Rosenkranz Stephan, Caglayan Evren, Erdmann Erland
Klinik III für Innere Medizin, Universität zu Köln, Köln.
Med Klin (Munich). 2007 Aug 15;102(8):617-30. doi: 10.1007/s00063-007-1078-4.
Phosphodiesterase type 5 (PDE5) induces the breakdown of cyclic guanosine monophosphate (cGMP) in smooth muscle cells. Hence, PDE5 inhibitors promote vasodilative effects by enhancing intracellular cGMP levels. Three PDE5 inhibitors, sildenafil, vardenafil, and tadalafil, have been approved for the treatment of "erectile dysfunction" (ED). All three show an excellent effectiveness regarding ED therapy, but differ from one another regarding their pharmacokinetic properties. Recent experimental studies and clinical trials indicate that PDE5 inhibitors are also effective in the treatment of various other diseases such as pulmonary arterial hypertension (PAH), Raynaud's disease, gastrointestinal disorders, and stroke, and furthermore exert cardioprotective effects. This review describes the cardiovascular safety of PDE5 inhibitors and provides an overview of the current literature regarding potential novel indications.
5型磷酸二酯酶（PDE5）可诱导平滑肌细胞中环磷酸鸟苷（cGMP）的分解。因此，PDE5抑制剂通过提高细胞内cGMP水平来促进血管舒张作用。三种PDE5抑制剂，西地那非、伐地那非和他达拉非，已被批准用于治疗“勃起功能障碍”（ED）。这三种药物在ED治疗方面均显示出极佳的疗效，但在药代动力学特性方面彼此不同。最近的实验研究和临床试验表明，PDE5抑制剂在治疗其他各种疾病如肺动脉高压（PAH）、雷诺病、胃肠道疾病和中风方面也有效，并且还具有心脏保护作用。这篇综述描述了PDE5抑制剂的心血管安全性，并概述了有关潜在新适应症的当前文献。
