Clinical Considerations for Roflumilast: A New Treatment for COPD.

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Kelly Freeman ML

Clinical Considerations for Roflumilast: A New Treatment for COPD.

Consult Pharm. 2012 Mar;27(3):189-93. doi: 10.4140/TCP.n.2012.189.

PubMed ID

22421519 [ View in PubMed

]

Abstract

Chronic obstructive pulmonary disease (COPD) causes significant morbidity and mortality and represents the fourth leading cause of death in the world. Roflumilast is the first oral phosphodiesterase inhibitor indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and history of exacerbations. Roflumilast and its active metabolite have been associated with increased cyclic adenosine monophosphate (cyclic AMP) in the lungs and positive responses with inflammatory markers. Significant improvements in forced expiratory volume (1 sec) have been observed in clinical trials comparing roflumilast with placebo. Combination therapy of roflumilast (500 mug) with long-acting beta agonists resulted in reduced COPD exacerbations in patients with severe COPD. Adverse effects include weight loss, diarrhea, nausea, and psychiatric disturbances. Roflumilast may be associated with significant drug-drug interactions with CYP3A4 inducers (strong) and immunosuppressants. Roflumilast is a promising new agent in the treatment of COPD; however, additional studies comparing roflumilast with inhaled corticosteroids plus long-acting bronchodilators are needed.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Roflumilast	Cytochrome P450 3A4	Protein	Humans	No	Substrate	Details