Lieu Hsiao D, Shryock John C, von Mering Gregory O, Gordi Toufigh, Blackburn Brent, Olmsted Ann W, Belardinelli Luiz, Kerensky Richard A
Portola Pharmaceuticals, South San Francisco, Calif, USA.
J Nucl Cardiol. 2007 Jul;14(4):514-20. doi: 10.1016/j.nuclcard.2007.02.016.
Regadenoson is a selective A2A adenosine receptor agonist and vasodilator used to increase the heterogeneity of distribution of coronary blood flow during myocardial perfusion imaging. This study characterized the dose dependence of regadenoson-induced coronary hyperemia.
An open-label, dose-escalation study of regadenoson (10-500 microg, rapid intravenous bolus) was performed in 34 subjects; in 4 additional subjects, the effect of aminophylline to reverse the response to regadenoson was determined. Intracoronary peak blood flow velocity in either the left anterior descending or left circumflex artery was measured by continuous Doppler signal recording, heart rate, central aortic blood pressure, and adverse effects were recorded. Regadenoson increased peak blood flow velocity by up to 3.4-fold in a dose-dependent manner. The mean duration of the increase in flow velocity of 2.5-fold or greater caused by 400 to 500 microg of regadenoson was 2.3 to 2.4 minutes. Regadenoson (400-500 microg) increased heart rate by up to 21 +/- 6 beats/min and decreased systolic blood pressure (-5 +/- 8 mm Hg to -24 +/- 16 mm Hg) and diastolic blood pressure (-8 +/- 4 mm Hg to -15 +/- 14 mm Hg). Aminophylline (100 mg) attenuated the increase in peak flow velocity but not tachycardia caused by 400 microg of regadenoson.
The results of this study demonstrate the utility of regadenoson as a coronary vasodilator for myocardial perfusion imaging.
瑞加德松是一种选择性A2A腺苷受体激动剂和血管扩张剂，用于在心肌灌注成像期间增加冠状动脉血流分布的异质性。本研究对瑞加德松诱导的冠状动脉充血的剂量依赖性进行了表征。
对34名受试者进行了一项瑞加德松（10 - 500微克，快速静脉推注）的开放标签、剂量递增研究；在另外4名受试者中，测定了氨茶碱逆转对瑞加德松反应的效果。通过连续多普勒信号记录测量左前降支或左旋支动脉的冠状动脉内峰值血流速度，记录心率、中心主动脉血压和不良反应。瑞加德松以剂量依赖性方式使峰值血流速度增加高达3.4倍。400至500微克瑞加德松引起的流速增加2.5倍或更大的平均持续时间为2.3至2.4分钟。瑞加德松（400 - 500微克）使心率增加高达21±6次/分钟，并使收缩压（-5±8毫米汞柱至-24±16毫米汞柱）和舒张压（-8±4毫米汞柱至-15±14毫米汞柱）降低。氨茶碱（100毫克）减弱了400微克瑞加德松引起的峰值流速增加，但未减弱心动过速。
本研究结果证明了瑞加德松作为心肌灌注成像冠状动脉血管扩张剂的效用。
