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Published online: 4 September 2015
© Springer International Publishing Switzerland 2015
Abstract Roflumilast (Daliresp®, Daxas®) is a selective phosphodiesterase 4 (PDE4) inhibitor that decreases systemic and pulmonary inflammation and improves disease symptoms in patients with severe chronic obstructive pulmonary disease (COPD). This article reviews the pharmacological properties of roflumilast and its clinical efficacy and tolerability in patients with COPD. Roflumilast is an effective treatment in patients with moderate to severe COPD; it improves lung function and is generally associated with a lower risk of exacerbation, particularly in patients with more severe disease and/or chronic bronchitis, cough and sputum. It is generally well tolerated; the most common adverse event was diarrhoea. While associated with an increased risk of psychiatric adverse events and weight loss, roflumilast is not associated with an increased risk of respiratory disease and infection, and may decrease the risk of cardiovascular adverse events. Roflumilast is a useful addition to the treatment options for patients with COPD.
1 Introduction
Chronic obstructive pulmonary disease (COPD) is associated with significant morbidity, mortality and economic and social burden worldwide, and that burden is steadily increasing [1]. Aside from non-pharmacological therapies (e.g. smoking cessation, pulmonary rehabilitation), and influenza and pneumococcal vaccinations, recommended treatments for COPD include bronchodilators [such as short- and long-acting b-adrenoceptor agonists (SABAs and LABAs, respectively), short- and long-acting muscarinic antagonists (SAMAs and LAMAs) and methylxanthines], inhaled corticosteroids (ICS), and the phosphodiesterase 4 (PDE4) inhibitor roflumilast (Daliresp®, Daxas®)[1]. Combination therapy is often required for optimal efficacy [1].
Roflumilast is an anti-inflammatory drug which was developed to target systemic and pulmonary inflammation [2], and was the first selective PDE4 inhibitor to be licensed for the treatment of COPD [3]. As it had a novel, potentially complementary, mechanism of action compared with that of ICS and bronchodilators, it was expected that coadministration of roflumilast with other COPD therapies would result in an enhanced clinical benefit [4]. This article reviews the pharmacological properties of roflumilast and its clinical efficacy and tolerability in patients with COPD.
2 Pharmacodynamic Properties of Roflumilast
Roflumilast and roflumilast N-oxide, the only major roflumilast metabolite observed in human plasma, are both selective PDE4 inhibitors [2, 5]. PDE4 is a major cyclic AMP (cAMP)-metabolizing enzyme present in structural and inflammatory cells in the lung, which...