Pulmonology

Theophylline & Roflumilast song

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Theophylline & Roflumilast

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Key points in this song10

Theophylline is a nonselective phosphodiesterase (PDE) inhibitor that increases cAMP, causing bronchodilation and mild anti-inflammatory effects, used as a third-line agent in COPD and asthma.
Theophylline has a narrow therapeutic index (target serum level 5–15 mcg/mL); toxicity causes seizures, arrhythmias, nausea, and vomiting.
Theophylline is metabolized by CYP1A2; levels are increased by cimetidine, fluoroquinolones, and macrolides, and decreased by rifampin, phenytoin, and smoking.
Adenosine receptor antagonism by theophylline contributes to its CNS stimulant effects and explains why caffeine (a methylxanthine) shares a similar mechanism.
Roflumilast is a selective PDE-4 inhibitor that reduces cAMP breakdown specifically in inflammatory cells, providing anti-inflammatory effects without direct bronchodilation.
Roflumilast is indicated for severe COPD (FEV1 <50% predicted) with a chronic bronchitis phenotype and frequent exacerbations, used as an add-on to bronchodilators.
Key adverse effects of roflumilast include weight loss, diarrhea, nausea, and neuropsychiatric effects (depression, suicidal ideation), requiring caution in patients with psychiatric history.
Unlike theophylline, roflumilast does not require serum level monitoring and has no significant bronchodilatory effect on its own.
Both theophylline and roflumilast reduce COPD exacerbation frequency but are never first-line; LABAs and LAMAs remain the preferred maintenance agents.
Theophylline toxicity is managed with supportive care, activated charcoal for acute ingestion, and hemodialysis in severe cases; beta-blockers can control tachyarrhythmias cautiously.