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roflumilast

Phosphodiesterase 4 (PDE4) inhibitor · Anti-inflammatory

Phosphodiesterase 4 (PDE4) inhibitorAnti-inflammatory
CDSCO approved
EXCRETION
not curated
INTERACTIONS
1 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 3
  • CladribineSevereDatabaseDDInter

Mechanism

Roflumilast is an oral nonselective PDE4 inhibitor, extensively metabolized to its more active and long-acting N-oxide metabolite. It inhibits PDE4, which is the predominant PDE isoform in various inflammatory cells (mast cells, eosinophils, neutrophils, T lymphocytes, macrophages) and structural cells (sensory nerves, epithelial cells). PDE4B inhibition is particularly important for its anti-inflammatory effects.

Indications

Severe COPD with chronic bronchitis (add-on to triple inhaled therapy, for patients who continue to have exacerbations)Mild asthma (improvement in FEV1 similar to an ICS)Moderate to severe asthma (add-on to montelukast)Predominantly neutrophilic inflammationReduced exacerbation frequency in patients with severe COPD, chronic bronchitis, and a prior history of exacerbations

Pharmacokinetics

Bioavailability
~80%
Protein binding
Active metabolite is long-acting
Metabolism
Extensively metabolized by CYPs 3A4 and 1A2 to N-oxide active metabolite

Side effects

Common
DiarrheaHeadachesNauseaWeight loss

Drug interactions

Cladribine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cyp4a3 Inhibitors Inducers
Moderate
Textbook

Potential alteration of roflumilast plasma levels, leading to increased adverse effects or reduced efficacy.

Monitoring for efficacy or side effects and dose adjustment may be necessary if CYP4A3 inhibitors or inducers are co-administered.

Source: G&G 14e · p895

Enoxacin
Moderate
Database

Enoxacin will increase the area under the curve (AUC) for roflumilast, potentially leading to increased side effects.

Monitor for increased adverse effects of roflumilast; dose adjustment may be necessary.

Source: DDInter

9 additional low-confidence interactions hidden — those rows lack a documented mechanism or management plan in our sources.

Related guidelines

Ask House about roflumilast

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team