roflumilast: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
roflumilast: clinical details
Prescribing considerations
- Confirm adult severe COPD with chronic bronchitis and frequent exacerbations despite bronchodilator treatment.
- Roflumilast is maintenance treatment, not an acute bronchodilator.
- Assess baseline weight, liver impairment, psychiatric history, interacting medicines and pregnancy potential.
- Reassess persistent gastrointestinal effects, headache, insomnia or other intolerability.
- Relevant experience is lacking in severe immunological or acute infectious disease, most cancers, long-term immunosuppression and advanced congestive heart failure.
Contraindications and cautions
- Hypersensitivity to roflumilast or a formulation excipient.
- Moderate or severe hepatic impairment.
- The selected product contains lactose and is unsuitable for specified rare hereditary disorders of galactose handling.
- A history of depression associated with suicidal ideation or behaviour is a strong product-specific reason not to use roflumilast.
Monitoring
- Check underweight patients at each visit and advise regular self-monitoring of weight; stop and investigate unexplained, clinically concerning loss.
- Monitor for insomnia, anxiety, depression, behavioural change and suicidal ideation, particularly early in treatment.
- Review persistent diarrhoea, nausea, abdominal pain or headache and reassess benefit versus tolerability.
- Review continued suitability if severe infection, immunological disease, cancer or significant psychiatric symptoms develop.
Clinical pharmacology
Roflumilast and its active N-oxide metabolite inhibit PDE4. Metabolism involves CYP1A2 and CYP3A4; the N-oxide metabolite is the principal contributor to total in-vivo PDE4 inhibitory activity. Food does not change total PDE4 inhibition.
Formulation and product differences
- The selected product is a yellow, D-shaped film-coated tablet containing lactose monohydrate.
- It is an oral systemic treatment rather than an inhaled bronchodilator.
roflumilast preparations and strengths
Tablet
Route: Oral
Strengths: 250 micrograms, 500 micrograms
roflumilast interactions
Check all prescribed, over-the-counter and herbal products with a pharmacist or prescriber. Important examples include:
Rifampicin, phenobarbital, carbamazepine or phenytoin
These strong enzyme inducers can substantially reduce roflumilast exposure and effectiveness, so combined treatment is not recommended.
Fluvoxamine, cimetidine or enoxacin
These medicines can increase roflumilast exposure and make persistent adverse effects more likely, requiring treatment reassessment.
Theophylline
Combined use for maintenance treatment is not recommended because supporting clinical evidence is lacking.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.