Cho Min Chul, Paick Jae-Seung
Department of Urology, Seoul National University Boramae Medical Center, Seoul, Korea.
Department of Urology, Seoul National University College of Medicine, 28, Yongon-Dong, Chongno-Ku, Seoul 110-744, Korea.
Ther Adv Urol. 2016 Apr;8(2):100-17. doi: 10.1177/1756287215625408. Epub 2016 Jan 19.
Erectile dysfunction (ED) is a common disorder that can jeopardize quality of life and the partnership of patients and their sexual partners. The advent of oral phosphodiesterase type 5 inhibitors (PDE5Is) has revolutionized a treatment for ED, and they are recognized as the first-line therapy for ED, regardless of its etiology. Mirodenafil, a second-generation PDE5I, has biochemical profiles such as high affinity for PDE5 and high selectivity for PDE5 over other PDE isoforms, compared to other existing PDE5Is such as sildenafil, vardenafil and tadalafil. Available evidence has suggested that doses of 50 and 100 mg mirodenafil effectively improve ED [with improvements in the erectile function domain of the International Index of Erectile Function (IIEF-EF) scores, positive responses to questions 2 of the Sexual Encounter Profiles (SEP2) and questions 3 of the Sexual Encounter Profiles (SEP3): 7.6-11.6 points, 27.72-38.98% and 44.20-67.33%, respectively] in a broad range of patient populations with ED of a variety of underlying etiologies, severities and ages, without any serious treatment-related adverse effects. In the treatment of diabetic ED, a traditionally difficult-to-treat population, 100 mg mirodenafil has been reported to offer favorable efficacy (with improvements in the IIEF-EF scores, and positive responses to the SEP2 and the SEP3: 9.3 points, 36.1% and 61.8%, respectively) and tolerability (mild adverse effects of less than 19.6%), which are comparable with results from clinical studies on other PDE5Is. Mirodenafil appears to be effective, safe and well tolerated in men with both ED and hypertension or lower urinary tract symptoms (LUTS)/benign prostatic hyperplasia (BPH) who are taking concomitant antihypertensive medications or α1-blockers. Furthermore, recent evidence has indicated that mirodenafil may be a potential option for chronic dosing in the treatment of ED despite its short half-life (T 1/2). Most of the available clinical studies have reported that adverse effects (up to 53.7%) caused by 50 and 100 mg mirodenafil are mild or moderate in severity, with headache (1.8-14.8%) and flushing (6.7-24.1%) being the most common. Due to the pharmacodynamic profiles of mirodenafil, its tolerability is expected to be somewhat better than those of the other PDE5Is. However, further well designed studies with larger cohorts of different ethnicities, flexible dosing schedules and long-term follow up are necessary to confirm the favorable efficacy and tolerability profiles of mirodenafil for the treatment of ED.
勃起功能障碍(ED)是一种常见疾病,会危及患者及其性伴侣的生活质量和伴侣关系。口服5型磷酸二酯酶抑制剂(PDE5Is)的出现彻底改变了ED的治疗方式,无论病因如何,它们都被视为ED的一线治疗药物。与西地那非、伐地那非和他达拉非等其他现有的PDE5Is相比,第二代PDE5I米罗地那非具有对PDE5亲和力高、对PDE5比对其他PDE同工型选择性高的生化特性。现有证据表明,50毫克和100毫克剂量的米罗地那非能有效改善ED(国际勃起功能指数勃起功能领域评分、性接触概况问题2和性接触概况问题3的阳性反应分别改善7.6 - 11.6分、27.72 - 38.98%和44.20 - 67.33%),适用于各种潜在病因、严重程度和年龄的广泛ED患者群体,且无任何严重的治疗相关不良反应。在治疗传统上难以治疗的糖尿病性ED患者时,据报道100毫克米罗地那非具有良好的疗效(国际勃起功能指数勃起功能领域评分、性接触概况问题2和性接触概况问题3的阳性反应分别改善9.3分、36.1%和61.8%)和耐受性(轻度不良反应发生率低于19.6%),与其他PDE5Is的临床研究结果相当。对于同时患有ED和高血压或下尿路症状(LUTS)/良性前列腺增生(BPH)且正在服用抗高血压药物或α1受体阻滞剂的男性,米罗地那非似乎有效、安全且耐受性良好。此外,最近的证据表明,尽管米罗地那非半衰期短(T 1/2),但它可能是治疗ED长期给药的一个潜在选择。大多数现有临床研究报告称,50毫克和100毫克米罗地那非引起的不良反应(高达53.7%)严重程度为轻度或中度。最常见的是头痛(1.8 - 14.8%)和面部潮红(6.7 - 24.1%)。由于米罗地那非的药效学特性,预计其耐受性会比其他PDE5Is略好。然而,需要进一步设计更完善的研究,纳入更大规模不同种族的队列、灵活的给药方案和长期随访,以确认米罗地那非治疗ED的良好疗效和耐受性。