Buy Roflumilast
Roflumilast

1.04
A maintenance treatment used to reduce flare-ups of severe COPD in adults.


Ingredient
Availability
In Stock
Delivery
Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Alternative/Local Brand
Daxas
Active Ingredient(s)
Roflumilast
Primary Category
COPD Treatment
Therapeutic Class
Drugs for obstructive airway diseases, Phosphodiesterase 4 inhibitors
Pharmacological Class
PDE4 inhibitor
Indications
Severe Chronic Obstructive Pulmonary Disease (COPD), Chronic bronchitis
Contraindications
Moderate to severe liver impairment, Hypersensitivity to roflumilast
Minor Side Effects
Decreased appetite, Diarrhoea, Headache
Moderate Side Effects
Weight loss, Nausea, Abdominal pain, Sleep disturbances
Serious Side Effects
Suicidal ideation, Anxiety, Severe weight loss, Angioedema
Dosage Forms
Tablet
Administration Route
Oral
Mechanism of Action
Roflumilast is a non-steroid, anti-inflammatory drug that works by inhibiting the enzyme PDE4. By doing so, it reduces the inflammation in the lungs that causes the narrowing of airways in patients with COPD and chronic bronchitis.
Prescription Status
Rx
Manufacturer
AstraZeneca UK Ltd
Patient Summary
A maintenance treatment used to reduce flare-ups of severe COPD in adults.
Onset Time
Full effect may take several weeks
Duration
Daily long-term use
Storage Instructions
No special storage conditions
Drug Interactions
Rifampicin, Phenobarbital, Carbamazepine, Theophylline
Age Restrictions
Adults over 18
Pregnancy Use
Not recommended during pregnancy or breastfeeding.
Alternative Drugs
Theophylline, Salmeterol, Tiotropium

Roflumirast: Generic Medication Overview

Roflumirast is a respiratory-health medication classified as a phosphodiesterase-4 (PDE4) inhibitor. It is available as a single-strength pill containing 500 mg of the active ingredient roflumirast. In Hong Kong, roflumirast is a prescription-only product regulated by the Hong Kong Department of Health, Medicines Division. The drug is marketed under a variety of generic names and may appear in different branding depending on the manufacturer.

How Roflumirast Works in the Body

Roflumirast belongs to the class of PDE4 inhibitors. PDE4 is an enzyme that breaks down cyclic adenosine monophosphate (cAMP) inside inflammatory cells of the airways. By blocking PDE4, roflumirast raises intracellular cAMP levels, which leads to:

  • Reduced release of pro-inflammatory cytokines (such as TNF-α, IL-6, and IL-8)
  • Decreased activation of neutrophils and eosinophils
  • Diminished airway inflammation and mucus hyper-secretion

These actions collectively help improve lung function and reduce the frequency of exacerbations in chronic respiratory conditions. The onset of anti-inflammatory effect typically occurs within days, with the full therapeutic benefit developing over several weeks of daily use. Roflumirast is administered orally, and its bioavailability is high; it is metabolised primarily by the liver via the CYP3A4 pathway and excreted in the urine and feces.

Treating Chronic Obstructive Pulmonary Disease with Roflumirast

Roflumirast is approved in Hong Kong for the maintenance treatment of severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis. It is intended for patients who experience frequent exacerbations despite standard inhaled therapies (such as long-acting bronchodilators). The medication is not a rescue inhaler; rather, it is used on a long-term basis to lessen the inflammatory component of COPD.

Typical patients who may benefit include adults with:

  • A history of two or more COPD exacerbations per year
  • Persistent symptoms despite optimal inhaled therapy
  • No contraindications to PDE4 inhibition

Roflumirast does not replace bronchodilator or inhaled corticosteroid treatment; it is an add-on therapy aimed at further reducing exacerbation risk.

Patient Suitability and Contraindications

Who Should Consider Roflumirast?

  • Adults with severe COPD and chronic bronchitis phenotype
  • Individuals whose disease remains unstable despite maximal inhaled therapy
  • Patients who can be monitored for potential side effects such as gastrointestinal discomfort or weight loss

Absolute Contraindications

  • Known hypersensitivity to roflumirast or any of its excipients
  • Severe liver impairment (Child-Pugh C)
  • Pregnancy (category not recommended)

Relative Contraindications

  • Moderate hepatic impairment (Child-Pugh B) - dose adjustment may be required
  • History of depression or suicidal ideation - patients should be closely observed
  • Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) - may increase plasma concentrations

Special Populations

  • Pregnancy & Lactation: Roflumirast is not recommended; benefit-risk must be evaluated by a specialist.
  • Elderly: Caution due to higher likelihood of hepatic dysfunction and polypharmacy.
  • Renal Impairment: No specific dose adjustment is required, but monitoring is advised.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Nausea, diarrhea, or abdominal discomfort (frequently reported)
  • Decreased appetite leading to weight loss
  • Headache and insomnia

These effects are usually mild to moderate and often improve with continued therapy or dose titration.

