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The pleiotropic effects of phosphodiesterase 5 inhibitors on function and safety in patients with cardiovascular disease and hypertension

机译:磷酸二酯酶5抑制剂对心血管疾病和高血压患者功能和安全性的多效性

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Phosphodiesterase 5 (PDE-5) inhibitors are selective blockers of PDE-5, which catalyzes the hydrolysis of cyclic guanosine monophosphate (cGMP) to its corresponding monophosphates. cGMP is a potent vasodilator and nitric oxide donor. Since PDE-5 is widely distributed in the body, it was hypothesized that inhibition of its actions could lead to significant vasodilation, which could benefit patients with coronary artery disease. This hypothesis led to the development of PDE-5 inhibitors, the first being sildenafil citrate. Studies of sildenafil in patients with coronary artery disease demonstrated a modest cardiovascular effect but a potent action on penile erection in men, resulting in sildenafil becoming first-line treatment of erectile dysfunction. Two more PDE-5 inhibitors are now US Food and Drug Administration-approved (vardenafil and tadalafil) for the treatment of erectile dysfunction. Recent studies have demonstrated several beneficial pleiotropic cardiovascular effects of PDE-5 inhibitors in patients with erectile dysfunction and multiple comorbidities, including coronary artery disease, heart failure, hypertension, and diabetes mellitus. Treatment of these conditions with PDE-5 inhibitors has been very effective, safe, and well tolerated. Drug interactions have been minimal with the exception of nitrates, where coadministration may result in severe vasodilation and hypotension. These beneficial pleiotropic and safe cardiovascular effects of PDE-5 inhibitors will be discussed in this concise review.
机译:磷酸二酯酶5(PDE-5)抑制剂是PDE-5的选择性阻滞剂,可催化环鸟苷单磷酸酯(cGMP)水解为其相应的单磷酸酯。 cGMP是有效的血管扩张剂和一氧化氮供体。由于PDE-5在人体中广泛分布,因此假设抑制其作用可能导致明显的血管舒张,从而使冠心病患者受益。该假设导致了PDE-5抑制剂的开发,第一个是柠檬酸西地那非。西地那非在冠心病患者中的研究显​​示出适度的心血管作用,但对男性的阴茎勃起有有效作用,导致西地那非成为勃起功能障碍的一线治疗。现在,另外两种PDE-5抑制剂已获得美国食品和药物管理局(vardenafil和tadalafil)的批准,用于治疗勃起功能障碍。最近的研究表明,PDE-5抑制剂对勃起功能障碍和多种合并症的患者具有多种有益的多效性心血管作用,包括冠心病,心力衰竭,高血压和糖尿病。用PDE-5抑制剂治疗这些疾病非常有效,安全且耐受性良好。除硝酸盐外,药物的相互作用极少,在硝酸盐中共同给药可能导致严重的血管扩张和低血压。这篇简明的综述将讨论PDE-5抑制剂的这些有益多效性和安全心血管作用。

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