Roflumilast: How to Use, Dosage, Side Effects

Roflumilast, a potent inhibitor of phosphodiesterase-4 (PDE4), helps reduce COPD worsening risk in severe COPD patients with chronic bronchitis and previous exacerbations. By blocking PDE4, it boosts cAMP levels, leading to anti-inflammatory effects and reduced release of inflammatory mediators, relieving COPD patients.

Roflumilast is a strong phosphodiesterase-4 inhibitor, helping to minimize severe COPD exacerbation risk in serious COPD patients with past exacerbations and chronic bronchitis. When it blocks PDE4 (phosphodiesterase -4), it increases cAMP levels, resulting in a reduction of inflammatory mediators and inflammation, ultimately, patients (with COPD) feel relief.

Roflumilast is available in a once-daily oral form, with tablets of 500 µg and an 80% bioavailability. It reaches peak plasma levels in about 1 hour for the main drug and around 8 hours for its active metabolite. Both forms are mostly bound to plasma proteins and have a half-life of approximately 17 hours. While the metabolite is more exposed, the drug is three times more potent.  Roflumilast is mainly metabolized by the liver, particularly by enzymes CYP1A2 and CYP3A4. Patients with liver issues may have slower elimination, but dose adjustments are usually unnecessary. It doesn't require dosage changes for kidney issues. However, it shouldn't be taken with strong inhibitors of CYP3A4 or dual inhibitors of CYP3A4 and CYP1A2. Azithromycin, a weaker CYP3A4 inhibitor commonly used in COPD patients, poses less interaction risk compared to erythromycin¹.

Why do healthcare providers prescribe roflumilast?

Healthcare providers prescribe roflumilast to patients with severe COPD to minimize the worsening, or a number of episodes that worsen the symptoms of COPD. 

COPD (chronic obstructive pulmonary disease) is a group of diseases that impact the airways and lungs².

According to a study

Roflumilast reduces COPD exacerbation risk by 15.5% to 11.9%, delaying disease development and improving lung function. In asthma patients, it reduces airway hyper-responsiveness, bronchoconstriction, and inflammation, improving the patient’s quality of life. Combining roflumilast with other agents enhances its efficacy.

How does it work?

Roflumilast is an oral, long-acting PDE-4 inhibitor with an outstanding impact on inflammation from eosinophils and neutrophils, airway altering, and bronchoconstriction. It's effective for treating asthma and COPD, showing significant clinical effects in mild to severe cases. Studies suggest a morning or night dosage of 500 mg is beneficial³.

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How to use Roflumilast?

Roflumilast medication is available in tablet form which you will take orally, with or without food once a day. It’s best to use it at around the same time daily. Make sure, to strictly follow the directions written on your prescription label. If, you don't understand any direction, ask your healthcare provider or pharmacist for clarification.

Furthermore, follow these instructions

• Don’t take less or more of roflumilast or take it more often than prescribed by your healthcare provider.
• Don’t use this medication to treat sudden attacks of breathing discomfort, until your healthcare provider suggests it.

Note:

Your healthcare provider will provide you the Medication Guide (manufacturer’s patient information sheet) when you start treatment with this medication and every time you refill the prescription. (You can visit the manufacturer’s website to obtain the Medication Guide. 

Remember, roflumilast can control COPD symptoms but it doesn’t cure it. Use it until you feel well, but don’t stop taking it without discussing it with your healthcare provider.

Precautions:

What precautions should I consider?

Before using roflumilast it’s crucial to take some measures including: 

1. Medical history:

Discuss with your provider if you have or ever had a history of any mental health issues, such as

• Depression
• Thoughts of killing or harming yourself or planning to do
• Unusual changes in your mood or behavior

2. Current medications:

Inform your provider what other prescription and nonprescription medicines, nutritional supplements, herbal products, vitamins, or plan to use. Tell your provider if you are using or plan to use these medications:

• Cimetidine (Tagamet)
• Enoxacin (it is not available in the U.S)
• Rifampicin
• Erythromycin (Erythrocin, E.E.S, E-Mycin)
• Certain contraceptives (birth control pills)
• Phenobarbital
• Fluvoxamine
• Phenytoin (Dilantin)
• Ketoconazole (Nizoral)

Your provider may change the dose or monitor you carefully for side effects.

