Pharmacology · Respiratory and GIT Pharmacology

Roflumilast is used as an add-on therapy in severe COPD. Its mechanism is:

  • A Selective phosphodiesterase-4 (PDE4) inhibitor that increases intracellular cAMP in airway smooth muscle and inflammatory cells, reducing inflammation and bronchoconstriction
  • B Long-acting beta-2 agonist with 24-hour bronchodilation
  • C Leukotriene receptor antagonist (CysLT1 blockade), reducing eosinophilic airway inflammation
  • D Inhibitor of mast cell tryptase, preventing histamine release in COPD exacerbations
Correct answer: A. Selective phosphodiesterase-4 (PDE4) inhibitor that increases intracellular cAMP in airway smooth muscle and inflammatory cells, reducing inflammation and bronchoconstriction

Explanation

Roflumilast is an oral selective PDE4 inhibitor. PDE4 is the predominant phosphodiesterase isoform in airway smooth muscle cells, neutrophils, macrophages, and T-cells in COPD. By inhibiting PDE4, roflumilast raises cAMP, reducing pro-inflammatory mediator release, neutrophil activation, and smooth muscle tone. It is indicated as add-on in severe COPD with frequent exacerbations and chronic bronchitis despite dual/triple inhaler therapy.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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