Roflumilast is used as an add-on anti-inflammatory in severe COPD with frequent exacerbations. Its mechanism involves inhibition of:

• A Phosphodiesterase-4 (PDE-4) in lung inflammatory cells, increasing intracellular cAMP and attenuating neutrophil and macrophage activation ✓
• B Leukotriene D4 receptors (CysLT1) in bronchial smooth muscle
• C 5-Lipoxygenase, blocking leukotriene synthesis
• D IL-5 receptor on eosinophils, reducing eosinophilic inflammation

Explanation

Roflumilast is a selective phosphodiesterase-4 (PDE-4) inhibitor. PDE-4 is the principal cAMP-degrading enzyme in immune and inflammatory cells (neutrophils, macrophages, T-cells, dendritic cells); its inhibition elevates intracellular cAMP, suppressing inflammatory mediator release (TNF-alpha, IL-8, LTB4) in the COPD airway. It is an oral agent indicated for severe COPD (FEV1 <50% predicted) with a chronic bronchitis phenotype and frequent exacerbations, taken alongside standard long-acting bronchodilators. Montelukast blocks CysLT1; zileuton inhibits 5-LOX; mepolizumab/benralizumab target IL-5/IL-5R (eosinophil-driven asthma).

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.