罗氟司特治疗慢性阻塞性肺病：改善中至重度患者肺功能

Roflumilast is an inhibitor called phosphodiesterase-4 (PDE-4). It was approved by the US FDA in 2011 for the treatment of chronic obstructive pulmonary disease (COPD), reducing the frequency of severe COPD acute exacerbations (exacerbations) and alleviating the worsening of symptoms. However, it is not used to treat other types of COPD such as primary emphysema. Selectively inhibits PDE4, blocks the transmission of inflammatory response signals, and thereby inhibits the damage to lung tissue caused by respiratory diseases such as COPD and asthma.

Chronic obstructive pulmonary disease (COPD) is a serious lung disease that causes difficulty breathing. Symptoms include difficulty breathing, chronic coughing, and excessive phlegm. Exacerbations can last for weeks at a time, leading to reduced lung function, increased risk of death, and possibly severe anxiety. Roflumilast was first successfully developed by the German company Altana and later became a product of Swiss Nycomed Pharma GmbH. Currently, the ownership of roflumilast belongs to AstraZeneca.

Effect of Roflumilast in the treatment of chronic obstructive pulmonary disease

Roflumilast, a PDE-4 inhibitor approved by the U.S. Food and Drug Administration, is available in 500 mcg tablets for once-daily dosing. In six placebo-controlled trials involving nearly 4500 patients with COPD of varying severity, use of roflumilast was associated with fewer COPD exacerbations and improved lung function, as determined by spirometry, with the greatest benefit observed in patients with severe COPD who had chronic bronchitis and a history of frequent exacerbations; clinical efficacy was demonstrated in patients who received roflumilast alone and in patients who also received an inhaled long-acting beta2-agonist (LABA).

The most common adverse events in clinical trials of roflumilast were diarrhea, nausea, and headache. Weight loss and an increased risk of psychiatric events have been reported with the use of roflumilast. Because roflumilast is rapidly converted to its active metabolite by cytochrome P-450 (CYP) isoenzymes, coadministration with strong CYP inducers is not recommended. It is recommended that patients take medication under the guidance of a doctor and receive symptomatic treatment.

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References

Lipari M, Benipal H, Kale-Pradhan P. Roflumilast in the management of chronic obstructive pulmonary disease. Am J Health Syst Pharm. 2013 Dec 1;70(23):2087-95. doi: 10.2146/ajhp130114. PMID: 24249758.