From the Guidelines
Roflumilast is a phosphodiesterase-4 (PDE4) inhibitor used to treat severe chronic obstructive pulmonary disease (COPD) in patients with chronic bronchitis who have frequent exacerbations, as evidenced by the most recent and highest quality study 1. Roflumilast is available under brand names like Daliresp and Daxas, typically prescribed as a 500 microgram tablet taken once daily. It works differently from other COPD medications as it reduces inflammation in the lungs rather than directly opening airways.
Key Points
- It's not a rescue medication for sudden breathing problems but works over time to reduce COPD flare-ups.
- Common side effects include diarrhea, weight loss, nausea, headache, and back pain.
- Some patients experience mood changes including depression.
- Roflumilast is usually added to other COPD treatments like bronchodilators when those medications alone aren't providing adequate control of symptoms and exacerbations.
- The medication works by blocking an enzyme that contributes to inflammation, thereby reducing the inflammatory response that worsens COPD symptoms, as supported by studies 1.
Patient Selection
Patients who have COPD with severe or very severe airflow obstruction, symptoms of chronic bronchitis, and exacerbations despite optimal inhaled therapy are suggested to be treated with roflumilast to prevent future exacerbations, according to the European Respiratory Society/American Thoracic Society guideline 1.
Adverse Effects
The adverse effects of roflumilast may include premature treatment discontinuation due to adverse effects, diarrhea, nausea, weight loss, psychiatric disorders including anxiety and depressive symptoms, and sleep disturbance/insomnia, as reported in studies 1.
Mortality and Cardiovascular Events
There is no significant difference in mortality or cardiovascular events between roflumilast and placebo groups, as shown in the study 1.
From the FDA Drug Label
ROFLUMILAST tablets, for oral use 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.
Roflumilast is a selective phosphodiesterase 4 inhibitor used to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations 2.
From the Research
Definition and Mechanism of Roflumilast
- Roflumilast is a phosphodiesterase-4 inhibitor that targets the systemic inflammation associated with chronic obstructive pulmonary disease (COPD) 3, 4, 5, 6, 7.
- It has anti-inflammatory effects, including decreasing inflammatory mediators and the expression of cell surface markers, and inhibition of apoptosis 7.
Efficacy of Roflumilast in COPD
- Roflumilast has been shown to improve lung function, including increases in mean pre- and postbronchodilator forced expiratory volume in 1 second (FEV1) and forced vital capacity 3, 4, 5, 6, 7.
- It reduces the frequency of moderate to severe exacerbations, with the benefit most well established in patients with severe disease 3, 4, 5, 6, 7.
- Roflumilast has been shown to suppress airway inflammation, which may contribute to its beneficial effect on COPD 6.
Safety and Tolerability of Roflumilast
- Roflumilast is generally well tolerated, with common adverse events including diarrhea, nausea, and headache 3, 4, 5, 6.
- It has been associated with an increased risk of neuropsychiatric abnormalities and dose-limiting weight loss 4.
- The majority of patients do not discontinue treatment due to adverse events, although a significant proportion may experience serious adverse events 5.