Roflumilast 250mcg (blster Pk) Tabs
It is used to treat COPD (chronic obstructive pulmonary disease).Do not use this drug to treat intense flare-ups of shortness of breath. Use a rescue inhaler. If you have questions, talk with the doctor.
Drug Class
Selective Phosphodiesterase-4 (PDE4) Inhibitor
Pharmacologic Class
Anti-inflammatory agent, PDE4 inhibitor
Pregnancy Category
C
FDA Approved
Mar 2011
DEA Schedule
Not Controlled
Overview
What is this medicine?
Roflumilast is a medication used to reduce the frequency of flare-ups (exacerbations) and improve lung function in people with severe chronic obstructive pulmonary disease (COPD) associated with chronic bronchitis and a history of exacerbations. It works by reducing inflammation in the lungs. It is not for sudden breathing problems.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding bathrooms. Keep all medications in a secure location, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs for a safe and environmentally friendly way to dispose of your medications.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, it's essential to take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding bathrooms. Keep all medications in a secure location, out of reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs for a safe and environmentally friendly way to dispose of your medications.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Continue all other prescribed COPD medications (e.g., bronchodilators, inhaled corticosteroids) as directed by your doctor.
- Roflumilast is not a bronchodilator and will not relieve sudden breathing problems.
- Do not stop smoking; however, smoking cessation is strongly encouraged for overall COPD management.
- Report any new or worsening mood changes, thoughts of self-harm, or unexplained weight loss to your doctor immediately.
- Take the medication exactly as prescribed, usually once daily. Do not crush, chew, or break the tablet.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
500 mcg orally once daily
Dose Range:
250 - 500 mg
Condition-Specific Dosing:
COPD maintenance:
500 mcg orally once daily. For patients experiencing intolerable side effects, an initial dose of 250 mcg orally once daily for 4 weeks may be used, then increased to 500 mcg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed; not significantly removed by dialysis
Hepatic Impairment:
Mild:
No adjustment (Child-Pugh A)
Moderate:
250 mcg orally once daily (Child-Pugh B)
Severe:
Contraindicated (Child-Pugh C)
Pharmacology
Mechanism of Action
Roflumilast and its active metabolite (roflumilast N-oxide) are selective inhibitors of phosphodiesterase 4 (PDE4). PDE4 is the predominant PDE in inflammatory and immune cells. Inhibition of PDE4 leads to an increase in intracellular cyclic AMP (cAMP), which in turn inhibits the activity of various inflammatory cells and mediators (e.g., neutrophils, macrophages, T-lymphocytes) involved in the pathogenesis of chronic obstructive pulmonary disease (COPD). This results in reduced inflammation in the lungs.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly quantified, but well absorbed
Tmax:
Roflumilast: ~1 hour; Roflumilast N-oxide: ~8 hours
FoodEffect:
Food delays Tmax but does not significantly affect AUC or Cmax. Can be taken with or without food.
Distribution:
Vd:
Roflumilast: ~2.9 L/kg; Roflumilast N-oxide: ~16.5 L/kg
ProteinBinding:
Roflumilast: ~99%; Roflumilast N-oxide: ~97%
CnssPenetration:
Yes
Elimination:
HalfLife:
Roflumilast: ~17 hours; Roflumilast N-oxide: ~30 hours
Clearance:
Not available as a single rate; extensively metabolized
ExcretionRoute:
Primarily renal (70% as metabolites), some fecal (20%)
Unchanged:
<1% (renal)
Pharmacodynamics
OnsetOfAction:
Not for acute relief; clinical effects (e.g., reduction in exacerbations) observed over weeks to months.
PeakEffect:
Not applicable for acute effect; steady-state plasma concentrations reached within 4 days for roflumilast and 6 days for roflumilast N-oxide.
DurationOfAction:
24 hours (once daily dosing)
Confidence:
High
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Increased risk of suicidal thoughts or actions, particularly in individuals with a history of such thoughts or actions. Monitor for new or worsening symptoms, including:
+ Depression
+ Nervousness
+ Restlessness
+ Irritability
+ Panic attacks
+ Changes in mood or behavior
If you experience any thoughts or actions of suicide, contact your doctor immediately.
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they persist or bother you:
Dizziness or headache
Upset stomach
Diarrhea
Weight loss
Back pain
Flu-like symptoms
Trouble sleeping
* Decreased appetite
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Increased risk of suicidal thoughts or actions, particularly in individuals with a history of such thoughts or actions. Monitor for new or worsening symptoms, including:
+ Depression
+ Nervousness
+ Restlessness
+ Irritability
+ Panic attacks
+ Changes in mood or behavior
If you experience any thoughts or actions of suicide, contact your doctor immediately.
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they persist or bother you:
Dizziness or headache
Upset stomach
Diarrhea
Weight loss
Back pain
Flu-like symptoms
Trouble sleeping
* Decreased appetite
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch. Your doctor can provide medical advice on managing side effects.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent diarrhea
- Nausea
- Abdominal pain
- Headache
- Insomnia
- Anxiety
- Depression
- Thoughts of harming yourself or others
- Unexplained or significant weight loss
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: carbamazepine, phenobarbital, phenytoin, or rifampin, as these may interact with this drug.
If you are breastfeeding, as you should not breastfeed while taking this medication.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Never start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have liver disease, as this may affect how your body processes the medication.
