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磷酸二酯酶5(PDE5)广泛分布于心脏、血管、平滑肌等组织器官,可催化环磷酸鸟苷(cGMP)水解产生血管扩张效应,同时也是一氧化氮(NO)的供体物质。他达拉非是首个获的FDA批准用于治疗勃起功能障碍(ED)的PDE 5抑制剂类药物,可选择性抑制PDE5。多个临床研究显示,对于合并心血管疾病(冠心病、高血压、慢性心脏衰竭、肺动脉高压)、糖尿病等疾病的ED患者,他达拉非不仅可以改善ED症状,同时可通过改善血管内皮细胞功能、增加内皮细胞源性NO水平、激活心肌细胞蛋白激酶A,上调细胞内钙离子浓度及改善血流动力学指标等作用,发挥其对ED患者的心血管保护作用,改善ED患者的生存质量。因此,他达拉非等PDE 5抑制剂类药物可作为合并心血管疾病的ED患者治疗用药选择之一。
Phosphodiesterase 5 (PDE5) is widely distributed in the heart, blood vessels, smooth muscle and other tissues and organs. It catalyzes the hydrolysis of cGMP to produce vasodilator effect and is also the donor of nitric oxide (NO). Tadalafil is the first PDE 5 inhibitor approved by the FDA for the treatment of erectile dysfunction (ED) and selectively inhibits PDE5. Several clinical studies have shown that tadalafil can not only improve the symptoms of ED in ED patients with cardiovascular diseases (coronary heart disease, hypertension, chronic heart failure, pulmonary hypertension) and diabetes mellitus, but also improve ED symptoms by improving vascular endothelial cells Function, increase the level of endothelial cell-derived nitric oxide, activate protein kinase A in cardiomyocytes, upregulate the concentration of intracellular calcium and improve the hemodynamic parameters, exert its cardiovascular protective effect on ED patients and improve the quality of life in ED patients . Therefore, PDT-5 inhibitors such as tadalafil can be used as one of the treatment options for ED patients with cardiovascular diseases.