英文药名: Enablex(Darifenacin Extended Release Tablets)

中文药名: 达非那新缓释片

品牌药生产厂家: Novartis

药品简介

美国FDA批准诺华制药公司的达非那新 (darifenacin)缓释片（Enablex）上市，用于治疗尿失禁、尿急和尿频等膀胱活动过度症（OAB）。
制剂规格：7.5，15mg/片。
达非那新通过阻断主要对膀胱肌肉收缩反应的M3受体发挥作用，是强效毒蕈碱受体阻断剂，有助于减轻尿失禁的发生率，增加膀胱尿储量，减少排尿次数和减少急于排尿的压迫感和尿急感。
达非那新的M3作用在所有OAB治疗药物中具有独特性，制成缓释片可减少中枢神经和心血管不良反应的发生率。Enablex以新观念治疗膀胱活动过度症非常有用。
美国FDA批准Enablex上市是基于采用其不同剂量对7000多例平均58岁患者治疗的4项关键研究的有效数据和安全性数据。在这些研究中，本品组患者减少了尿失禁和排尿的频率，增加了膀胱的尿储量。本品在治疗的开始2周内每周减少尿失禁率高达83%。12周治疗期间维持疗效，长期安全性研究长达1年。对Enablex总共进行了涉及1万多例98项临床研究，最常见的不良反应是口干和便秘，病人因不良反应停药率较低。本品禁用于尿潴留、胃液潴留或未控制的狭角型青光眼和有这些疾病危险的患者，也禁用于对本品过敏者。
药理作用

达非那新通过阻断主要对膀胱肌肉收缩反应的 M3受体发挥作用，是强效毒覃碱受体阻断剂，有助于减轻尿失禁的发生率，增加膀胱尿储量，减少排尿次数和减少急于排尿的压迫感和尿急感。
适应症

用于治疗尿失禁、尿急和尿频等膀胱活动过度症。
用法用量

该药为缓释片，初始剂量通常为7.5mg/d，可在用药开始后２周内将剂量增加至15mg/d。每日一次用水服用，可与食物同服。 或遵医嘱！
不良反应

在临床试验中达非那新缓释片最常见的不良反应为口干和便秘（发生率超过安慰剂对照组），少数病例出现消化不良和头痛。
禁 忌 症

狭角性青光眼患者、尿潴留或胃潴留患者禁用该药。

包装规格：

15mg *28 缓释片
7.5mg *28 缓释片
7.5mg *90 缓释片

ENABLEX

ENABLEX® (darifenacin) extended-release tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency. 
CONTRAINDICATIONS

ENABLEX® (darifenacin) extended-release tablets are contraindicated in patients with urinary retention, gastric retention or uncontrolled narrow-angle glaucoma and in patients who are at risk for these conditions. ENABLEX is also contraindicated in patients with known hypersensitivity to the drug or its ingredients.

PRECAUTIONS

General

Risk of Urinary Retention

ENABLEX® (darifenacin) extended-release tablets should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention.

Decreased Gastrointestinal Motility

ENABLEX should be administered with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention. ENABLEX, like other anticholinergic drugs, may decrease gastrointestinal motility and should be used with caution in patients with conditions such as severe constipation, ulcerative colitis, and myasthenia gravis.

Controlled Narrow-Angle Glaucoma

ENABLEX should be used with caution in patients being treated for narrow-angle glaucoma and only where the potential benefits outweigh the risks.

Patients with Hepatic Impairment

There are no dosing adjustments for patients with mild hepatic impairment. The daily dose of ENABLEX should not exceed 7.5 mg for patients with moderate hepatic impairment. ENABLEX has not been studied in patients with severe hepatic impairment and therefore is not recommended for use in this patient population
Ask your doctor if Enablex® can help you
Enablex® blocks the nerve signals that cause your bladder to contract on its own (involuntary contraction)
When taken daily, Enablex® may help improve your symptoms so you can go to the bathroom less often and get there in time when you need to go
With Enablex®, you may start to see improvement in about 2 weeks.Enablex® is a prescription medicine used in adults to treat the following symptoms of Overactive Bladder: a strong need to urinate with leaking or wetting accidents (“urge urinary incontinence”), a strong need to urinate right away (“urgency”), and having to urinate often (“urinary frequency”).

