Generic
Roflumilast
12 brands available in the market
At a glance
Roflumilast is a PDE-4 inhibitor used to reduce exacerbations and symptoms of chronic obstructive pulmonary disease (COPD). It relaxes airway muscles and reduces inflammation by increasing cAMP in lung tissue, making breathing easier.
Description
Roflumilast is a selective phosphodiesterase-4 (PDE-4) inhibitor that increases intracellular cyclic adenosine monophosphate (cAMP) in lung tissue. Elevated cAMP reduces inflammatory cell activity and relaxes airway smooth muscles, decreasing COPD exacerbations and symptoms.
Indications
- Chronic Obstructive Pulmonary Disease (COPD) – reduction of exacerbations and symptoms
Therapeutic class
COPD Medications
Pharmacological class
Phosphodiesterase-4 (PDE-4) Inhibitor
Pharmacology
Roflumilast selectively inhibits PDE-4, preventing cAMP breakdown and increasing intracellular cAMP in inflammatory cells (macrophages, neutrophils, eosinophils). This reduces the release of inflammatory mediators and relaxes airway smooth muscles, decreasing inflammation, bronchoconstriction, and COPD exacerbations.
Mechanism of action
Inhibits PDE-4 enzyme, increasing cAMP in lungs, reducing inflammation and relaxing airways.
Dosage
Adult Dose (Oral):
- COPD (exacerbation reduction): 500 mcg (0.5 mg) once daily
Administration
- Take with or without food (fixed time is better)
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as possible; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Headache
- Weight loss
- Dizziness
- Insomnia
- Back pain
- Nausea and diarrhea
- Decreased appetite and flu-like symptoms
Precautions & warnings
- Not for acute bronchospasm (sudden breathing attacks)
- Do not use in history of depression or suicidal thoughts/behavior
- Discontinue if unexplained and significant weight loss occurs
- Usually does not affect driving ability; avoid if dizzy
- Do not use in serious diseases like HIV, multiple sclerosis, lupus
Contraindications
- Hypersensitivity to roflumilast or any component
- Moderate to severe hepatic impairment (Child-Pugh B/C)
Drug interactions
- Erythromycin, ketoconazole, fluvoxamine: CYP1A2/3A4 inhibitors increase roflumilast levels
- Rifampicin, phenobarbital, carbamazepine: CYP1A2/3A4 inducers decrease efficacy
- Theophylline, oral contraceptives: Possible interactions
Food interactions
It is not known whether alcohol is safe with Roflumilast; consult your doctor.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; use only if clearly needed; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably unsafe; limited data suggests drug may pass into breast milk and harm the baby; consult your doctor.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
Caution required in elderly patients; dose adjustment may be needed.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; no dose adjustment needed; consult your doctor.
Hepatic Impairment: Caution in mild liver disease; dose adjustment may be needed; avoid in moderate-severe liver disease; consult your doctor.
Overdose effects
Limited overdose information; excessive doses may increase side effects; consult your doctor.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Roflumilast