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 详细处方信息以本药内容附件PDF文件（201471418344120.pdf）的“原文Priscribing Information”为准
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 部分中文曲司氯铵处方资料（仅供参考）

分类名称
一级分类：泌尿系统药物 二级分类：其他
 
药品英文名
Trospium
 
药品别名
盐酸曲司氯铵、Trospium Hydrochloride、Sanctura
 
药物剂型
盐酸曲司氯铵片剂：20mg/片。20～25℃室温保存。
 
药理作用
本品为季铵盐化合物，具有抗胆碱作用和解痉作用。本品作用于胆碱能神经所支配效应器上的M受体，能拮抗乙酰胆碱对M受体的作用。其副交感神经阻滞作用可引起膀胱平滑肌的舒张，使膀胱容量增加。治疗剂量下，本品对烟碱受体作用微弱。
 
药动学
本品口服后吸收率不足10%，平均生物利用度9.6%。给药后5～6h血药浓度达峰值(Cmax)，给药剂量从20mg增加到40mg和60mg，Cmax分别增加3倍和4倍。药时曲线下面积(AUC)随剂量呈线性变化。高脂饮食可使本品的AUC和Cmax降低70%～80%。体外研究显示，0.5～50ng/ml浓度范围内，本品血浆蛋白结合率50%～85%，本品主要分布在血浆，口服20mg的表观分布容积为395L。本品可能通过水解作用与葡萄糖醛酸结合，代谢产物占排出物的40%。本品消除半衰期约20h，85.2%经粪便排出，5.8%经肾脏排出，肾脏排出物的60%为原形药物。本品的肾脏排泄主要经肾小管分泌，严重肾功能不全患者的AUC和Cmax分别提高4.5倍和2倍，半衰期延长至33h。肝功能轻度至中度异常患者的Cmax分别升高12%和63%。
 
适应证
本品用于膀胱过度刺激引起的尿频、尿急、尿失禁。
 
禁忌证
1.对本品及其中成分过敏者禁用。
2.尿潴留、胃潴留及未控制的闭角型青光眼患者禁用。
 
注意事项
1.儿童用药安全性尚未评价。
2.本品过量可引起严重抗胆碱作用，有过量后引起瞳孔散大和心动过速的病例。出现药物过量应采取对症治疗和支持治疗，并监测心电图。
3.慎用：(1)由于尿潴留的可能，有明显膀胱尿道阻塞症状的患者使用时应谨慎。(2)本品具有抗胆碱作用，能降低胃肠道动力，胃肠道阻塞性疾病患者有胃潴留的可能，使用时应谨慎。严重便秘、溃疡性结肠炎和重症肌无力患者慎用。(3)中度至重度肝功能不全患者慎用。(4)只有当可能的受益高于危险时，方可在严密监护下用于已控制的闭角型青光眼患者。(5)本品生殖毒性分级为C，只有对母体的益处高于对胎儿的危险时方可用于孕妇。(6)本品可经大鼠乳汁分泌，尚不知本品是否经人乳汁分泌，只有当可能的受益高于对新生儿的危险时方可用于哺乳期妇女。
 
不良反应
本品最常见的不良反应为便秘、口干。其他不良反应包括以下几方面。
1.消化系统：口干、便秘、腹痛加剧、便秘加重、消化不良、胃肠胀气、呕吐、味觉障碍、咽干、胃炎。
2.泌尿生殖系统：尿潴留。
3.神经系统：头痛、晕厥、幻觉、躁狂。
4.全身：无力、胸痛。
5.代谢及营养疾病：有血管神经性水肿的报道。
6.心血管系统：心动过速、心悸、室上性心动过速、高血压危象。
7.皮肤：皮肤干燥、渗出性多形性红斑、过敏反应。
8.其他：眼干、视力模糊、视觉异常、横纹肌溶解。
 
用法用量
口服，推荐剂量为每次20mg，2次/d，空腹服用或饭前1h服用。严重肾功能损伤患者(肌酐清除率＜30ml/min)，推荐剂量为20mg/d，睡前服用。75岁以上老年患者，起始剂量为20mg/d。
 
药物相应作用
1.本品从肾脏排出主要经肾小管分泌作用，与其他经肾小管分泌排泄的药物(如地高辛、普鲁卡因胺、双哌雄双酯、吗啡、万古霉素、二甲双胍及替诺福韦)同时使用，有可能引起二者血药浓度的提高，应对患者进行严密监护。
2.与混合性P450抑制剂西咪替丁合用，本品的Cmax和AUC增加。
3.本品为CYP2D6和CYP3A4抑制剂，与主要经CYP2D6代谢的治疗窗较窄的药物(如氟卡尼、硫利达嗪及三环类抗抑郁药)合用时应谨慎。本品可使丙咪嗪的Cmax和AUC增加。
4.与其他抗胆碱药合用，可能加剧口干、便秘、视力模糊及其他抗胆碱症状。
5.由于本品的胃肠道动力降低作用，本品可影响其他药物的胃肠道吸收。

Sanctura (trospium chloride)
Company: Indevus Pharmaceuticals
Approval Status: Approved May, 2004
Treatment for: Overactive bladder
Areas: Urology & Kidneys

General Information
Sanctura oral tablets contain trospium, an antimuscarinic antispasmodic agent. Antimuscarinic agents act as parasympathetolytics in muscular tissues, and has been shown to reduce the tonus (elastic tension) of smooth muscles of the bladder.

It is specifically indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Sanctura is administered via oral tablets of 20 mg twice daily, with a possible reduction in dosage, to 20 mg once daily, in the elderly and in subjects with renal impairment. Dosing should occur at least 1 hour prior to meal times.

Clinical Results
FDA approval of Sanctura was based upon two 12 week, double-blind, placebo controlled studies. The first study enrolled a total of 523 subjects with urge or mixed (predominantly urge) incontinence, with >70 micturitions and >7 urge incontinence episodes per week. Subjects received either 20 mg. Sanctura (n=262) or placebo (n=261) twice daily for 12 weeks. Subjects receiving Sanctura were shown to have significantly fewer micturitions per day (p < 0.001), significantly fewer urge incontinence episodes per week (p = 0.012), and significantly greater void volume per micturition (p < 0.001). The second trial, which enrolled 658 subjects (329 Sanctura, 329 placebo), consistently confirmed the results of the first.

Side Effects
Adverse events associated with the use of Sanctura may include, but are not limited to, the following:
Dry mouth
Constipation
Dyspepsia
Headache
In addition, angioneurotic edema was observed in one subject during clinical investigation; it is has not been determined if this reaction represents a clinically relevant event.

Mechanism of Action
Trospium chloride acts as a direct antagonist at muscarinic acetylcholine receptors in cholinergically innervated organs. It has been shown to have negligible affinity for nicotinic acteylcholine receptors at therapeutic doses, and to not easily cross the blood-brain barrier, yielding a localized, potent anticholinergic for peripheral targets. Its anticholinergic-parasympatholytic action reduces the tonus of smooth muscle in the bladder, effectively reducing the number of required voids, urge incontinence episodes, urge severity and improving retention, facilitating increased volume per void.

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 详细处方信息以本药内容附件PDF文件（201471418344120.pdf）的“原文Priscribing Information”为准
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