a Department of Pharmacology, Faculty of Medical Sciences , University of Campinas , Campinas , Sao Paulo , Brazil.
Expert Opin Pharmacother. 2019 Jun;20(8):929-937. doi: 10.1080/14656566.2019.1589452. Epub 2019 Mar 22.
In men, lower urinary tract symptoms (LUTS) are primarily attributed to benign prostatic hyperplasia (BPH). Therapeutic options are targeted to relax prostate smooth muscle and/or reduce prostate enlargement. Areas covered: This article reviews the major preclinical and clinical data on PDE5 inhibitors with a specific focus on tadalafil. It includes details of the role of the nitric oxide (NO)-cyclic guanosine monophosphate (cGMP) - PDE5 pathway in the LUT organs (bladder and prostate) in addition to the available data on tadalafil in patients with LUTS secondary to BPH with or without erectile dysfunction (ED). Expert opinion: Preclinical and clinical data have clearly demonstrated that PDE5 inhibitors induce bladder and prostate relaxation, which contributes to the improvement seen in storage symptoms in both animal models of bladder and prostate hypercontractility. Tadalafil is effective both as a monotherapy and add-on therapy in patients with LUTS secondary to BPH. Furthermore, as LUTS-BPH and ED are urological disorders that commonly coexist in aging men, tadalafil is more advantageous than α1-adrenoceptors and should be used as the first option. Tadalafil is a safe and tolerable therapy and unlike α1- adrenoceptors and 5-alpha reductase inhibitors, which can cause sexual dysfunctions, tadalafil improves sexual function.
在男性中，下尿路症状（LUTS）主要归因于良性前列腺增生（BPH）。治疗选择旨在放松前列腺平滑肌和/或减少前列腺增大。
本文综述了 PDE5 抑制剂的主要临床前和临床数据，特别关注他达拉非。它包括了一氧化氮（NO）-环鸟苷单磷酸（cGMP）-PDE5 途径在 LUT 器官（膀胱和前列腺）中的作用的详细信息，以及关于他达拉非在伴有或不伴有勃起功能障碍（ED）的 BPH 继发 LUTS 患者中的可用数据。
临床前和临床数据清楚地表明，PDE5 抑制剂可诱导膀胱和前列腺松弛，这有助于改善膀胱和前列腺高收缩性动物模型中的储存症状。他达拉非作为单一疗法和附加疗法在 BPH 继发 LUTS 患者中均有效。此外，由于 LUTS-BPH 和 ED 是常见于老年男性的泌尿科疾病，他达拉非比α1-肾上腺素受体更具优势，应作为首选。他达拉非是一种安全且耐受良好的治疗方法，与α1-肾上腺素受体和 5-α 还原酶抑制剂不同，后者会引起性功能障碍，他达拉非可改善性功能。
