Stehlik Josef, Movsesian Matthew A
University of Utah School of Medicine, Cardiology Section, VA Salt Lake City Healthcare System, 500 Foothill Boulevard, Salt Lake City, UT 84117, USA.
Expert Opin Investig Drugs. 2006 Jul;15(7):733-42. doi: 10.1517/13543784.15.7.733.
Cyclic nucleotide phosphodiesterases (PDE) 3 and 5 regulate cAMP and cGMP signalling in cardiac and smooth muscle myocytes. Important advances in the understanding of the roles of these enzymes have recently been made. PDE3 inhibitors have inotropic and vasodilatory properties, and although they acutely improve haemodynamics in patients with heart failure, they do not improve long-term morbidity and mortality. Although combination therapy with beta-adrenergic receptor antagonists or selective inhibition of specific PDE3 isoforms might result in a more favourable long-term outcome, more clinical data are needed to test this proposition. The role of PDE5 inhibitors in the treatment of cardiac disease is evolving. PDE5 inhibitors cause pulmonary and systemic vasodilation. How these drugs will compare with other vasodilators in terms of long-term outcomes in patients with heart failure is unknown. Recent studies also suggest that PDE5 inhibitors may have antihypertropic effects, exerted through increased myocardial cGMP signalling, that could be of additional benefit in patients with heart failure.
环核苷酸磷酸二酯酶（PDE）3和5调节心肌细胞和平滑肌细胞中的cAMP和cGMP信号传导。最近在理解这些酶的作用方面取得了重要进展。PDE3抑制剂具有正性肌力和血管舒张特性，虽然它们能急性改善心力衰竭患者的血流动力学，但并不能改善长期发病率和死亡率。尽管与β-肾上腺素能受体拮抗剂联合治疗或选择性抑制特定的PDE3亚型可能会带来更有利的长期结果，但仍需要更多临床数据来验证这一观点。PDE5抑制剂在心脏病治疗中的作用正在不断演变。PDE5抑制剂可引起肺血管和全身血管舒张。在心力衰竭患者的长期预后方面，这些药物与其他血管舒张剂相比如何尚不清楚。最近的研究还表明，PDE5抑制剂可能具有抗肥厚作用，通过增加心肌cGMP信号传导发挥作用，这可能对心力衰竭患者有额外益处。
