Formulary
Roflumilast: Indications, Dosing, Side Effects and Interactions
Roflumilast is a phosphodiesterase type-4 inhibitor with anti-inflammatory properties.
MedNext Academy | 3 min read
Roflumilast: Indications, Dosing, Side Effects and Interactions
Roflumilast is a phosphodiesterase type-4 inhibitor with anti-inflammatory properties.
Drug action
Roflumilast is a phosphodiesterase type-4 inhibitor with anti-inflammatory properties.
Indications and dose
**Adjunct to bronchodilators**
- **Adult** (By Mouth): for the maintenance treatment of patients with severe chronic obstructive pulmonary disease associated with chronic bronchitis and a history of frequent exacerbations Initially 250 micrograms once daily for 28 days, then maintenance 500 micrograms once daily.
Cautions
History of psychiatric illness (discontinue if new or worsening psychiatric symptoms occur); latent infection (such as tuberculosis, viral hepatitis, herpes infection)
Contraindications
Cancer (except basal cell carcinoma); concomitant treatment with immunosuppressive drugs (except short-term systemic corticosteroids); history of depression associated with suicidal ideation or behaviour; moderate to severe cardiac failure; severe acute infectious disease; severe immunological disease
Side effects
Common or very common Appetite decreased; diarrhoea; gastrointestinal discomfort; headache; insomnia; nausea; weight decreased Uncommon Anxiety; asthenia; back pain; dizziness; gastrointestinal disorders; malaise; muscle complaints; muscle weakness; palpitations; skin reactions; tremor; vertigo; vomiting Rare or very rare Angioedema; constipation; depression; gynaecomastia; haematochezia; respiratory tract infection; suicidal behaviours; taste altered
Interactions
**Other interactions (13):**
- A major step in roflumilast metabolism is the N-oxidation of roflumilast to roflumilast N-oxide by CYP3A4 and CYP1A2.
- Both roflumilast and roflumilast N-oxide have intrinsic phosphodiesterase-4 (PDE4) inhibitory activity.
- Therefore, following administration of roflumilast, the total PDE4 inhibition is considered to be the combined effect of both roflumilast and roflumilast N-oxide.
- Interaction studies with CYP1A2/3A4 inhibitor enoxacin and the CYP1A2/2C19/3A4 inhibitors cimetidine and fluvoxamine, resulted in increases of the total PDE4 inhibitory activity of 25%, 47% and 59%,...
- A combination of roflumilast with these active substances might lead to an increase of exposure and persistent intolerability.
- In this case, roflumilast treatment should be reassessed (see section 4.4).
Pregnancy
Manufacturer advises avoid-toxicity in animal studies.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises caution in mild impairment; avoid in moderate to severe impairment.
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
Inside MedNext for this topic
- 411 MedNext-authored chapters
- 80,000+ MCQ bank
- 15 study modes
- Growing visual cheat sheets
Study modes
- Notes
- MCQ
- Audio
- Video
- Visual
- 3D Anatomy
- Trace
- Flashcards
- Mnemonics
- Image Bank
- Clinical
- Microscopy
- Audio QBank
- Cadaver
- Book Match
Continue reading
Subject HubPharmacology Hub
All pharmacology resources in one place.
Drug SchedulesIndian Drug Schedules
Schedule H, H1, X and G classifications.
FormularyBrowse all drugs
Search 1,850+ drug profiles.
Study Roflumilast in the MedNext app
Challenge yourself with targeted pharmacology MCQs on this drug class. Every explanation links back to the chapter that teaches the concept.
Start drug challengeExplore the full formulary