Important Safety Information for Enablex® (darifenacin) extended-release tablets
Enablex is not for everyone. You should not take Enablex if you are not able to empty your bladder (“urinary retention”), have delayed or slow emptying of your stomach (“gastric retention”), or have an eye problem called “uncontrolled narrow-angle glaucoma.” 

Enablex may cause allergic reactions that may be serious. If you have hives, skin rash, or swelling, severe itching, experience swelling of the face, mouth or tongue, or if you have trouble breathing, stop taking Enablex and get medical help right away. Medicines like Enablex can cause blurred vision or dizziness. Do not drive or operate heavy machinery until you know how Enablex affects you. 

The most common side effects include dry mouth, constipation, headache, heartburn, nausea, urinary tract infection, blurred vision, heat exhaustion or heat stroke which can happen when Enablex is used in hot environments. Symptoms of heat exhaustion may include: decreased sweating, dizziness, tiredness, nausea, and increased body temperature.

Tell your doctor about all of the medicines you take. Enablex and certain other medicines may affect each other, causing side effects.

For more information, please see Full Prescribing Information and Patient Product Information.

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch, or call 1-800-FDA-1088.

FDA批准Enablex用于治疗神经性膀胱过动症（尿失禁症）

据瑞士巴赛尔2004年12月23日报道，诺华公司今天宣布，美国FDA已经批准了其产品Enablex（darifenacin)缓释片（7.5 mg 和15 mg）用于治疗有急性尿失禁、尿急和尿频等症状的神经性膀胱过动症（OAB）。该Enablex制剂一日一服，有望在2005年尽早上市。

M3受体是引起膀胱肌肉收缩的主要原因，Enablex通过阻断M3受体而发挥疗效。Enablex为一有效的乙酰胆碱受体拮抗剂，有助于缓解尿失禁，提升膀胱可容纳尿量，减少排尿频率，缓解尿液对膀胱的压力。

纽约医院Cornell医学中心的泌尿学副教授、医学博士David Chaikin博士说：“Enablex能够有效治疗神经性膀胱过动症，能减少对中枢神经系统和心血管方面的副作用。该药物为神经性膀胱过动症的治疗特别有用。”

FDA批准Enablex用于临床是基于大量的试验数据的基础上的，四个关键性研究和安全性数据结果是由超过7000个平均年龄在58岁的病例应用了不同剂量的该药物后得到的。在这些研究种，病人服用Enablex后，减少了排尿频率与尿失禁情况，提升了膀胱的容尿量，缓解了病人的尿急感。在开始服药两周内，由83％的病例显示降低了尿失禁次数。治疗期间，药效持续稳定12周，进行了一年以上的长期安全性研究。

诺华公司总裁及CEO Paulo Costa说：“由于许多治疗手段都效果不尽人意，所以有许多的膀胱过动症病人都放弃了治疗。我们的药物在美国上市，有望为这些病人提供有效治疗以解决他们目前所面临的困境。”

在美国大约有3千3百万的OAB患者由于膀胱肌肉不由自主的收缩而备受困扰。40岁以上的人至少有16％都有慢性OAB疾病或者类似症状。虽然该疾病随着年龄的增长而更为流行，但是几乎所有年龄段的人都有类似困扰。为了避免当众出现尿失禁的尴尬局面，OAB患者常常减少旅游、社会活动甚至工作等。

国家自制协会（National Association for Continence）执行总裁Nancy Muller先生说：“有成千上万的膀胱过动症患者以及他们家属都深受基本的困扰。我们一如既往的研究新技术，为OBA疾病患者提供帮助，以利于他们改善生活质量是十分重要的。”

总的来说，Enablex在98年开始的临床试验有超过1万的病例。该药物临床试验中最常出现的副作用是口干与便秘，但是很少有病人因此而中止接受治疗。服用Enablex后的主要副作用都是轻度和中度的，多数都在服药的头两个星期内。同别的OAB治疗药物一样，对于有尿储留、胃储留或者青光眼病人应该禁用。对该药物过敏的病人也应该禁用该药。