Department of Medicine, Einstein Medical Center, Philadelphia, PA; Department of Medicine and Einstein Institute for Heart and Vascular Health, Einstein Medical Center, and Jefferson College of Medicine, Philadelphia, PA.
Rev Cardiovasc Med. 2014;15(2):158-67. doi: 10.3909/ricm0679.
Phosphodiesterase-5 (PDE5) inhibitors have been approved by the US Food and Drug Administration for the treatment of erectile dysfunction and more recently for pulmonary arterial hypertension (World Health Organization functional class I). PDE5 inhibitors can induce vasodilation; in addition, through a complex pathway involving nitric oxide, cyclic guanosine monophosphate, and protein kinase G, it can reduce apoptosis and suppress cell proliferation. The presence of PDE5 inhibitors in various tissues and systemic vasculature make them potential targets in a variety of cardiovascular diseases. In many in vitro and in vivo studies, PDE5 inhibitors have been shown to have positive effects in systolic and diastolic congestive heart failure, ischemic heart disease, doxorubicin cardiomyopathy, and pulmonary arterial hypertension. They also improved vasoconstriction in Raynaud phenomenon, peripheral artery disease, and hypoxic brain conditions. This article reviews the therapeutic potentials of PDE5 inhibitors in different cardiovascular diseases.
磷酸二酯酶-5（PDE5）抑制剂已获美国食品和药物管理局批准用于治疗勃起功能障碍，最近又用于治疗肺动脉高压（世界卫生组织功能分类 I）。PDE5 抑制剂可引起血管舒张；此外，通过涉及一氧化氮、环鸟苷单磷酸和蛋白激酶 G 的复杂途径，它可以减少细胞凋亡并抑制细胞增殖。PDE5 抑制剂存在于各种组织和全身脉管系统中，使它们成为多种心血管疾病的潜在靶点。在许多体外和体内研究中，PDE5 抑制剂已被证明在收缩性和舒张性充血性心力衰竭、缺血性心脏病、多柔比星心肌病和肺动脉高压中具有积极作用。它们还改善了雷诺现象、外周动脉疾病和缺氧性脑疾病中的血管收缩。本文综述了 PDE5 抑制剂在不同心血管疾病中的治疗潜力。
