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【名称】
通用名：西洛多辛  
英文名：Silodosin
【适 应 症】
是一种α1-肾上腺素受体拮抗剂，对与良性前列腺增生有关的排尿障碍有疗效。
Silodosin是日本Kissei制药公司发明的α1－受体拮抗剂，可用于治疗与良性前列腺增生（BPH）或肥大相关的症状。
Kissei公司与Daiichi Sankyo公司合作申请，已于2006年5月在日本获得上市批准，使用的商品名是Urief（R）。
【药 效 学】
西洛辛为选择性α1A-肾上腺能阻滞剂，临床前研究表明，其对尿道的选择性效应分别较哌唑嗪(prazosin)和坦洛辛高12和7.5倍。西洛辛能明显抑制去甲肾上腺素引起的人前列腺收缩；对大鼠良性前列腺肥大模型的膀胱活动亢进有剂量依赖性的抑制作用，并能提高膀胱收缩的压力阈值。
这些数据提示，西洛辛除可改善膀胱功能外，对缓解良性前列腺肥大相关症状也有效。
良性前列腺增生（BPH）是老年男性常见病之一，以前列腺的非恶性增大为特征。在60岁或以上的老年人中有50%以上患有此症，而在85岁及以上的老年人中有90%以上者发病。其发病原因尚未阐明，一般认为与性激素和胆固醇等的分泌、代谢失调有关。
有人认为，老年人因垂体－促性腺激素－睾丸的作用途径减弱或因内源性变化，使睾丸退化、性机能下降、睾酮值降低、前列腺因结缔组织增多，使腺上皮改变、前列腺增大。前列腺的增大会压迫尿道，导致膀胱尿流不畅，甚至堵塞膀胱出口。在人类前列腺中存在α1A-肾上腺素受体，该受体的激活会加重尿道梗阻和排尿困难症状。因此，通过阻断α1A-肾上腺素受体的结合，可使梗阻的前列腺平滑肌松弛，从而改善症状。
【临床研究】 
在对药物与α1受体的结合程度进行评估时，采用了有关Silodosin与人和大鼠体内前列腺α1受体结合的有关参数。结果表明，口服用药0.5～6小时后，被药物结合的α1受体比率在60%～90%范围内，24小时后降为40%。
与同类药物哌唑嗪和坦索罗辛不同，Silodosin（赛洛多辛）对位于前列腺和膀胱颈的α1A－受体有高度选择性，而对α1B－和α1D－受体的亲和力不明显。
它阻滞这部位的α1A－受体，松弛平滑肌，导致尿流速改善和BPH症状减轻。
Silodosin对α1A－受体的选择性结合较对心血管相关的α1B－受体的选择性大，从而使对目标器官的活性最大化，而对血压的潜在影响最小化。多中心、随机双盲、安慰剂对照的Ⅲ期临床试验，923例BPH患者每天1次口服8mg本品，12周。主要终点以国际前列腺症状分（IPSS）测定，与安慰剂组比较，BPH症状显著改善。次要终点包括尿流速和生活质量的改善也明显。在2项研究中发生率大于2％的最常见副作用是射精（精液）减少和眩晕。

 

Description

This medicine lowers internal pressure of the urethra by blocking α1A -receptors in the urethra and prostate gland, and consequently improves dysuria associated with prostatic hyperplasia.It is usually used in the treatment of dysuria associated with prostatic hyperplasia.

Presentation

50 tablets

Feature

white to faintly yellowish white oval tablet, major axis: 11.0 mm, minor axis: 6.0 mm, thickness: 3.7 mm

Active Ingredients

Silodosin 4mg

Effect/Efficacy

This medicine lowers internal pressure of the urethra by blocking α1A -receptors in the urethra and prostate gland, and consequently improves dysuria associated with prostatic hyperplasia.It is usually used in the treatment of dysuria associated with prostatic hyperplasia.

Usage/Dosage

Cautions

If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you have: orthostatic hypotension, hepatic dysfunction or renal dysfunction.
If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.)

Contraindication

The most commonly reported adverse reactions include ejaculation disorder (retrograde ejaculation), thirst, diarrhea, loose stools, dizziness on standing up, nasal congestion, dizziness, light-headedness and headache. If any of these symptoms occur, consult with your doctor or pharmacist.
The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately.
decreased blood pressure, fainting, loss of consciousness  [faint, loss of consciousness]
general malaise, loss of appetite, yellowing in skin and white of eyes  [hepatic dysfunction, jaundice]
The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above.