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罗氟司特片（ROFLUMILAST，DALIRESP）

2012-09-23 21:16:05 作者：新特药房来源：中国新特药网天津分站浏览次数：597 文字大小：【大】【中】【小】

简介： 部分中文罗氟司特处方资料（仅供参考）美国FDA 2011年3月1日批准Daliresp(罗氟司特[roflumilast])片 – 既往名Daxas美国食品和药品监督管理局(FDA)批准Daliresp (roflumilast)，每天服用一药丸减低来 ...

关键字：罗氟司特片（ROFLUMILAST DALIRESP）

美国食品和药品监督管理局(FDA)批准Daliresp(roflumilast)，每天服用一药丸减低来自严重慢性阻塞性肺疾病(COPD)频繁发作(加重)或症状的恶化.
COPD是一种使呼吸困难的严重肺病疾病。症状可包括气短，慢性咳嗽，和过多痰。1次加重可能持续几周和导致肺不功能衰退, 死亡风险增加，而且可能伴有严重焦虑。
按美国心，肺，和血液研究所吸烟是COPD的主要病因，在美国COPD是美国第四位死亡原因。
Roflumilast，治疗COPD 新药类别，是一种被称为4型磷酸二酯酶(PDE-4)酶的抑制剂。适用于有严重COPD人们治疗咳嗽症状和与支气管炎关联的多量粘液。Roflumilast不意向治疗主要肺气肿的另一种形式COPD。
FDA的药物评价和研究中心中药物评价II部主任Curtis Rosebraugh, M.D., M.P.H说“COPD是一种随时间变坏的严重疾病，”“新的治疗选择减低发作或加重频数在帮助有COPD伴慢性支气管炎和加重史患者处理这种使人衰弱疾病是很重要的。”
在包括超过1,500例患者年龄40和以上接受roflumilast的两项3期临床研究证实Roflumilast的安全性和有效性。被治疗患者有COPD史伴慢性支气管炎和开始治疗前12个月期间曾经受疾病加重。
FDA批准roflumilast有一个药物指导告知患者精神健康问题潜在风险，包括情绪变化，思维，或行为，以及不能解释的体重减轻。
Roflumilast不应用于治疗突然呼吸困难(急性支气管痉挛)，和不推荐为小于18岁的人们。接受roflumilast患者最常报道副作用包括腹泻，恶心，头痛，失眠，背痛，食欲减退，和头晕。
批准日期：2011年3月1日；公司：Forest Pharmaceuticals, Inc.

一般描述
DALIRESP片中的活性成分是roflumilast。Roflumilast及其活性代谢物(roflumilast氮氧化物)是选择性磷酸二酯酶4 (PDE4) 抑制剂。roflumilast的化学名是N-(3,5-dichloropyridin-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxy-benzamide。其经验式是C17H14Cl2F2N2O3和分子量为403.22。
化学结构是：

药物物质是一种白色至灰白色不吸潮粉，熔点160°C。实际上不溶于水和正己烷，略溶于乙醇和易溶于丙酮。
DALIRESP以白色至灰白色圆片供应，一侧雕与“D” 和另侧“500”。每片含500 μg的roflumilast。每片口服给药DALIRESP含以下无活性成分：一水乳糖，玉米淀粉，聚乙烯吡啶酮和硬脂酸镁。

作用机制
Roflumilast及其活性代谢物(roflumilast氮氧化物)是磷酸二酯酶4(PDE4)的选择性抑制剂。Roflumilast和roflumilast氮氧化物抑制PDE4(在肺组织中一种主要的环-3’,5’-磷酸腺苷(环AMP)-代谢酶)活性导致细胞内环AMP的蓄积。而通过这种特殊机制DALIRESP在COPD患者中发挥其治疗作用未充分确定，被认为是增加肺细胞细胞内环AMP的作用有关。

适应证和用途
DALIRESP是适用于治疗有严重COPD伴有慢性支气管炎和加重史的患者中以减低COPD加重的风险(1, 14)
使用的限制：DALIRESP不是一种支气管扩张剂而且不适用于为缓解急性支气管扩张。(1, 14)
剂量和给药方法
对有COPD患者的推荐剂量为每天一片500 μg，有或无食物。(2)
剂型和规格
片：500 μg (3)
禁忌证
（1）中度至严重肝受损(Child-Pugh类别B或C)。(4)
警告和注意事项
（1）急性支气管痉挛：不要用予缓解急性支气管痉挛。(5.1)
（2）精神事件包括自杀行为：建议患者，他们的护理人员，和家庭警惕失眠，焦虑，抑郁, 自杀念头或其他情绪变化出现或恶化，和如发生这类变化联系他们的医疗卫生提供者。在有抑郁和/或自杀念头或行为史患者中仔细权衡用DALIRESP治疗的风险和获益。(5.2)
（3）体重减轻：常规监查体重。如发生不能解释或有临床意义的体重减轻，评价体重减轻和考虑停止DALIRESP。(5.3)
（4）药物相互作用：建议不要与强细胞色素P450酶诱导剂使用(如利福平[rifampicin]，苯巴比妥[Phenobarbital]，卡马西平[carbamazepine]，苯妥英[phenytoin])。(5.4)
不良反应
最常见不良反应(≥ 2%)是腹泻，体重减轻，恶心，头痛，背痛，流感，失眠，头晕和食欲减退。(6.1)
为报告不良反应联系Forest Laboratories, Inc.改善电话1-800-678-1605或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.
药物相互作用
（1）与CYP3A4抑制剂或CYP3A4和CYP1A2双重抑制剂使用(如，红霉素[erythromycin], 酮康唑ketoconazole]，氟伏沙明[fluvoxamine]，依诺沙星[enoxacin]，西咪替丁[cimetidine])将增加roflumilast全身暴露和可能导致增加不良反应。这类同时使用的风险应仔细对效益权衡。(7.2)
特殊人群中使用
（1）哺乳母亲：因为roflumilast和/或其代谢物可能排泄至人乳和尚无DALIRESP对母乳唯有婴儿的研究，正在哺乳的妇女不应使用DALIRESP。(8.3)

