部份中文罗氟司特处方资料（仅供参考）
商品名：Daxas Filmtabletten
英文名：Roflumilast
中文名：罗氟司特薄膜片
生产商：武田制药
药品简介
罗氟司特；每日一片能减少严重的慢性阻塞性肺病(COPD)急性发作频率，减缓症状恶化.
2010年7月，欧盟批准Daxas®（Daliresp®，罗氟司特）上市,用于慢性阻塞性肺疾病(COPD)的治疗，可减轻全身和肺部炎症并改善患有严重慢性阻塞性肺疾病（COPD）的患者的疾病症状。
本品为一日1次用药的口服片剂，须与其他支气管扩张药合用，适用于有频繁加重病史的成人患者慢性支气管炎相关严重COPD(舒张后FEV1小于预计值的50%)的维持治疗。本品作为新一类COPD治疗药物，首先上市的国家为德国和英国。
作用机制
罗氟司特是一种PDE4抑制剂，一种非类固醇抗炎活性物质，旨在靶向与COPD相关的全身和肺部炎症。其作用机制是抑制PDE4，PDE4是一种主要的环磷酸腺苷（cAMP）代谢酶，存在于对COPD发病机制重要的结构和炎症细胞中。罗氟司特靶向PDE4A、4B和4D剪接变体，在纳摩尔范围内具有相似的效力。对PDE4C剪接变体的亲和力低5到10倍。这种作用机制和选择性也适用于罗氟司特的主要活性代谢产物——N-氧化物。
适应症
Daxas适用于有频繁急性发作史的成年患者中与慢性支气管炎相关的严重慢性阻塞性肺疾病（COPD）（支气管扩张剂后FEV1低于预测的50%）的维持治疗，作为支气管扩张剂治疗的补充。
用法与用量
剂量
起始剂量
推荐的起始剂量是一片250微克的罗氟司特，每天服用一次，持续28天。
该起始剂量旨在减少开始治疗时的不良反应和患者停药，但它是亚治疗剂量。因此，250微克剂量应仅用作起始剂量。
维持剂量
在用250微克的起始剂量治疗28天后，患者必须滴定至一片500微克的罗氟司特，每天服用一次。
可能需要服用500微克罗氟司特数周才能达到其全部效果。罗氟司特500微克已在临床试验中研究长达一年，旨在用于维持治疗。
特殊人群
老年人
无需调整剂量。
肾功能损害
无需调整剂量。
肝损伤
对于归类为Child-Pugh A的轻度肝损伤患者，罗氟司特的临床数据不足以建议调整剂量，因此这些患者应谨慎使用达克萨。归类为Child-Pugh B或C级的中度或重度肝损伤患者不得服用达克斯。
儿科人群
Daxas在儿科人群（18岁以下）中没有用于慢性阻塞性肺病的适应症
给药方法
用于口服。
片剂应与水一起吞服，每天同一时间服用。药片可以与食物一起服用或不服用。
禁忌症
对活性物质或列出的任何赋形剂过敏。
中度或重度肝损伤（Child-Pugh B或C）。
保质期
3年。
储存特别注意事项
这种药品不需要任何特殊的储存条件。
容器的性质和内容物
10、14、28、30、84、90或98片薄膜包衣片剂包装中的PVC/PVDC铝泡罩。
上市持证商
阿斯利康英国有限公司
请参阅随附的Daxas完整处方信息：
https://www.medicines.org.uk/emc/product/5650/smpc
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Daliresp (Roflumilast), Treatment to Reduce COPD, United States of America
Daliresp (Roflumilast) is an oral tablet that is proved to reduce the risk of exacerbations in patients suffering from severe chronic obstructive pulmonary disease (COPD). The drug has been developed by Nycomed.
Marketed as Daxas in the European markets, Daliresp was approved by the US FDA in March 2011. The European marketing approval for Daxas was received in 2010.
Daliresp will be available in US markets in the second quarter of 2011. It will be marketed by Nycomed's partner Forest Laboratories.
Chronic obstructive pulmonary disease
COPD is a progressive and irreversible lung disease which narrows the airways, thus causing respiratory problems. Breathlessness, chronic cough and congestion of phlegm in the lungs are the major symptoms associated with COPD.
These symptoms worsen further to cause exacerbation that lasts for weeks, requiring immediate hospitalisation and intensive medication. If left unattended, exacerbation can result in failure of lungs and could even be fatal.
Daliresp
Daliresp is an oral tablet to be taken once daily. It is the first and the only selective phosphodiesterase-4 (PDE4) inhibitor approved by the FDA.
Although the mechanism of action of the drug is not known, it is believed that the therapeutic action is exerted in patients by effects related to increase in intracellular cyclic adenosine metaphosphate (cAMP) in lung cells.
Clinical trials
Daliresp was eva luated in eight clinical trials conducted in a randomised double-blind, controlled parallel group. Around 9,394 patients of 40 years and above were enrolled in these trials.
Trials 1 and 2 were placebo-controlled dose selection trials of six months duration. These trials were conducted on 1,929 patients to eva luate the efficacy of Daliresp 250mcg and 500mcg tablet once daily. The median age of the enrolled patients was 63 years, associated with severe COPD in the range of 30%-80%.
Of the total randomised population, 751 patients were administered with 250mcg Daliresp and 724 with 500mcg. The 500mcg was selected over 250mcg based on the nominal improvement in lung function.
Trials 3, 4, 5 and 6 were once-year placebo-controlled trials. These were conducted to eva luate the efficacy of the treatment in patients who reported to have less than 50% of COPD severity and faced exacerbations. The enrolled patients were in the median age of 64 years.
Trials 3 and 4 included patients with less than 50% severity with chronic bronchitis and smoking history of 10 years. Trial 3 enrolled 1,176 patients of whom 567 were tested with Daliresp. Trial 4 was conducted on 1,514 patients of whom 760 were treated with Daliresp.
Both these trials failed to show significant reduction in the exacerbations in majority of the population. However, exploratory studies revealed that the treatment showed better response in reduction of COPD exacerbation in a small section of the population. Therefore further trials 5 and 6 were conducted on patients associated with chronic bronchitis, at least one COPD exacerbation in the previous year and a 20 pack year of smoking history.
Trial 5 had enrolled a total of 1,525 patients of whom 765 were administered Daliresp. Trial 6 had a total of 1,571 patients enrolled of whom 772 were tested with Daliresp. In both the trials, 500mcg Daliresp once daily confirmed that the treatment of Daliresp had resulted in a significant reduction of moderate or severe exacerbations compared to placebo. These two trials proved the safety and supported the use of Daliresp in the reduction of exacerbations of COPD.
Trials 7 and 8 were six months trails conducted to eva luate the efficacy of Daliresp as an add-on therapy to a bronchodilator. Patients enrolled for these trials were with moderate to severe COPD and of 65 years of median age.
The trials were conducted on patients with moderate to severe (40%-70% predicted) COPD without any chronic bronchitis or history of exacerbations. The results indicated that the drug showed significant response in reducing the exacerbations.