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次极量运动期间具有内在拟交感活性的β-肾上腺素能受体阻滞剂的心脏效应

Cardiac effects of beta-adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.

作者信息

Ades P A

机构信息

University of Vermont School of Medicine, Medical Center Hospital of Vermont, Division of Cardiology, Burlington 05401.

出版信息

Br J Clin Pharmacol. 1987;24 Suppl 1(Suppl 1):29S-33S. doi: 10.1111/j.1365-2125.1987.tb03265.x.

Abstract
  1. beta-adrenoceptor blocking agents with intrinsic sympathomimetic activity (ISA) are characterized by lesser depression of cardiac performance during low levels of sympathetic stimulation than beta-adrenoceptor blocking agents lacking ISA. Studies of the effects of ISA on cardiac output and on the determinants of myocardial oxygen demand during submaximal exercise are described and distinct differences between beta-adrenoceptor antagonists with and without ISA emerge. 2. At doses which produce similar effects on maximal exercise heart rate, and resting and exercise systolic blood pressure, pindolol, a beta-adrenoceptor blocking agent with substantial ISA, allows a higher submaximal exercise cardiac output and submaximal heart rate X systolic blood pressure product than does propranolol, a beta-adrenoceptor antagonist without ISA. 3. These findings may have clinical relevance in specific groups of patients such as those with arterial hypertension, where the preservation of cardiac function may allow for a more physiologic exercise response. Implications in patients with coronary artery disease and chronic heart failure await further study.
摘要
  1. 具有内在拟交感活性(ISA)的β肾上腺素受体阻滞剂的特点是,在低水平交感神经刺激期间,其对心脏功能的抑制作用比缺乏ISA的β肾上腺素受体阻滞剂小。本文描述了ISA对次极量运动期间心输出量和心肌需氧量决定因素的影响研究,有ISA和无ISA的β肾上腺素受体拮抗剂之间出现了明显差异。2. 在对最大运动心率、静息和运动收缩压产生相似作用的剂量下,具有显著ISA的β肾上腺素受体阻滞剂吲哚洛尔比无ISA的β肾上腺素受体拮抗剂普萘洛尔能使次极量运动心输出量和次极量心率×收缩压乘积更高。3. 这些发现可能对特定患者群体具有临床意义,如动脉高血压患者,在这类患者中,心脏功能的保留可能允许更生理性的运动反应。对冠心病和慢性心力衰竭患者的影响有待进一步研究。

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Intrinsic sympathomimetic activity: clinical fact or fiction?内在拟交感活性:临床事实还是虚构?
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本文引用的文献

1
Measurement of partial agonist activity of pindolol.吲哚洛尔部分激动剂活性的测定。
Clin Pharmacol Ther. 1981 Nov;30(5):581-6. doi: 10.1038/clpt.1981.207.
2
Attenuation of exercise conditioning by beta-adrenergic blockade.
Circulation. 1982 Apr;65(4):679-84. doi: 10.1161/01.cir.65.4.679.
5
Attenuation of exercise conditioning by low dose beta-adrenergic receptor blockade.
J Am Coll Cardiol. 1983 Sep;2(3):551-6. doi: 10.1016/s0735-1097(83)80284-8.

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