如何供应/贮存/处置
1 如何供应
DALIRESP以白色至灰白色圆片供应，一侧凹有“D”和另一侧“500”。每片含500 μg roflumilast。
DALIRESP片可得到在瓶中s含30片 - NDC 0456-0095-30或90片 - NDC 0456-0095-90.
2 贮存和处置
贮藏DALIRESP 500 μg片在20° - 25°C (68° - 77°F)‘外出时允许至15° - 30°C(59° - 86°F)。[见USP控制室温]。

Daliresp
Generic Name: roflumilast
Date of Approval: February 28, 2011
Company: Forest Pharmaceuticals, Inc.
Treatment for: Chronic Obstructive Pulmonary Disease (COPD)
FDA Approves Daliresp
The U.S. Food and Drug Administration has approved Daliresp (roflumilast), a pill taken daily to decrease the frequency of flare-ups (exacerbations) or worsening of symptoms from severe chronic obstructive pulmonary disease (COPD).
Roflumilast, a new drug class for the treatment of COPD, is an inhibitor of an enzyme called phosphodiesterase type 4 (PDE-4). It is indicated for people with severe COPD to treat the symptoms of cough and excess mucus linked to bronchitis. Roflumilast is not intended to treat another form of COPD which involves primary emphysema.
Daliresp Medication Guide
Read this Medication Guide before you start taking Daliresp and each time you get a refill. There may be new information. This information does not take the place of talking with your healthcare provider about your medical condition or treatment.
Important information about Daliresp
Daliresp can cause serious side effects. Tell your healthcare provider right away if you have any of the symptoms listed below while taking Daliresp.
1.Daliresp may cause mental health problems including suicidal thoughts and behavior. Some people taking Daliresp may develop mood or behavior problems including:
◦thoughts of suicide or dying
◦attempt to commit suicide
◦trouble sleeping (insomnia)
◦new or worse anxiety
◦new or worse depression
◦acting on dangerous impulses
◦other unusual changes in your behavior or mood
2.Weight loss. Daliresp can cause weight loss. You should check your weight on a regular basis. You will also need to see your healthcare provider regularly to have your weight checked. If you notice that you are losing weight, call your healthcare provider. Your healthcare provider may ask you to stop taking Daliresp if you lose too much weight.
Daliresp may affect the way other medicines work, and other medicines may affect how Daliresp works. Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.
What is Daliresp?
Daliresp is a prescription medicine used in adults with severe Chronic Obstructive Pulmonary Disease (COPD) to decrease the number of flare-ups or the worsening of COPD symptoms (exacerbations).
Daliresp is not a bronchodilator and should not be used for treating sudden breathing problems. Your healthcare provider may give you other medicine to use for sudden breathing problems.
It is not known if Daliresp is safe and effective in children.
Who should not take Daliresp?
Do not take Daliresp if you:
•have certain liver problems. Talk with your healthcare provider before you take Daliresp if you have liver problems.
Before taking Daliresp
Before you take Daliresp, tell your healthcare provider if you:
•have or have had a history of mental health problems including depression and suicidal behavior.
•have liver problems
•have any other medical conditions
•are pregnant or plan to become pregnant. It is not known if Daliresp will harm your unborn baby. Talk to your healthcare provider if you are pregnant or plan to become pregnant.
•are breastfeeding or plan to breastfeed. It is not known if Daliresp passes into your breast milk. You and your healthcare provider should decide if you will take Daliresp or breastfeed. You should not do both.
How should I take Daliresp?
•Take Daliresp exactly as your healthcare provider tells you to take it.
•Daliresp can be taken with or without food.
•If you take more than your prescribed dose of Daliresp, call your healthcare provider or go to the nearest hospital emergency room right away.
Daliresp side effects
Daliresp can cause serious side effects, including:
•See "Important information about Daliresp"
The most common side effects of Daliresp include:
•diarrhea
•weight loss
•nausea
•headache
•back pain
•flu like symptoms
•problems sleeping (insomnia)
•dizziness
•decreased appetite
Tell your healthcare provider if you have any side effect that bothers you or that does not go away.
These are not all the possible side effects of Daliresp.
How do I store Daliresp Tablets?
•Store Daliresp at 68°F to 77°F (20°C to 25°C); excursions permitted to 15° - 30°C (59° - 86°F). [See USP Controlled Room Temperature].
Keep Daliresp Tablets and all medicines out of the reach of children.
General information about Daliresp
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use Daliresp for a condition for which it was not prescribed. Do not give Daliresp to other people, even if they have the same symptoms that you have. It may harm them.
This Medication Guide summarizes the most important information about Daliresp. For more information about Daliresp, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about Daliresp that is written for health professionals.
What are the ingredients in Daliresp?
Active ingredient: roflumilast
Inactive ingredients: lactose monohydrate, corn starch, povidone and magnesium stearate.

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原产地英文商品名:
DALIRESP 500mcg/tab 30tabs/bottle
原产地英文药品名:
ROFLUMILAST
中文参考商品译名:
DALIRESP 500微克/片 30片/瓶
中文参考药品译名:
罗氟司特
生产厂家中文参考译名:
森林制药
生产厂家英文名:
FOREST RES INST INC