Rofaday (Roflumilast 500mcg) Tablets

Rofaday general information

What is Rofaday used for?

Chronic obstructive pulmonary disease (COPD) is a chronic lung disease group that causes breathing difficulties due to lung damage.  COPD cannot be cured or reversed, therefore, COPD gets worse with time.  Rofaday tablets 500mcg are used for long-term maintenance treatment of severe COPD in patients with frequent exacerbations (worsening symptoms) and chronic bronchitis.  Regular use of Rofaday tablets helps control symptoms, reduce the frequency of exacerbations, and prevent lung damage from worsening in severe COPD.  You will probably already be taking an inhaled bronchodilator medication, and Rofaday tablets add to this treatment. 

What causes COPD?

COPD includes other chronic lung diseases, including emphysema, chronic bronchitis, and chronic asthma.  It is caused by inhaling irritants that gradually damage the lung cells with time to a point where the damage cannot be reversed.  Smoking is the most common cause, also workplace chemicals.  Asthma and COPD are similar conditions, but asthma is reversible.  Asthma is caused by inflammation of the airways, triggered either by an allergic reaction or chemical irritation.  The effects on the lungs are not permanent and can be reversed using the right medications.  However, untreated asthma can cause scarring of the lung tissue that leads to COPD.  Scarring results in airway remodelling, which means thickening of the airway walls and narrowing of the tubes, which blocks the airways, making breathing permanently and irreversibly difficult.  Chronic bronchitis is inflammation of the upper airways, including the bronchi (large airways) and the bronchioles (small airways).  Emphysema develops due to damage to the alveoli or air sacs of the lungs, making it increasingly difficult for the lungs to get enough oxygen into the blood. 

Inflammation

Inflammation is your body’s response to injury and infection.  It is a process that involves cells of the immune system and a range of chemicals.  These include cytokines like interleukins and leukotrienes, prostaglandins, and hormones like histamine.  These inflammatory mediators protect and heal the injured or infected tissues.  Inflammation that lasts for a short time is acute inflammation, for example, following surgery, soft tissue damage, or infection.  However, if inflammation persists, it becomes chronic inflammation and can cause further damage, such as in COPD. 

Vascular changes are the first stage of the inflammatory response when small blood vessels dilate (widen) and become more permeable (leaky).  This allows proteins and blood cells into the injured tissues to fight invading pathogens, remove dead tissue, and promote healing.  These changes result in swelling and redness, and heat is generated by increased blood flow.  Pain is caused by chemicals produced by inflammatory cells, and these chemicals, such as prostaglandins, also induce fever.  If inflammation persists, it becomes a chronic condition.  The inflammatory process is no longer regulated and continues, even though the original cause is no longer a threat.  Tissue damage worsens due to the continued infiltration of immune cells.  Macrophages and leukocytes produce other mediators, including growth factors and enzymes, which cause more tissue damage followed by repair that leads to scarring. 

Symptoms of COPD

COPD symptoms are the result of inflammation and bronchospasm, which is tightening of the smooth muscle that lines the airways, causing narrowing of the airways.  Symptoms include a chronic cough with the production of thick mucus or phlegm, wheezing, and tightness of the chest.  Breathing is difficult, making you feel short of breath.  At first, shortness of breath is related to exercise or mild exertion but eventually happens even when you are resting.  You are more likely to get a chest infection and feel tired and exhausted much of the time.  In all its forms, COPD limits daily activities, restricts exercise and exertion, and reduces the quality of life.

How does Rofaday work?

Rofaday tablets 500mcg contain roflumilast, a non-steroid, anti-inflammatory medication that is used to treat severe COPD.  Roflumilast in Rofaday tablets 500mcg works by inhibiting inflammatory processes in the lungs and systemic inflammation associated with COPD.  Roflumilast is a potent and selective inhibitor of phosphodiesterase-4 (PDE4), which is an enzyme that results in the breakdown (hydrolysis) of cyclic adenosine monophosphate (cAMP). 

cAMP is an intracellular messenger involved in many biological processes.  It works by transmitting signals between a receptor on the cell surface that has been activated by a first messenger, such as a hormone, neurotransmitter, or other chemical messenger like a prostaglandin, and other targets within the cell.  The outcomes of this activation vary depending on the cell type and the initial trigger.  Phosphodiesterase-4 regulates the amount of cAMP inside the cell and, therefore, how the cell responds.

Inflammatory mediators produced by cells of the immune system such as macrophages, neutrophils and lymphocytes include cytokines like leukotrienes, and interleukins.  Low levels of intracellular cAMP result in increased production of inflammatory mediators.  The inhibition of PDE4 by roflumilast in Rofaday tablets 500mcg increases intracellular cAMP.  This, in turn, blocks the production of inflammatory cytokines from immune cells and reduces the inflammatory response, both in the lungs and in other parts of the body.  Rofaday tablets 500mcg help dampen down the inflammatory response, which slows down the worsening of COPD and reduces the number and frequency of exacerbations.

What does Rofaday contain?

Rofaday tablets 500mcg contains the active ingredient roflumilast, a phosphodiesterase-4 (PDE4) inhibitor that works as a bronchodilator and is used to treat severe COPD. 

What are the side effects of Rofaday?

Most medications have some side effects, but they are not experienced by everyone.  Some side effects are commonly experienced when taking Rofaday tablets 500mcg, but others are not so common, and you should discuss any problems or concerns with your primary care physician. 

Common side effects when taking Rofaday include weight loss and decreased appetite, insomnia, headache, diarrhoea, nausea, abdominal pain.

When should Rofaday not be used?

Have a talk with your primary healthcare physician before taking Rofaday tablets 500mcg so that you have a full understanding of what this medicine is for and how to use it.  There are some reasons for not taking a medication; these are called contraindications, and for Rofaday you should consider the following before taking Rofaday:

• Have you ever had an unusual reaction or an allergy when taking Rofaday?
• Are you pregnant or breastfeeding?
• Do you have any problems with your liver?
• Do you have a severe immunological disease such as HIV infection, multiple sclerosis, lupus erythematosus, or progressive multifocal leukoencephalopathy?
• Do you have a severe acute infectious disease such as hepatitis?
• Do you have cancer (except basal cell carcinoma)?
• Do you have congestive heart failure?

What medications interact with Rofaday?

Some medicines interact with Rofaday tablets 500mcg and may affect the way it works, or are affected by Rofaday or increase side effects; you should discuss possible interactions with your primary care physician.  These may include cimetidine for ulcers, the antidepressant fluvoxamine, the antibiotic rifampicin, the antiepileptics carbamazepine and phenytoin, theophylline for respiratory disorders.

If other medications may interact with Rofaday, your doctor will discuss these with you. 

How should Rofaday be taken and for how long?

You should take your Rofaday tablets 500mcg swallowed whole once daily with or without food and at the same time each day.  The dose you take depends on your doctor’s recommendation and may be increased after 28 days.  You should continue to take your Rofaday tablets 500mcg for as long as recommended by your doctor, and it may take several weeks before you feel better.

Missed dose of Rofaday

If you miss a dose of Rofaday tablets 500mcg take it as soon as you remember, unless it is time to take the next dose, then skip the missed dose.  Do not take a double dose.

How should Rofaday be stored?

You should store your Rofaday tablets 500mcg below 25°C in a cool dry place.