Yoshida Masaki, Homma Yukio, Kawabe Kazuki
Graduate School of Kumamoto University, Department of Urology, Graduate School of Medical Sciences, Honjo, Kumamoto 860-8556, Japan.
Expert Opin Investig Drugs. 2007 Dec;16(12):1955-65. doi: 10.1517/13543784.16.12.1955.
Silodosin is a novel selective alpha(1A)-adrenoceptor (AR) antagonist generated by Kissei Pharmaceutical Co. Ltd. This drug selectively binds to alpha(1A)-AR, which is widely distributed in the prostate, urethra and bladder trigone, involved in their contraction, located at the lower urinary tract. This high selectivity for alpha(1A)-AR contributes to inhibition of sympathetic nerve stimulation and relaxation of smooth muscle tone of the lower urinary tract tissues, resulting in suppression of increase in intraurethral pressure. Clinical data suggested that silodosin showed significant improvement in lower urinary tract symptoms associated with benign prostatic hyperplasia, as well as in quality of life. The improvements were observed in both voiding and storage symptoms. In addition, the clinical effects occurred in the early treatment phase, and were observed not only in mild cases, but also in cases with severe symptoms. Long-term study revealed that the efficacy and safety was sustained for 1 year. Although silodosin showed relatively high incidence rate of abnormal ejaculation, the adverse events associated with lowering of blood pressure were low. This article reviews preclinical and clinical data of silodosin, and introduces the usefulness of the drug for treatment of benign prostatic hyperplasia patients.
西洛多辛是由日本积水化学工业株式会社研发的一种新型选择性α(1A)-肾上腺素能受体（AR）拮抗剂。该药物选择性地与α(1A)-AR结合，α(1A)-AR广泛分布于前列腺、尿道和膀胱三角区，参与这些部位的收缩，位于下尿路。对α(1A)-AR的这种高选择性有助于抑制交感神经刺激并松弛下尿路组织的平滑肌张力，从而抑制尿道内压升高。临床数据表明，西洛多辛在与良性前列腺增生相关的下尿路症状以及生活质量方面均有显著改善。排尿和储尿症状均有改善。此外，临床疗效在治疗早期即出现，不仅在轻症患者中可见，在重症患者中也可观察到。长期研究表明，其疗效和安全性可持续1年。尽管西洛多辛的异常射精发生率相对较高，但与血压降低相关的不良事件较少。本文综述了西洛多辛的临床前和临床数据，并介绍了该药物对良性前列腺增生患者的治疗作用。
