罗氟司特：一种磷酸二酯酶-4 抑制剂，用于治疗严重的慢性阻塞性肺疾病。
Roflumilast: a phosphodiesterase-4 inhibitor for the treatment of severe chronic obstructive pulmonary disease.
机构信息
Department of Pharmacy Practice, Auburn University Harrison School of Pharmacy, Auburn, Alabama, USA.
出版信息
Clin Ther. 2012 Jan;34(1):56-66. doi: 10.1016/j.clinthera.2011.12.008.
BACKGROUND
Roflumilast is a newly approved phosphodiesterase-4 inhibitor for the treatment of severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis and a history of exacerbations.
OBJECTIVE
The objective of this article is to review the pharmacology, clinical efficacy, and tolerability of roflumilast in the treatment of COPD.
METHODS
Articles were identified using MEDLINE (1966-August 1, 2011) and EMBASE (1947-August 1, 2011). Searches were conducted using the terms roflumilast and COPD. Included in the search were all English-language clinical trials that were randomized, had durations of >6 weeks, and studied the effects of roflumilast on the forced expiratory volume in 1 second (FEV(1)) or rates of exacerbations in patients with COPD. Abstracts from the annual meetings of the American Thoracic Society, American College of Chest Physicians, and European Respiratory Society were also searched to identify relevant publications. In addition, all pertinent studies evaluating the pharmacokinetics and pharmacodynamics of roflumilast were included.
RESULTS
A total of 6 clinical trials (4 publications) evaluating the efficacy of roflumilast were identified and included. For the treatment of COPD, roflumilast was associated with a significant improvement in lung function (increase in FEV(1) of 36-88 mL) when compared with placebo. Roflumilast also reduced the rate of exacerbations in subsets of patients with chronic cough and a history of exacerbations. Overall, health-related quality of life was not significantly affected. Adverse effects were common in clinical trials, with 9% to 16% of patients discontinuing therapy as a result. The most frequently reported adverse effects were gastrointestinal issues, headache, and weight loss. Suicide-related adverse effects have occurred in 5 patients receiving roflumilast and 1 patient receiving placebo.
CONCLUSION
Roflumilast significantly improved FEV(1) in clinical trials but had inconsistent reductions in the rates of exacerbations. Comparative studies with recommended therapies for COPD, particularly inhaled corticosteroids, are needed to better assess the role of roflumilast in the management of COPD.
背景
罗氟司特是一种新型磷酸二酯酶-4 抑制剂，用于治疗伴有慢性支气管炎病史和加重史的严重慢性阻塞性肺疾病（COPD）。
目的
本文旨在综述罗氟司特治疗 COPD 的药理学、临床疗效和耐受性。
方法
通过 MEDLINE（1966 年 8 月 1 日-2011 年 8 月 1 日）和 EMBASE（1947 年 8 月 1 日-2011 年 8 月 1 日）检索文献，检索词为罗氟司特和 COPD。纳入的研究为所有用英语发表的随机、疗程超过 6 周、评估罗氟司特对 COPD 患者第 1 秒用力呼气量（FEV1）或加重率影响的临床试验。还检索了美国胸科学会、美国胸科医师学会和欧洲呼吸学会年会的摘要，以确定相关文献。另外，还纳入了所有评估罗氟司特药代动力学和药效学的相关研究。
结果
共确定了 6 项（4 篇文献）评估罗氟司特疗效的临床试验。与安慰剂相比，罗氟司特治疗 COPD 可显著改善肺功能（FEV1 增加 36-88ml）。罗氟司特还降低了慢性咳嗽和加重史亚组患者的加重率。总体而言，健康相关生活质量无显著影响。临床试验中常见不良反应，导致 9%-16%的患者停药。最常报告的不良反应为胃肠道问题、头痛和体重减轻。使用罗氟司特的 5 例患者和使用安慰剂的 1 例患者出现了与自杀相关的不良反应。
结论
罗氟司特可显著改善临床试验中的 FEV1，但对加重率的降低作用不一致。需要与 COPD 的推荐疗法（特别是吸入性皮质激素）进行对比研究，以更好地评估罗氟司特在 COPD 治疗中的作用。
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