性

Central hemodynamics of beta-adrenoceptor blocking drugs: beta 1 selectivity versus intrinsic sympathomimetic activity.

作者信息

Svendsen T L

出版信息

J Cardiovasc Pharmacol. 1983;5 Suppl 1:S21-5.

PMID:6188916
Abstract

It was the purpose of the present study to assess the hemodynamic effects of adrenergic beta-receptor blocking drugs possessing intrinsic sympathomimetic activity (ISA) and/or beta 1 selectivity, both at rest and during exercise. The hemodynamic effects of seven different beta-blockers (propranolol, atenolol, acebutolol, ICI 72,222, ICI 89,406, and pindolol) were studied at rest in patients with ischemic heart disease. Heart rate (HR), cardiac output (CO), arterial blood pressure (BP), and pulmonary artery pressure (PP) were determined. At rest, it was possible to subdivide the various beta-blockers into three main groups according to the degree of ISA. One group without ISA, including propranolol and atenolol, reduced CO by 25% and HR by 15%. A second group with moderate ISA, represented by practolol, acebutolol and ICI 72,222, reduced CO only by 15% and HR by 10%. A third group with pronounced ISA, represented by pindolol and ICI 89,406, did not change CO and HR significantly. All three groups consisted of drugs both with and without beta 1 selectivity. During exercise, pindolol and propranolol reduced CO, HR, and BP to the same extent. In conclusion, the central hemodynamic response to beta-blockers at rest is determined by the degree of ISA, whereas beta 1 selectivity does not modify the central hemodynamic response to beta-blockade. However, the hemodynamic differences between adrenergic beta-blocking drugs with and without ISA disappear in situations with increased sympathetic drive, such as exercise.

摘要

本研究的目的是评估具有内在拟交感活性(ISA)和/或β1选择性的肾上腺素能β受体阻滞剂在静息和运动时的血流动力学效应。在缺血性心脏病患者静息状态下,研究了七种不同β受体阻滞剂(普萘洛尔、阿替洛尔、醋丁洛尔、ICI 72,222、ICI 89,406和吲哚洛尔)的血流动力学效应。测定心率(HR)、心输出量(CO)、动脉血压(BP)和肺动脉压(PP)。静息时,根据ISA程度可将各种β受体阻滞剂分为三大组。一组无ISA,包括普萘洛尔和阿替洛尔,使CO降低25%,HR降低15%。第二组具有中度ISA,以心得宁、醋丁洛尔和ICI 72,222为代表,仅使CO降低15%,HR降低10%。第三组具有明显ISA,以吲哚洛尔和ICI 89,406为代表,CO和HR无显著变化。所有三组均包含有和无β1选择性的药物。运动时,吲哚洛尔和普萘洛尔使CO、HR和BP降低的程度相同。总之,静息时对β受体阻滞剂的中心血流动力学反应取决于ISA程度,而β1选择性并不改变对β受体阻滞的中心血流动力学反应。然而,在交感神经驱动增加的情况下,如运动时,有和无ISA的肾上腺素能β受体阻滞剂之间的血流动力学差异消失。

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