他达拉非治疗合并心血管疾病的ED患者及对心血管的保护作用

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。

Cardiovascular-protective effect of tadalafil in the treatment of erectile dysfunction

The enzyme phosphodiesterase-5 （PDE-5）, widely distributed in the heart, smooth muscle, and blood vessels, cata- lyzes the hydrolysis of cyclic guanosine monophosphate （cGMP）, a potent vasodilator, and is also a nitric oxide （NO） donor. Tadalafil is the first PDE 5 inhibitor approved by FDA for the treatment of ED. Recent studies have shown several pleiotropic beneficial effects of PDE-5 inhibitors in patients with cardiovascular diseases （coronary heart disease, hypertension, heart failure, and pulmonary arterial hypertension） and diabetes mellitus. It has been demonstrated that tadalafil can not only improve sexual function, but also elevate the endothelial cell-derived NO level, activate protein kinase A, upregulate the intraeellular Ca2 ＋ concentration, and improve hemody- namic indexes. Thus, the PDE-5 inhibitor tadalafil, with its cardiovascular-protective effect, can be a therapeutic option for the treat- ment of ED patients with cardiovascular disease.