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心绞痛患者血浆普萘洛尔浓度与治疗反应的相关性。

Correlation of plasma propranolol concentration with therapeutic response in patients with angina pectoris.

作者信息

Pine M, Favrot L, Smith S, McDonald K, Chidsey C A

出版信息

Circulation. 1975 Nov;52(5):886-93. doi: 10.1161/01.cir.52.5.886.

Abstract

The therapeutic response to propranolol was evaluated in patients with documented coronary artery disease at doses varying from 40 to 320 mg/day. Therapeutic response was quantified by evaluating exercise performance on a treadmill and then related to plasma propranolol concentration. Plasma propranolol was defined in terms of beta-adrenergic blockade by comparison with dose (concentration) response curves in normal subjects. Individual therapeutic benefit occurred at doses which averaged 144 +/- 21 mg/day and at concentrations which averaged 30 +/- 7 ng/ml. There was a wide variation between both dose and concentration among the patients at maximum therapeutic response, but when the plasma propranolol was related to pharmacologic activity, the maximum therapeutic response was observed between 64 to 98% of total blockade. Despite the increased exercise performance in these patients, the double product of heart rate and systolic blood pressure was always less, suggesting either an alteration of the relation between myocardial oxygen consumption and the double product during propranolol or a reduction on oxygen delivery to the myocardium as the result of beta-adrenergic blockade of the coronary vasculature.

摘要

对确诊为冠状动脉疾病的患者,评估了每日40至320毫克不同剂量普萘洛尔的治疗反应。通过评估跑步机上的运动表现来量化治疗反应,然后将其与血浆普萘洛尔浓度相关联。通过与正常受试者的剂量(浓度)反应曲线比较,根据β-肾上腺素能阻滞来定义血浆普萘洛尔。个体治疗获益出现在平均每日剂量为144±21毫克、平均浓度为30±7纳克/毫升时。在最大治疗反应时,患者之间的剂量和浓度差异很大,但当血浆普萘洛尔与药理活性相关时,在总阻滞的64%至98%之间观察到最大治疗反应。尽管这些患者的运动表现有所提高,但心率与收缩压的乘积始终较低,这表明在服用普萘洛尔期间,心肌耗氧量与该乘积之间的关系发生了改变,或者是由于冠状动脉血管的β-肾上腺素能阻滞导致心肌氧输送减少。

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