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罗氟司特:一种用于治疗心力衰竭的选择性腺苷A1受体拮抗剂。

Rolofylline: a selective adenosine 1 receptor antagonist for the treatment of heart failure.

作者信息

Slawsky Mara T, Givertz Michael M

机构信息

Tufts University School of Medicine, Baystate Medical Center, Division of Cardiology, Springfield, MA (MTS), USA.

出版信息

Expert Opin Pharmacother. 2009 Feb;10(2):311-22. doi: 10.1517/14656560802682213.

DOI:10.1517/14656560802682213
PMID:19236201
Abstract

BACKGROUND

Co-existent cardiac and renal dysfunction is increasingly recognized as both a predictor and mediator of poor outcomes in patients with advanced heart failure. Novel therapies, including adenosine receptor antagonists, are currently under development for the treatment of 'cardiorenal syndrome'.

OBJECTIVES

To review the pathophysiologic rationale for using rolofylline, a selective adenosine 1 receptor antagonist, in patients with cardiorenal syndrome; and to provide a critical overview of safety and efficacy data from clinical studies.

METHODS

We reviewed published data on the pharmacology of rolofylline, and used this to inform a comprehensive summary of preclinical and clinical trials. Cardiac and renal effects, and safety data with a particular reference to seizures, are highlighted.

RESULTS/CONCLUSION: Rolofylline facilitates diuresis and preserves renal function in patients with acute decompensated heart failure and renal dysfunction. Pilot data also suggest beneficial effects on symptoms and short-term outcomes. The risk of seizures may be minimized by excluding high-risk patients.

摘要

背景

心脏和肾脏功能障碍并存日益被认为是晚期心力衰竭患者不良预后的预测因素和介导因素。包括腺苷受体拮抗剂在内的新型疗法目前正在研发用于治疗“心肾综合征”。

目的

综述在患有心肾综合征的患者中使用选择性腺苷A1受体拮抗剂罗氟司特的病理生理依据;并对临床研究的安全性和有效性数据进行批判性概述。

方法

我们回顾了已发表的关于罗氟司特药理学的数据,并以此为基础对临床前和临床试验进行全面总结。重点介绍了心脏和肾脏效应以及特别提及癫痫发作的安全性数据。

结果/结论:罗氟司特可促进急性失代偿性心力衰竭和肾功能不全患者的利尿并保护肾功能。初步数据还表明对症状和短期预后有有益影响。通过排除高危患者,癫痫发作风险可降至最低。

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Rolofylline: a selective adenosine 1 receptor antagonist for the treatment of heart failure.罗氟司特:一种用于治疗心力衰竭的选择性腺苷A1受体拮抗剂。
Expert Opin Pharmacother. 2009 Feb;10(2):311-22. doi: 10.1517/14656560802682213.
2
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