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雷加曲班

Regadenoson.

作者信息

Bengalorkar G M, Bhuvana K, Sarala N, Kumar T N

机构信息

Department of Pharmacology, Sri Devaraj Urs Medical College, Tamaka, Kolar, Karnataka, India.

出版信息

J Postgrad Med. 2012 Apr-Jun;58(2):140-6. doi: 10.4103/0022-3859.97177.

Abstract

Single-photon emission computerized tomography for myocardial perfusion imaging (MPI) is a non-invasive technique. MPI is performed by subjecting the patient to exercise or by using a pharmacological stress agent. Regadenoson is a selective A 2A adenosine receptor agonist used when MPI with exercise is contraindicated. It binds to the A 2A receptor and stimulates adenylate cyclase, resulting in increased cAMP, which phosphorylates protein kinase A thereby opening the ATP-dependant potassium channels leading to hyperpolarization in the coronary vascular smooth muscle. After a single bolus dose of regadenoson 400 μg, a peak plasma concentration (C max) of 13.6 ng/mL is attained in 1-4 min, with a terminal half-life of 2 h. It has a quick onset, short duration sufficient enough for hyperemic response, with comparable efficacy to adenosine, but with fewer side-effects. The adverse effects of this drug are dyspnea, headache, flushing, chest pain and atrioventricular block. Regadenoson is used for MPI in patients with co-morbid conditions like mild-to-moderate reactive airway disease, obstructive lung disease and renal impairment.

摘要

用于心肌灌注成像(MPI)的单光子发射计算机断层扫描是一种非侵入性技术。MPI通过让患者进行运动或使用药物应激剂来进行。瑞加德松是一种选择性A2A腺苷受体激动剂,当运动MPI禁忌时使用。它与A2A受体结合并刺激腺苷酸环化酶,导致环磷酸腺苷(cAMP)增加,cAMP使蛋白激酶A磷酸化,从而打开ATP依赖性钾通道,导致冠状血管平滑肌超极化。单次静脉推注400μg瑞加德松后,1 - 4分钟内可达到13.6 ng/mL的血浆峰浓度(Cmax),终末半衰期为2小时。它起效迅速,持续时间短,足以产生充血反应,疗效与腺苷相当,但副作用较少。该药物的不良反应有呼吸困难、头痛、潮红、胸痛和房室传导阻滞。瑞加德松用于患有轻度至中度反应性气道疾病、阻塞性肺病和肾功能损害等合并症的患者的MPI检查。

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