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Cardiovascular effects of phosphodiesterase type 5 inhibitors.

机译:磷酸二酯酶5型抑制剂的心血管作用。

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INTRODUCTION: Phosphodiesterase type 5 (PDE5) inhibitors are widely used as first-line therapy for erectile dysfunction (ED). Their efficacy and safety combined with an increasing understanding of cyclic guanosine monophosphate (cGMP)-regulated mechanisms have triggered a number of attempts to determine their effects on the cardiovascular system and their potential benefits in cardiovascular conditions. AIM: To review and discuss recent findings regarding the cardiovascular effects of PDE5 inhibitors and to highlight current and future clinical applications beyond ED. MAIN OUTCOME MEASURES: Results of preclinical and clinical studies evaluating the cardiovascular effects of PDE5 inhibitors are analyzed and critically put into perspective. METHODS: Extensive PubMed literature search reviewing relevant data on effects and mechanisms of PDE5 inhibitors on the cardiovascular system. RESULTS: In recent years, extensive but very heterogeneous preclinical and clinical evidence has been reported. PDE5 inhibition has proven collateral benefits for a multitude of risk factors or diseases associated with or accompanying ED. However, these agents appear to have the potential of expanding their indications. To date, PDE5 inhibition has been shown to be effective for the treatment of idiopathic pulmonary artery hypertension, and sildenafil is approved for this indication. Importantly, accumulating data show that the therapeutic potential extends to the myocardium, the coronary and peripheral arteries, subliclinical inflammation, oxidative stress, thrombosis, neurological recovery, and pathways of fibrosis. Thus, the spectrum of patients who may benefit has expanded to include, for instance, patients with heart failure or coronary artery disease. CONCLUSIONS: PDE5 inhibitors are an exciting class of drugs with pleiotropic effects. Current or future PDE5 inhibitors are a conceptually attractive therapeutic strategy with potential clinical applications in a variety of cardiovascular conditions.
机译:简介:5型磷酸二酯酶(PDE5)抑制剂被广泛用作勃起功能障碍(ED)的一线治疗。它们的功效和安全性以及对环鸟苷一磷酸(cGMP)调控机制的日益深入的了解引发了许多尝试,以确定它们对心血管系统的影响以及它们在心血管疾病中的潜在益处。目的:回顾和讨论有关PDE5抑制剂对心血管作用的最新发现,并强调除ED以外的当前和未来临床应用。主要观察指标:对评估PDE5抑制剂的心血管作用的临床前和临床研究结果进行分析,并进行了严格的展望。方法:广泛的PubMed文献检索,回顾了有关PDE5抑制剂对心血管系统的作用和机制的相关数据。结果:近年来,已报道了广泛但非常不同的临床前和临床证据。事实证明,抑制PDE5对于与ED相关或伴随的多种危险因素或疾病具有附带益处。但是,这些药物似乎有扩大其适应症的潜力。迄今为止,已显示抑制PDE5可有效治疗特发性肺动脉高压,西地那非已被批准用于该适应症。重要的是,积累的数据表明,治疗潜力扩展到了心肌,冠状动脉和外周动脉,亚临床炎症,氧化应激,血栓形成,神经恢复和纤维化途径。因此,可能受益的患者范围已经扩大到包括例如患有心力衰竭或冠状动脉疾病的患者。结论:PDE5抑制剂是一类令人兴奋的具有多效作用的药物。当前或将来的PDE5抑制剂是一种在概念上具有吸引力的治疗策略,在各种心血管疾病中都有潜在的临床应用。

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