Initial clinical experience with regadenoson, a novel selective A2A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging
Initial clinical experience with regadenoson, a novel selective A2A agonist for pharmacologic stress single-photon emission computed tomography myocardial perfusion imaging
复制标题
DOI：
10.1016/j.jacc.2005.05.097
复制
发表时间：
2005-12-06
影响因子：
24
通讯作者：
Mahmarian, JJ
中科院分区：
文献类型：
--
作者：
Hendel, RC;Bateman, TM;Mahmarian, JJ
Regadenoson是一种选择性A（2A）腺苷受体激动剂，当与单光子发射计算机断层扫描（SPECT）结合时，评价其作为检测可逆性心肌灌注不足的药理学应激剂的耐受性和有效性。尽管已被证明的安全性，这些药物往往会导致不良的副作用，需要一个连续的infrations.METHODS这第二阶段，多中心，开放标签的试验进行了36例谁证明缺血6分钟腺苷SPECT成像研究在过去的2至46天。患者接受regadenoson快速静脉推注剂量为400 μ g（n = 18）或500 μ g（n = 18）。放射性药物随后在一分钟内输送。以标准方式采集SPECT图像，并在中心实验室进行统一处理。瑞伽腺苷和腺苷研究以随机顺序呈现，并由三名观察员用17段模型进行盲解。此外，定量分析进行了4D-MSPECT软件（密歇根大学，安阿伯，密歇根州）。400 μ g剂量耐受性更好。总体而言，regadenoson耐受性良好;副作用（例如，胸部不适、潮红、呼吸困难）的严重程度一般为轻度，并具有自限性。高级房室传导阻滞和支气管痉挛没有observed.CONCLUSIONS Regadenoson是耐受性良好，似乎有效的腺苷检测和定量的程度与SPECT灌注成像观察到的低灌注。鉴于regadenoson副作用的减少和推注给药的简单性，III期临床试验正在进行中。
OBJECTIVES Regadenoson, a selective A(2A) adenosine receptor agonist, was evaluated for tolerability and effectiveness as a pharmacological stress agent for detecting reversible myocardial hypoperfusion when combined with single-photon emission computed tomography (SPECT).BACKGROUND Adenosine and dipyridamole are nonselective adenosine agonists currently used as pharmacologic stressors. Despite proven safety, these agents often cause undesirable side effects and require a continuous infusion.METHODS This Phase II, multicenter, open-label trial was conducted in 36 patients who had demonstrated ischemia on a 6-min adenosine SPECT imaging study within the previous 2 to 46 days. Patients received regadenoson as a rapid intravenous bolus dose of 400 mu g (n = 18) or 500 mu g (n = 18). The radiopharmaccutical was then delivered within one minute. The SPECT images were acquired in a standard manner and uniformly processed at a central laboratory. Regadenoson and adenosine studies were presented in random order and interpreted blindly with a 17-segment model by three observers. Additionally, quantitative analysis was performed with 4D-MSPECT software (University of Michigan, Ann Arbor, Michigan).RESULTS Overall agreement for the presence of reversible hypoperfusion was 86%. The 400-mu g dose was better tolerated. Overall, regadenoson was well-tolerated; side effects (e.g., chest discomfort, flushing, dyspnea) were generally mild in severity and self-limiting. High-grade atrioventricular block and bronchospasm were not observed.CONCLUSIONS Regadenoson is well-tolerated and seems as effective as adenosine for detecting and quantifying the extent of hypoperfusion observed with SPECT perfusion imaging. Phase III clinical trials are now underway, given the promise of regadenoson's reduced side effects and simplicity of bolus administration.