Clinical application of highly selective α1A-AR antagonist silodosin in benign prostatic hyperplasia
NA Yan-qun
Peking University People's Hospital, Peking University Shougang Hospital, Wujieping Urology Medical Center of Peking University,
Department of Urology, Beijing 100144, China
Abstract:Objective: To review the application and the latest development of silodosin which is a highly selective α1A-AR antagonist in the treatment of benign prostatic hyperplasia (BPH). Methods: Multiple databases were searched for the term ‘‘silodosin’’, and a systematic analysis was conducted to review the pharmacological characteristics and the clinical application of silodosin. Results and conclusion: Silodosin has a much higher selectivity to α1A-AR subtype than α1B-AR subtype. Silodosin can improve the BPH patients’ international prostate symptom score (IPSS) and maximum flow rate (Qmax) rapidly. Silodosin is generally well tolerated and is associated with minimal cardiovascular adverse effects. Silodosin provides a new therapeutic selection to improve lower urinary tract symptoms (LUTS) and quality of life of BPH patients.
[1] Parsons J K. Commentary on BPH and public health-have we lost the forest through the trees?[J]. J Urol, 2008, 179(5 Suppl): S81.
[2] 那彦群, 叶章群, 孙颖浩, 等. 中国泌尿外科疾病诊断治疗指南[M]. 北京:人民卫生出版社, 2014:245-266.
[3] Abrams P, Cardozo L, Fall M, et al. The standardisation of terminology of lower urinary tract function: report from the standardisation sub-committee of the international continence society[J].Am J Obstet Gynecol, 2002, 187(1): 116-126.
[4] Nickel J C, Mendez-Probst C E, Whelan T F, et al. 2010 Update:Guidelines for the management of benign prostatic hyperplasia[J].Can Urol Assoc J, 2010, 4(5): 310-316.
[5] Lepor H, Kazzazi A, Djavan B. α-blockers for benign prostatic hyperplasia: the new era[J]. Curr Opin Urol, 2012, 22(1): 7-15.
[6] Guimaraes S, Moura D. Vascular adrenoceptors: an update[J].Pharmacol Rev, 2001, 53(2): 319-356.
[7] Michel M C. The pharmacological profile of the α1A-adrenoceptor antagonist silodosin[J]. Eur Urol Suppl, 2010, 9(4): 486-490.
[8] Roehrborn C G, Schwinn D A. Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia[J]. J Urol, 2004,171(3): 1029-1035.
[9] Yoshida M, Homma Y, Kawabe K. Silodosin, a novel selective α1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia[J]. Expert Opin Investig Drugs, 2007,16(12):1955-1965.
[10] Murata S, Taniguchi T, Takahashi M, et al. Tissue selectivity of KMD-3213, an alpha(1)-adrenoreceptor antagonist, in human prostate and vasculature[J]. J Urol, 2000, 164(2): 578-583.
[11] Shibata K, Foglar R, Horie K, et al. KMD-3213, a novel, potent, α1Aadrenoceptor-selective antagonist: characterization using recombinant human α1-adrenoceptors and native tissues[J]. Mol Pharmacol,1995, 48(2): 250-258.
[12] Morishima S, Suzuki F, Nishimune A, et al. Visualization and tissue distribution of α1L-adrenoceptor in human prostate by the fluorescently labeled ligand Alexa-488-silodosin[J]. J Urol, 2010,183(2): 812-819.
[13] Tatemichi S, Kobayashi K, Maezawa A, et al. α1-adrenoceptor subtype selectivity and organ specificity of silodosin (KMD-3213) [J].Yakugaku Zasshi ,2006, 126:209-216.
[14] Yamada S, Okura T, Kimura R. In vivo demonstration of α1Aadrenoceptor subtype selectivity of KMD-3213 in rat tis sues[J].J Pharmacol Exp Ther, 2001, 296(1): 160-167.
