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Roflumilast

PharmacologyRespiratoryImmune

Summary

Selective phosphodiesterase-4 (PDE-4) inhibitor used as add-on therapy in severe COPD with chronic bronchitis phenotype and history of exacerbations. Reduces inflammation by increasing intracellular cAMP in immune cells.

Detail

Roflumilast inhibits PDE-4, the dominant phosphodiesterase in inflammatory cells, increasing cAMP and dampening neutrophilic inflammation characteristic of COPD. It is indicated as add-on to bronchodilator therapy in severe COPD patients with chronic bronchitis and frequent exacerbations; it does not acutely bronchodilate. Key adverse effects include weight loss, diarrhea, nausea, headache, and psychiatric effects (mood disturbance, depression, suicidality). It is contraindicated in moderate-to-severe hepatic impairment. Boards association: PDE-4 inhibitor for COPD exacerbation prevention (contrast with cilostazol = PDE-3 for PAD).

Sources

  • First Aid for USMLE Step 1 2024
  • Sketchy Pharmacology

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Related pharmacology terms

Roflumilast — Medical Glossary