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Roflumilast: a review of its use in the treatment of COPD

Authors Wedzicha J, Calverley PM, Rabe K

Received 4 June 2015

Accepted for publication 5 August 2015

Published 6 January 2016 Volume 2016:11(1) Pages 81—90

DOI https://doi.org/10.2147/COPD.S89849

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Richard Russell


Jadwiga A Wedzicha,1 Peter MA Calverley,2 Klaus F Rabe3,4

1Airways Disease Section, National Heart and Lung Institute, Imperial College London, London, 2Institute of Ageing and Chronic Disease, University of Liverpool, Liverpool, UK; 3Department of Internal Medicine, Christian-Albrechts University, Kiel, 4Department of Pulmonary Medicine and Medical Director, LungenClinic Grosshansdorf, Airway Research Centre North, German Centre for Lung Research, Grosshansdorf, Germany


Abstract: COPD is a progressive condition involving chronic inflammation and parenchymal destruction with resulting airflow limitation. COPD is associated with worsening airflow limitation over time and increased frequency of COPD exacerbations, leading to increased mortality and morbidity. The effects of COPD extend beyond the lungs, as multiple comorbidities may occur with COPD, including cardiovascular disease, diabetes mellitus, osteoporosis, depression, and pneumonia. COPD exacerbations are associated with a rapid worsening of baseline symptoms that requires prompt management and may necessitate hospitalization in the case of a severe episode. Patients with COPD exacerbations require urgent management of symptoms to prevent further worsening, and preventative steps may be taken to help reduce the number and frequency of future exacerbations. Roflumilast is a potent and selective inhibitor of the enzyme phosphodiesterase-4 that targets the systemic inflammation associated with COPD. Roflumilast has a variety of anti-inflammatory effects including decreasing inflammatory mediators and the expression of cell surface markers and inhibition of apoptosis. Several clinical trials evaluating roflumilast in the treatment of COPD have demonstrated significant improvements from baseline versus placebo in lung function, including increases in mean pre- and postbronchodilator forced expiratory volume in 1 second and forced vital capacity. Data suggest that roflumilast reduces moderate to severe exacerbations with the benefit most well established in patients with severe disease. Given this evidence, roflumilast, as part of a combination regimen with long-acting bronchodilators, appears to be a reasonable treatment option for patients with severe to very severe COPD associated with chronic bronchitis and a history of exacerbations.

Keywords: COPD, exacerbations, phosphodiesterase-4 inhibitors, roflumilast, chronic bronchitis

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