3. Allergies:

Discuss with your provider if you are allergic to roflumilast, any other medicine, or any ingredient in a roflumilast tablet. You can check the Medication Guide for a list of the ingredients.

4. Pregnancy and breastfeeding:

Inform your provider if you are conceived, plan to become pregnant, or are a breastfeeding mother. If you are taking Roflumilast and become pregnant immediately talk with your provider.  

5. Liver disease:

Inform your provider if you have liver disease, jaundice, or experience some symptoms, as roflumilast may cause further liver problems. These symptoms are:

• Nausea
• Abdominal pain
• Vomiting

6. Weight loss:

Roflumilast can cause weight loss. You need to check your weight regularly. If you feel you are losing weight while taking roflumilast immediately inform your provider.

Be sure your caretaker or family member should knows these facts mentioned above, so they can call the provider if you are unable to seek treatment on your own.

Other precautions or dietary instructions:

Avoid operating or driving heavy machinery while taking roflumilast, as it may cause drowsiness or dizziness.

Don’t consume grapefruit or grapefruit juice, while using roflumilast.

Side effects:

What are the side effects that roflumilast can cause?

Roflumilast may cause some side effects including:

• Dizziness
• Nausea
• Diarrhea
• Back pain
• Muscle spasm
• Decrease appetite
• Headache
• Uncontrollable shaking of a part of the body

Roflumilast may cause other side effects. Call your provider if you have any unusual problems while using it.

If you experience any severe side effects, your provider may send a report to the FDA on the website

http://www.fda.gov/Safety/MedWatch

Or by calling this number

1-800-332-1088

Where should I store this medication?

• Store a roflumilast at room temperature.
• Keep away it from excess moisture and heat, even not in the bathroom.
• Keep roflumilast in the container you bought, tightly closed.
• Keep all medicines out of the reach of kids. To protect children from poisoning always lock safety caps and place the medicine in a safe location, right away.

Where to dispose of it?

Unnecessary medicines should be disposed of in special ways to make sure that children, pets, and other individuals can’t use them. However, you should not flush roflumilast down the toilet, as an alternative, the best way to dispose of your medicines is through a medicine take-back program. Call your provider or call your local recycling/garbage department to learn about the take-back program in your community.

What to do if I forgot a dose?

If you forget to take your dose on time, consume it immediately when you remember. However, if the time is for the next dose, don’t consume the missed dose, just continue your regular dosing schedule. Remember don’t take a double dose, to make up for a missed one.

What to do if I take an overdose?

In case of overdose, immediately call the poison control helpline at

1-800-222-1222.

Online information is available at this website

https://www.poisonhelp.org/help

Call the emergency services at 911, as soon as possible, if the patient

• Had a seizure
• Has collapsed
• Can’t be awakened

What additional measures should I follow?

You must keep a written list of all the prescription and over-the-counter (nonprescription) medication you are taking, and any supplement for example minerals, vitamins, or other dietary supplements. You must bring this list with you each time you visit your provider. It is also significant to carry with you in case of emergencies.

FAQ’S:

Q. What is the brand name of roflumilast?

A. The brand name of roflumilast is “Daliresp”.

Q. What type of drug is roflumilast?

A. Roflumilast is used in patients with serious chronic obstructive pulmonary disease to minimize the number of episodes or worsening of COPD symptoms. Roflumilast falls in a class of medications called phosphodiesterase inhibitors.  

Q. Why is roflumilast used in COPD?

Roflumilast is a strong inhibitor of PDE-4, which is well effective in improving lung function and reducing exacerbations in patients with severe to very severe COPD linked with chronic bronchitis. This can help reduce the number of exacerbation episodes and hospitalizations in patients who experience frequent exacerbations.