Selective phosphodiesterase-4 (PDE-4) inhibitor
ATC code: R03DX07 (Roflumilast)
Brand names
Daxas, Daliresp
A selective phosphodiesterase-4 inhibitor mainly expressed in pulmonary inflammatory cells (neutrophils, T-lymphocytes, eosinophils, macrophages). Increases intracellular cAMP, suppressing release of pro-inflammatory cytokines and chemokines. Effect develops over weeks – not a bronchodilator but an anti-inflammatory drug. CYP1A2- and CYP3A4-metabolized to active roflumilast N-oxide (30-hour half-life enables once-daily dosing).
Second line
Add-on therapy in severe COPD with frequent-exacerbator chronic bronchitis phenotype per 2024. Dose 500 mcg once daily. REACT and RE2SPOND showed 15–20% reduction in exacerbations in patients on triple inhaled therapy (LABA + LAMA + ICS). Not used as monotherapy or replacement for inhaled foundation therapy. Often poorly tolerated due to nausea, diarrhea, and weight loss.
Only in patients with severe COPD (FEV1 below 50%), chronic bronchitis, and frequent exacerbations.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Roflumilast is a selective phosphodiesterase-4 (PDE4) inhibitor. It is prescribed for severe COPD with a frequent-exacerbation phenotype and chronic bronchitis ( 2024, AEMPS Ficha Técnica). In biohacker circles, roflumilast is occasionally promoted to suppress chronic inflammation and for anti-aging. In healthy adults, no clinical studies of such use exist. The drug has serious risks: pronounced weight loss (5-10% of baseline), GI disturbances (nausea, diarrhea, abdominal pain), neuropsychiatric adverse effects (insomnia, anxiety, depression, suicidal ideation – warning), and sleep disturbances. If roflumilast was recommended to a healthy person, seek a second opinion immediately.
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Contraindicated. Stop in advance when planning pregnancy.
Contraindicated during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Roflumilast is evaluated for the following indications with varying evidence strength: Severe COPD with emphysema and frequent exacerbations (evidence tier B), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Roflumilast (≥ 1 in 100): Diarrhea (10–20%), Nausea, Weight loss (mean 2–3 kg), Headache, Insomnia, Reduced appetite. See the Safety section for uncommon and serious reactions.
FDA category C. Contraindicated. Stop in advance when planning pregnancy.
Contraindicated during lactation.
Roflumilast is contraindicated in: Roflumilast hypersensitivity; Severe hepatic impairment (Child-Pugh B or C); History of depression or suicidal ideation; Severe immunological diseases (multiple sclerosis, SLE, progressive multifocal leukoencephalopathy); Acute infections. Full list in the Safety section.