Uses

Roflumilast is a selective phosphodiesterase-4 (PDE4) inhibitor indicated to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. It is not a bronchodilator and is not indicated for acute bronchospasm.

Do not use if

Contraindicated in patients with moderate to severe liver impairment (Child-Pugh B or C). Avoid in patients with a history of depression or suicidality.

Side effects

The most common adverse effects include diarrhea, weight decrease, nausea, headache, back pain, influenza, insomnia, dizziness, and decreased appetite. Psychiatric events including suicidal ideation have been reported.

Warnings

Monitor for psychiatric symptoms including worsening of depression, insomnia, anxiety, and suicidal thoughts; inform patients, caregivers, and families. Unexplained weight loss should be evaluated. Not for use in acute bronchospasm. Use with caution in patients with a low body weight.

How it works

Roflumilast and its active N-oxide metabolite selectively inhibit PDE4, the major enzyme metabolizing cyclic AMP in lung tissue. This leads to accumulation of intracellular cyclic AMP, which suppresses the activity of inflammatory cells such as neutrophils and macrophages, reducing pulmonary inflammation.

Storage

Store at room temperature (20–25°C). Keep away from moisture and light.