If you are currently taking any of the following medications: carbamazepine, phenobarbital, phenytoin, or rifampin, as these may interact with this drug.
If you are breastfeeding, as you should not breastfeed while taking this medication.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to:
Inform your doctor and pharmacist about all medications you are taking, including prescription and over-the-counter drugs, natural products, and vitamins.
Discuss all your health problems with your doctor and pharmacist to verify that it is safe to take this medication in conjunction with your other treatments.
* Never start, stop, or change the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
While taking this drug, you may experience weight loss, and regular weight checks will be necessary to monitor this potential effect. Be sure to discuss any concerns or questions you have about weight loss with your doctor.
If you are pregnant or planning to become pregnant, it is crucial to consult with your doctor to thoroughly discuss the potential benefits and risks associated with using this medication during pregnancy.
While taking this drug, you may experience weight loss, and regular weight checks will be necessary to monitor this potential effect. Be sure to discuss any concerns or questions you have about weight loss with your doctor.
If you are pregnant or planning to become pregnant, it is crucial to consult with your doctor to thoroughly discuss the potential benefits and risks associated with using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Severe gastrointestinal symptoms (nausea, vomiting, diarrhea)
- Headache
- Dizziness
- Palpitations
What to Do:
Call 911 or Poison Control (1-800-222-1222) immediately. Seek emergency medical attention. Treatment is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inducers (e.g., rifampin, phenobarbital, carbamazepine, phenytoin) due to significant reduction in roflumilast exposure.
Moderate Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, clarithromycin, fluvoxamine, cimetidine): May increase roflumilast exposure. Use with caution.
- Dual CYP3A4/CYP1A2 inhibitors (e.g., fluvoxamine, cimetidine): May increase roflumilast exposure. Use with caution.
- Oral contraceptives containing ethinyl estradiol and gestodene: May increase roflumilast exposure.
Monitoring
Baseline Monitoring
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function, as roflumilast is extensively metabolized by the liver and contraindicated in severe hepatic impairment.
Timing: Prior to initiation
Psychiatric history (depression, suicidal ideation)
Rationale: Roflumilast can cause psychiatric adverse effects, including mood changes and suicidal ideation.
Timing: Prior to initiation
Weight
Rationale: Roflumilast can cause weight loss.
Timing: Prior to initiation
Routine Monitoring
Weight
Frequency: Periodically (e.g., monthly for first few months, then every 3-6 months)
Target: Maintain stable weight
Action Threshold: Significant, unexplained weight loss (>5-10% body weight); consider discontinuation or investigation.
Psychiatric symptoms (mood changes, anxiety, insomnia, suicidal ideation)
Frequency: Ongoing, especially during initial treatment
Target: Absence of new or worsening symptoms
Action Threshold: Any new or worsening psychiatric symptoms; consider discontinuation and psychiatric evaluation.
Gastrointestinal symptoms (diarrhea, nausea, abdominal pain)
Frequency: Ongoing, especially during initial treatment
Target: Tolerable symptoms
Action Threshold: Severe or persistent symptoms; consider dose reduction or discontinuation.
Symptom Monitoring
- Diarrhea
- Nausea
- Abdominal pain
- Headache
- Insomnia
- Anxiety
- Depression
- Suicidal ideation or behavior
- Unexplained weight loss
Special Patient Groups
Pregnancy
Pregnancy Category C. Limited human data. Animal studies show adverse effects on development at doses higher than clinical exposure. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for developmental effects observed in animal studies.
Second Trimester:
Potential for developmental effects observed in animal studies.
Third Trimester:
Potential for developmental effects observed in animal studies.
Lactation
Roflumilast and its metabolites are excreted in the milk of lactating rats. It is unknown if it is excreted in human milk. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for roflumilast and any potential adverse effects on the breastfed infant from roflumilast or from the underlying maternal condition.
Infant Risk:
L3 (Limited data â probably compatible). Monitor for gastrointestinal upset (diarrhea, vomiting) and weight loss in the infant.
Pediatric Use
Safety and effectiveness not established in pediatric patients. Not indicated for use in this population for COPD.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects. No specific dose adjustment is required based on age, but greater sensitivity of some older individuals cannot be ruled out. Monitor for adverse effects.
Clinical Information
Clinical Pearls
- Roflumilast is NOT a bronchodilator and is NOT for acute bronchospasm or rescue therapy.
- It is indicated for severe COPD associated with chronic bronchitis and a history of exacerbations, as an add-on therapy.
- The 250 mcg dose is typically an initial titration dose for 4 weeks to improve tolerability (especially GI side effects) before increasing to the maintenance dose of 500 mcg.
- Common side effects include diarrhea, nausea, weight loss, and headache, which often improve over time. Counsel patients on these potential effects.
- Monitor patients for psychiatric adverse events, including depression and suicidal ideation, especially during the initial treatment period.
- Contraindicated in moderate to severe hepatic impairment (Child-Pugh B and C, respectively).
Alternative Therapies
- Inhaled corticosteroids (ICS) for anti-inflammatory effects in COPD.
- Long-acting beta-agonists (LABAs) and long-acting muscarinic antagonists (LAMAs) for bronchodilation.
- Macrolide antibiotics (e.g., azithromycin) for exacerbation prevention in select patients.
Cost & Coverage
Average Cost:
$400 - $600 per 30 tablets (500mcg)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or 4 (non-preferred brand or specialty)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.