From the Guidelines
Roflumilast is recommended for patients with severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis and a history of exacerbations to reduce the risk of COPD exacerbations. This recommendation is based on the most recent and highest quality study, which found that roflumilast decreased the number of moderate or severe exacerbations per patient-year (rate ratio 0.85,95% CI 0.78–0.91) and increased time to next exacerbation (hazard ratio 0.88,95% CI 0.81–0.96) 1. Roflumilast works as a selective phosphodiesterase-4 (PDE4) inhibitor, which helps reduce inflammation in the lungs by preventing the breakdown of cyclic AMP, ultimately decreasing inflammatory cell activity.
Patient Selection
Roflumilast is typically prescribed for patients with severe COPD, defined as a post-bronchodilator FEV1/FVC <0.70 and an FEV1 % pred of 30–49%, and a history of one or more COPD exacerbations during the previous year 1. Patients with chronic bronchitis and severe to very severe COPD may also benefit from roflumilast therapy, as it has been shown to improve lung function and reduce moderate and severe exacerbations in this population 1.
Dosage and Administration
Roflumilast is typically prescribed as a 500 microgram tablet taken once daily, with or without food. It is not a rescue medication for acute bronchospasm and should be used as part of a comprehensive COPD management plan alongside bronchodilators.
Side Effects and Interactions
Common side effects of roflumilast include diarrhea, weight loss, nausea, headache, and back pain 1. Patients should be monitored for psychiatric adverse effects, including insomnia and depression. Roflumilast is contraindicated in patients with moderate to severe liver impairment and may interact with certain medications like rifampicin, erythromycin, and ketoconazole that affect its metabolism.
Benefits and Risks
The benefits of roflumilast therapy include a reduction in the risk of COPD exacerbations and an improvement in lung function 1. However, roflumilast therapy is also associated with an increased risk of adverse events, including diarrhea, weight loss, and psychiatric adverse effects. Therefore, patients should be carefully selected and monitored for potential side effects. Overall, the benefits of roflumilast therapy outweigh the risks for patients with severe COPD and a history of exacerbations, and it is a valuable addition to a comprehensive COPD management plan.
From the FDA Drug Label
Roflumilast tablet is a selective phosphodiesterase 4 inhibitor indicated as a treatment to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. The main use of roflumilast is to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations 2. Key points about roflumilast include:
- It is a selective phosphodiesterase 4 inhibitor
- It is not a bronchodilator and is not indicated for the relief of acute bronchospasm
- The starting dose is 250 mcg for the first 4 weeks of treatment only, and is not the effective (therapeutic) dose 2.
From the Research
Roflumilast Overview
- Roflumilast is a selective phosphodiesterase 4 inhibitor used for the maintenance treatment of severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis and a history of exacerbations 3, 4, 5, 6, 7.
- It is available in 500-μg tablets to be administered once daily, offering an advantage over inhaler therapy as an oral tablet 3.
Efficacy
- Roflumilast has been shown to improve lung function and reduce exacerbations in patients with severe COPD, especially those with chronic bronchitis, frequent exacerbations, or who require frequent rescue inhaler therapy 3, 4, 5, 6.
- Clinical efficacy has been demonstrated in patients receiving roflumilast alone as well as those receiving concomitant inhaled long-acting β2-agonist (LABA) therapy 5.
- The greatest benefit of roflumilast was observed in patients with moderate-to-severe COPD associated with chronic bronchitis and a recent history of exacerbations 4.
Safety and Adverse Events
- Common adverse events associated with roflumilast include diarrhea, nausea, headache, and weight loss 3, 4, 5, 6.
- Roflumilast has also been associated with an increased risk of neuropsychiatric abnormalities and dose-limiting weight loss 4.
- Serious adverse events, including suicide-related adverse effects, have been reported in patients receiving roflumilast 6.
Patient Selection and Management
- Clear identification of patients eligible for roflumilast will require improved characterization and phenotyping of patients in primary care, including lung function measurement, accurate health status classification, and recording of chronic cough and regular sputum production 7.
- Roflumilast is currently licensed in Europe and is indicated as maintenance treatment in severe COPD associated with chronic bronchitis in adult patients with a history of frequent exacerbations as an add-on to bronchodilator treatment 3, 7.