Serious Adverse Events

  • Severe depression, suicidal thoughts, or mood changes - immediate medical evaluation required
  • Significant hepatic enzyme elevation - monitor liver function tests (LFTs) regularly
  • Allergic reactions such as rash or angioedema - discontinue and seek urgent care

Drug Interactions

  • Major: Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) can raise roflumirast levels, increasing the risk of adverse reactions.
  • Moderate: CYP3A4 inducers (e.g., rifampin, carbamazepine) may reduce efficacy.
  • Pharmacodynamic: Caution when combined with other medications that depress the central nervous system or affect mood.

Patients should provide a complete medication list-including over-the-counter drugs, supplements, and herbal products-to their healthcare provider before initiating roflumirast.

Food and Lifestyle Interactions

  • Roflumirast can be taken with or without food; however, taking it with meals may lessen gastrointestinal upset.
  • Alcohol does not have a direct interaction but may exacerbate central nervous system side effects.
  • No specific restrictions on driving, but patients experiencing severe nausea or dizziness should exercise caution.

How to Take Roflumirast

  • Standard dosing: One 500 mg tablet taken once daily, preferably at the same time each day.
  • Dose adjustments: In patients with moderate hepatic impairment, a lower dose (e.g., 250 mg) may be considered under specialist supervision.
  • Administration: Swallow the tablet whole with a full glass of water. Do not crush, chew, or split the tablet unless instructed by a pharmacist.
  • Missed dose: If a dose is missed, take it as soon as remembered unless the next scheduled dose is near; do not double the dose.
  • Overdose: Symptoms may include severe nausea, vomiting, and marked dizziness. Seek emergency medical care; supportive care and monitoring are the mainstays of treatment.
  • Discontinuation: Abrupt cessation is generally safe, but patients should discuss tapering with a clinician if they have experienced significant side effects.

Monitoring and Follow-Up

  • Liver Function Tests (LFTs): Baseline and periodic monitoring (e.g., every 3-6 months) are recommended, especially in patients with hepatic risk factors.
  • Weight and Nutritional Status: Assess at each visit to detect unintended weight loss early.
  • Mental Health Screening: Evaluate for depression or mood changes at regular intervals.
  • COPD Exacerbation Frequency: Document number and severity of exacerbations to gauge therapeutic benefit.

If any concerning laboratory abnormalities or clinical symptoms arise, timely communication with the prescribing clinician is essential.

Storage and Handling

  • Store the tablets at room temperature (15-30 °C), away from excess moisture and direct sunlight.
  • Keep the medication out of reach of children; use child-proof containers when available.
  • Do not use the product beyond the expiration date printed on the pack.
  • For disposal, follow local Hong Kong pharmacy take-back programs or community waste guidelines.

Medication-Specific Glossary

Phosphodiesterase-4 (PDE4) Inhibitor
A drug class that blocks the PDE4 enzyme, increasing intracellular cAMP and reducing inflammatory cell activity in the airways.
cAMP (Cyclic Adenosine Monophosphate)
A second messenger involved in cellular signaling; higher levels in inflammatory cells lead to reduced release of pro-inflammatory mediators.
Child-Pugh Score
A scoring system that assesses the severity of chronic liver disease, guiding dose adjustments for hepatically cleared medications.
QT Prolongation
An extension of the QT interval on an electrocardiogram, which can predispose to irregular heart rhythms; a rare concern with PDE4 inhibitors.

Medical Disclaimer

This article provides educational information about roflumirast and is not a substitute for professional medical advice. Treatment decisions, including the use of unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Roflumilast FAQ

What form does roflumirast come in?

Roflumirast is supplied as a single-strength oral pill containing 500 mg of the active ingredient. The tablet is typically white to off-white and may have a scored line for easy handling, though it is not intended to be split.

Can roflumirast be used for asthma?

Roflumirast is approved specifically for severe COPD with chronic bronchitis. Its use in asthma is not endorsed by regulatory agencies in Hong Kong and should only be considered within a clinical trial or under specialist supervision.

Will roflumirast appear on a drug test for work or sports?

Roflumirast is not classified as a prohibited substance by most occupational or sports drug-testing programs. However, athletes should verify with their governing bodies, as policies may change.

How does roflumirast differ from inhaled corticosteroids?

Unlike inhaled corticosteroids, which act locally in the lungs, roflumirast works systemically by inhibiting an enzyme that reduces airway inflammation. It is used as an add-on therapy when inhaled treatments alone are insufficient.

What should I do if I experience severe nausea?

If nausea becomes persistent or severe, contact your healthcare provider. They may advise taking the medication with food, adjusting the dose, or prescribing an anti-emetic.

Is it safe to take roflumirast with antifungal medications?

Strong CYP3A4 inhibitors such as certain antifungals (e.g., ketoconazole) can increase roflumirast levels and heighten side-effect risk. Discuss any antifungal therapy with your prescriber before combining them.

Can I travel internationally with roflumirast?

Yes, but keep the medication in its original packaging with a copy of the prescription. Some countries may require additional documentation for prescription drugs, so check local regulations before travel.

Does roflumirast have any impact on blood sugar?

Current evidence does not indicate a direct effect on glucose metabolism, but patients with diabetes should monitor their blood sugar regularly, as systemic inflammation changes can influence control.

What are the most common reasons for discontinuing roflumirast?

The leading reasons include intolerable gastrointestinal side effects, significant weight loss, or emergence of depressive symptoms. Any decision to stop should be made together with a healthcare professional.

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