[15] Watson Laboratories Inc. US prescribing information: Rapaflo?(Silodosin) [EB/OL].(2014-04-07)[2014-11-02]. http://www.watson.com
[16] European Medicines Agency. Summary of product characteristics:Urorec? (Silodosin) [EB/OL].(2014-10-08)[2014-11-02]. http://www.ema.europa.eu.
[17] Daiichi Sankyo (China) Holdings Co., LTD. China Package Insert information: Urief? (Silodosin) [EB/OL].(2014-10-02)[2014-11-02].http://www. daiichisankyo.com.cn
[18] Kawabe K, Yoshida M, Homma Y, et al. Silodosin, a new alpha1Aadrenoceptor-selective antagonist for treating benign prostatic hyperplasia: results of a phase III randomized, placebo-controlled,double-blind study in Japanese men[J]. BJU Int, 2006, 98(5):1019-1024.
[19] Marks L S, Gittelman M C, Hill L A, et al. Rapid efficacy of the highly selective α1A-adrenoceptor antagonist silodosin in men with signs and symptoms of benign prostatic hyperplasia: pooled results of 2 phase 3 studies[J]. J Urol, 2013, 189(1 Suppl): S122-128.
[20] Chapple C R, Montorsi F, Tammela T L, et al. Silodosin therapy for lower urinary tract symptoms in men with suspected benign prostatic hyperplasia: results of an international, randomized, double-blind,placebo- and active-controlled clinical trial performed in Europe[J].Eur Urol, 2011, 59(3): 342-352.
[21] 李宁忱, 宋毅, 丁强, 等. 赛洛多辛治疗良性前列腺增生的随机双盲安慰剂对照多中心III 期临床研究[J]. 中华泌尿外科杂志,2013, 34(4): 305-309.
[22] Miyakita H, Yokoyama E, Onodera Y, et al. Short-term effects of crossover treatment with silodosin and tamsulosin hydrochloride for lower urinary tract symptoms associated with benign prostatic hyperplasia[J]. Int J Urol, 2010, 17(10): 869-875.
[23] Moon K H, Song P H, Yang D Y, et al. Efficacy and safety of the selective α1A-Adrenoceptor blocker silodosin for severe lower urinary tract symptoms associated with benign prostatic hyperplasia:a prospective, single-open-aabel, multicenter study in Korea[J].Korean J Urol, 2014, 55(5): 335-340.
[24] Kaplan S A, Roehrborn C G, Hill L A, et al. Effect of estimated prostate volume on silodosin-mediated improvements in the signs and symptoms of BPH: does prostate size matter?[J]. Open Access J Urol, 2011, 3:89-93.
[25] Takao T, Tsujimura A, Kiuchi H, et al. Improvement of nocturia and sleep disturbance by silodosin in male patients with lower urinary tract symptoms[J]. Int J Urol, 2015, 22(2):236-238.
[26] Kim T N, Nam J K, Lee K S, et al. Reasons for prescription change of α1-blockers in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia[J]. Urology, 2014, 84(2): 427-432.
[27] Lepor H, Hill L A. Silodosin for the treatment of benign prostatic hyperplasia: pharmacology and cardiovascular tolerability[J].Pharmacotherapy, 2010, 30(12): 1303-1312.
[28] Yu H J, Lin A T, Yang S S, et al. Non-inferiority of silodosin to tamsulosin in treating patients with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH)[J]. BJU Int, 2011, 108(11):1843-1848.
[29] Chapple C R, Montorsi F, Tammela T L, et al. Silodosin therapy for lower urinary tract symptoms in men with suspected benign prostatic hyperplasia: results of an international, randomized, double-blind,placebo- and active-controlled clinical trial performed in Europe[J].Eur Urol, 2011, 59(3): 342-352.
[30] Kalplan S A. Side effect of α-blocker use: retrograde ejaculation[J].Rev Urol, 2009, 11(1): S14-18.
[31] Gacci M, Ficarra V, Sebastianelli A, et al. Impact of medical treatments for male lower urinary tract symptoms due to benign prostatic hyperplasia on ejaculatory function: a systematic review and meta-analysis[J]. J Sex Med, 2014, 11(6):1554-1566.