Adis, a Wolters Kluwer Business, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand.
Drugs. 2011 May 7;71(7):897-907. doi: 10.2165/11204780-000000000-00000.
Silodosin is an α-adrenoceptor antagonist with high selectivity for α(1A)- relative to α(1B)- adrenoceptors. In men aged >50 years with benign prostatic hyperplasia (BPH), silodosin 8 mg once daily, compared with placebo, was associated with a significantly more rapid and effective improvement in the total International Prostate Symptom Score (IPSS) and the storage and voiding IPSS subscores in three 12-week, phase III trials conducted in Europe and the US. In the European trial, silodosin was at least as effective as tamsulosin 0.4 mg once daily in improving the total IPSS. Silodosin was significantly more effective than placebo (all three phase III trials) and tamsulosin (European phase III trial) in simultaneously improving nocturia, frequency and incomplete emptying, according to a post hoc analysis. Long-term, open-label extension trials demonstrated that silodosin provided sustained relief of the signs and symptoms of BPH for up to 1 year. Silodosin was generally well tolerated, and was associated with minimal cardiovascular adverse effects. Abnormal ejaculation, a class effect of α(1A)-adrenoceptor antagonists, was the most common silodosin-associated adverse reaction, but resulted in treatment withdrawal of only a limited number of patients.
西洛多辛是一种高选择性α1A-肾上腺素受体拮抗剂，对α1B-肾上腺素受体的选择性相对较高。在年龄>50 岁的男性良性前列腺增生（BPH）患者中，与安慰剂相比，西洛多辛 8mg 每日 1 次治疗可显著更快和更有效地改善总国际前列腺症状评分（IPSS）以及储存和排尿 IPSS 亚评分，这在欧洲和美国进行的三项为期 12 周的 III 期临床试验中得到证实。在欧洲试验中，西洛多辛在改善总 IPSS 方面至少与坦索罗辛 0.4mg 每日 1 次等效。根据事后分析，西洛多辛在同时改善夜间尿频、频率和不完全排空方面比安慰剂（所有三项 III 期试验）和坦索罗辛（欧洲 III 期试验）更有效。长期、开放性扩展试验表明，西洛多辛可提供长达 1 年的持续缓解 BPH 的体征和症状。西洛多辛总体上具有良好的耐受性，且与最小的心血管不良事件相关。异常射精是α1A-肾上腺素受体拮抗剂的一种常见的类效应，是西洛多辛最常见的不良反应，但仅有少数患者因该不良反应而停药。
