ENABLEX ®（darifenacin）缓释片 
美国初步批准：2004

适应症 
毒蕈碱受体拮抗剂Enablex是为膀胱过动症与急迫性尿失禁，紧迫性和频率症状的治疗表示。

剂量和用法 
建议的出发Enablex缓释片剂量为7.5毫克，每日一次。根据个人的反馈表明，剂量可增至15毫克，每天一次，如早两个星期后开始治疗。

对Enablex每日剂量不应超过7.5毫克以下患者：

中度肝功能不全患者（Child - Pugh分级乙） 
患者服用烈性CYP3A4抑制剂
Enablex不建议病人使用严重肝受损（Child - Pugh分级丙）。  
Enablex可采取或没有食物。吞下的药片应整水，而不是咀嚼，分裂或挤压。 
  
剂型和优势 
缓释片7.5毫克和15毫克。 
  
禁忌 
Enablex是禁忌的患者，或在风险中，下列条件：

尿潴留， 
胃潴留，或 
失控的窄角型青光眼。

注意事项： 
Enablex应谨慎加以管理与临床意义膀胱由于尿潴留的风险流出阻塞的病人。
Enablex应谨慎加以管理与因胃内滞留胃肠道阻塞性疾病患者的危险。 
Enablex应谨慎使用的患者正在接受治疗的窄角型青光眼，并且只有在潜在利益大于风险。

不良反应 
最常见的不良反应为Enablex（“3％）是：便秘，口干，头痛，消化不良，恶心，尿路感染，意外受伤，和流感症状。

药物相互作用 
注意事项时，应采取Enablex是随之而来的是主要由CYP2D6和代谢有一个狭窄的治疗窗口，如氟卡尼，甲硫达嗪和三环类抗抑郁药，药物使用。 
与其他的Enablex抗胆碱药物同时使用可能会增加的频率和/口干，便秘或严重程度，视力模糊等抗胆碱药理作用。抗胆碱药物可能会潜在地改变一些随之而来给药因肠胃蠕动影响吸收。

利用在种群 
怀孕：Enablex应该在怀孕期间使用只有在对母亲的潜在利益大于对胎儿的风险。  
哺乳母亲：这不知道是否darifenacin到人的乳汁排出，因此应谨慎前Enablex行使管理是一个哺乳妇女。
儿童用药：在安全性和有效性Enablex儿童患者尚未确定。

Emselex

Active Substance: darifenacin hydrobromide 
Common Name: darifenacin hydrobromide 
ATC Code: G04BD10
Marketing Authorisation Holder: Merus Labs Luxco II S.à R.L.
Active Substance: darifenacin hydrobromide 
Status: Authorised
Authorisation Date: 2004-10-22
Therapeutic Area: Urinary Incontinence, Urge Urinary Bladder, Overactive
Pharmacotherapeutic Group: Urinary antispasmodics

Therapeutic Indication

Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in adult patients with overactive bladder syndrome.

What is Emselex?

Emselex is a medicine that contains the active substance darifenacin. It is available as prolonged-release tablets (7.5 mg and 15 mg). ‘Prolonged-release’ means that darifenacin is released slowly from the tablet over a few hours.

What is Emselex used for?

Emselex is used in adults with overactive-bladder syndrome. It is used to treat the urge incontinence (sudden lack of control over urination), increased urinary frequency (need to urinate frequently) and urgency (sudden urge to pass urine) that are associated with the syndrome.

The medicine can only be obtained with a prescription.

How is Emselex used?

The recommended starting dose of Emselex is 7.5 mg once a day. For patients requiring greater symptom relief, the dose may be increased to 15 mg. The tablets should be swallowed whole with some liquid, and not chewed, divided or crushed.

How does Emselex work?

The active substance in Emselex, darifenacin, is an anticholinergic medicine. It blocks a receptor called the ‘muscarinic M3 receptor’. In the bladder, this causes the muscles that push urine out of the bladder to relax. This leads to an increase in the capacity of the bladder and changes in the way the bladder contracts, resulting in fewer bladder contractions. This helps Emselex to prevent unwanted urination.

How has Emselex been studied?

Emselex has been studied in four main studies in a total of 2,078 male and female patients with symptoms of overactive bladder. Emselex was used at various doses (from 3.75 mg to 30 mg a day) and compared with placebo (a dummy treatment) or with tolterodine (another medicine used in this condition). The main measure of effectiveness was the change in the number of incontinence episodes per week.

What benefit has Emselex shown during the studies?

When the results from all four studies were combined, Emselex was more effective in reducing the number of incontinence episodes than placebo. At the start of the studies, the patients had around 16 incontinence episodes per week. After 12 weeks of treatment, patients receiving Emselex 7.5 mg or 15 mg had 8.8 (68%) or 10.6 (77%) fewer episodes of incontinence per week, respectively, and patients receiving placebo had 7 or 7.5 (54 or 58%) fewer episodes per week.

What is the risk associated with Emselex?

The most common side effects with Emselex (seen in more than 1 patient in 10) are dry mouth and constipation. For the full list of all side effects reported with Emselex, see the package leaflet.

Emselex must not be used in people who are hypersensitive (allergic) to darifenacin or any of the other ingredients. It must not be used in patients with:

· urinary retention (difficulty passing urine);

· gastric retention (when the stomach does not empty properly);

· uncontrolled narrow-angle glaucoma (increased eye pressure even with treatment);

· myasthenia gravis (a disease causing muscle weakness);

· severe liver problems;

· severe ulcerative colitis (severe inflammation of the gut causing ulcers and bleeding);

· toxic megacolon (a very serious complication of colitis).

Emselex must not be taken by patients who are also taking medicines that could affect the way that Emselex is broken down in the body, such as protease inhibitors (used to treat HIV infection, such as ritonavir), or ketoconazole or itraconazole (used to treat fungal infections).

Why has Emselex been approved?

The CHMP concluded that Emselex showed an effectiveness similar to that of other anticholinergic medicines used in overactive bladder syndrome. The Committee decided that Emselex’s benefits are greater than its risks and recommended that it be given marketing authorisation.

Other information about Emselex

The European Commission granted a marketing authorisation valid throughout the European Union for Emselex on 22 October 2004.

For more information about treatment with Emselex, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.