磷酸二酯酶-5抑制剂在心血管疾病中的新用途不断涌现。
Emerging new uses of phosphodiesterase-5 inhibitors in cardiovascular diseases.
作者信息
Kukreja Rakesh C, Salloum Fadi N, Das Anindita, Koka Saisudha, Ockaili Ramzi A, Xi Lei
机构信息
Department of Internal Medicine, Division of Cardiology, Virginia Commonwealth University Pauley Heart Center, Richmond, Virginia, USA.
出版信息
Exp Clin Cardiol. 2011 Winter;16(4):e30-5.
Phosphodiesterase type-5 (PDE-5) is an enzyme that catalyzes the hydrolytic degradation of cyclic GMP - an essential intracellular second messenger that modulates diverse biological processes in living cells. Three selective inhibitors of PDE-5 - sildenafil, vardenafil and tadalafil - have been successfully used by millions of men worldwide for the treatment of erectile dysfunction. Also, sildenafil and tadalafil are currently approved for the treatment of pulmonary hypertension. Recent powerful basic science data and clinical studies suggest potential nonurological applications of PDE-5 inhibitors, including ischemia/reperfusion injury, myocardial infarction, cardiac hypertrophy, cardiomyopathy, heart failure, stroke, neurodegenerative diseases and other circulatory disorders including Raynaud's phenomenon. Future carefully controlled clinical trials would hopefully expedite their expanding therapeutic use in patients with cardiovascular disease.
5型磷酸二酯酶（PDE-5）是一种催化环磷酸鸟苷水解降解的酶，环磷酸鸟苷是一种重要的细胞内第二信使，可调节活细胞中的多种生物学过程。PDE-5的三种选择性抑制剂——西地那非、伐地那非和他达拉非——已在全球数百万男性中成功用于治疗勃起功能障碍。此外，西地那非和他达拉非目前已被批准用于治疗肺动脉高压。最近强有力的基础科学数据和临床研究表明，PDE-5抑制剂具有潜在的非泌尿学应用，包括缺血/再灌注损伤、心肌梗死、心脏肥大、心肌病、心力衰竭、中风、神经退行性疾病以及包括雷诺现象在内的其他循环系统疾病。未来精心控制的临床试验有望加快它们在心血管疾病患者中的治疗应用扩展。
Zotero 插件