Roflumilast (CAS: 162401-32-3) is a drug used in the treatment of chronic obstructive pulmonary disease (COPD). It belongs to the class of drugs known as phosphodiesterase-4 (PDE-4) inhibitors. Roflumilast is sold under the brand name Daliresp and was first approved by the FDA in 2011.
Chemical name: 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide Molecular formula: C17H14Cl2F2NO3 Formula weight: 403.20 g/mol CAS No: 162401-32-3
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Synonyms: 3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(2,2,2-trifluoroethoxy)benzamide, Daxas, 4-(difluoromethoxy)-3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)benzamide.
Health Benefits of Roflumilast: Roflumilast is primarily used for the treatment of chronic obstructive pulmonary disease (COPD) in adults with symptoms of chronic bronchitis and a history of exacerbations. It is not a bronchodilator, but it helps to reduce inflammation in the airways, which can improve breathing and decrease the risk of exacerbations.
Product Mechanism: Roflumilast works by inhibiting the enzyme phosphodiesterase-4 (PDE-4), which is involved in the breakdown of cyclic adenosine monophosphate (cAMP). By inhibiting PDE-4, roflumilast increases the levels of cAMP in cells, which has an anti-inflammatory effect. Roflumilast also has immunomodulatory effects, helping to reduce the inflammation that can lead to COPD exacerbations.
Potential Effects: The primary effect of roflumilast is reducing airway inflammation, which can improve pulmonary function and decrease the risk of exacerbations. In clinical trials, roflumilast has been shown to improve lung function and reduce the rate of exacerbations in patients with COPD. Roflumilast has also been shown to have a significant effect on symptoms such as cough and sputum production.
Safety: Common side effects of roflumilast include diarrhea, nausea, decreased appetite, and weight loss. More serious side effects include psychiatric symptoms such as depression and suicidal ideation. Roflumilast can also cause liver damage in some patients, and regular monitoring of liver function is recommended during treatment.
Side Effects and Dosing Information: The recommended dose of roflumilast is one 500-mcg tablet taken orally once a day, with or without food. Patients with moderate to severe liver impairment should not take roflumilast, and patients with mild liver impairment should take a lower dose. Patients with a history of depression, suicidal ideation, or other psychiatric disorders should be closely monitored for psychiatric symptoms while taking roflumilast.
Conclusion: Roflumilast is a phosphodiesterase-4 (PDE-4) inhibitor used in the treatment of chronic obstructive pulmonary disease (COPD). It works by reducing inflammation in the airways, which can improve pulmonary function and decrease exacerbations. While roflumilast is generally safe and well-tolerated, patients taking it should be monitored for potential side effects, particularly psychiatric symptoms. Roflumilast can be an effective treatment option for patients with COPD who have a history of exacerbations, but as with all medications, its use should be carefully monitored by a healthcare professional.