Roflumilast
DALIRESP
Pronunciation: roe-FLOO-mi-last (DA-li-resp)
What it isSelective PDE4 inhibitor with anti-inflammatory action; severe COPD with chronic bronchitis and exacerbations.
Why this oneIt reduces exacerbations in the chronic bronchitis phenotype, which bronchodilators alone do not.
What limits itWeight loss, diarrhea and psychiatric effects limit tolerability. It is not a bronchodilator and does nothing acutely.
Pearls
- Add-on only after maximal LABA/LAMA/ICS
- Does not improve symptoms or quality of life
- Start 250 mcg daily for 4 weeks to improve tolerance
- Topical roflumilast treats plaque psoriasis
Roflumilast prescription history
Animated chart of estimated U.S. prescriptions per year, Asthma/COPD meds (1924–2026). Roflumilast enters in 2011 (estimated).
FDA-approved for
- COPD (2011)
Principal riskWeight loss and psychiatric effects
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityDiarrhea, weight loss and psychiatric effects including suicidality; monitor weight and mood.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Reduce risk of COPD exacerbations | Adults | 250 mcg QD x 4 weeks (to improve tolerability), then 500 mcg QD | 500 mcg QD | 500 mcg QD |
Renal No dosage adjustment needed
Hepatic Mild (Child-Pugh A): weigh risk-benefit; contraindicated in moderate-severe (Child-Pugh B or C)
250 mcg is a starting/tolerability dose only and is not the effective (therapeutic) dose
Instructions
- Take once daily with or without food
- Not a bronchodilator - do not use for relief of acute bronchospasm
- Avoid strong CYP450 inducers (rifampicin, phenobarbital, carbamazepine, phenytoin)
Available strengths
- tab 250, 500 mcg
- cream 0.05, 0.15, 0.3 %
- foam 0.3 %
Contraindications
- Moderate to severe liver impairment (Child-Pugh B or C)
Cautions
- Psychiatric events including suicidality - weigh risk in patients with depression/suicidal history
- Weight decrease - monitor weight; evaluate and consider discontinuation if clinically significant loss
- Not for acute bronchospasm
- Use with strong CYP450 inducers not recommended
Adverse reactions
- Diarrhea
- Weight decrease
- Nausea
- Headache
- Back pain
- Influenza
- Insomnia
- Dizziness
- Decreased appetite
Pregnancy No human data; should not be used during labor and delivery; animal adverse effects at high multiples of MRHD.
Lactation Excretion into human milk probable; should not be used while nursing.
Cost
Generic entry2018
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Self-check
- Roflumilast: Which COPD phenotype benefits?
Chronic bronchitis with exacerbations. - Roflumilast: Is it an acute bronchodilator?
No.