Roflumilast (Oral)

Roflumilast helps to prevent COPD symptoms, such as wheezing, breathlessness and chest tightness, and is designed to be taken daily for an extended period of time.

Overview

Roflumilast is prescribed to people with Chronic Obstructive Pulmonary Disease (COPD) to prevent flare-ups of symptoms associated with the condition. The drug's mechanism of action is unknown, but it is thought to reduce inflammation in the lungs. It helps to prevent the following common symptoms:

  • Persistent cough
  • Shortness of breath
  • Wheezing, whistling or squeaking when breathing
  • Chest tightness

In the US, roflumilast is sold under the brand name Daliresp and is only available with a doctor's prescription. It is administered orally in tablet form.

Conditions Treated

  • Chronic Obstructive Pulmonary Disease (COPD)

Type of Medicine

  • Phosphodiesterase inhibitor

Side Effects

Roflumilast can cause a range of unwanted side effects, some of which are serious and require urgent medical attention. Check with your doctor immediately if you experience sudden, unexpected weight loss when taking this drug. This is one of the more common serious side effects of the drug.

The following side effects are less common, but should still be reported to your doctor as soon as possible.

  • Chills
  • Shivering
  • Fever
  • Sweating
  • Headache
  • Cough
  • Sore throat
  • Runny nose
  • Loss of appetite
  • Nausea
  • Vomiting
  • Diarrhea
  • Sleeplessness or difficulty sleeping
  • Unusual tiredness or weakness
  • Difficulty concentrating
  • Nervousness, fear or anxiety
  • Feelings of sadness or emptiness
  • Reduced interest or pleasure
  • Discouragement
  • Irritability
  • Suicidal thoughts
  • Changes in behavior
  • General feeling of illness or discomfort
  • Joint pain
  • Muscles aches or pain

Roflumilast can also cause less serious side effects, which may not require medical attention unless they become persistent or particularly bothersome. They may dissipate as your body gets used to the medicine. If you're struggling to cope with any of the following side effects, you could ask your doctor for advice:

  • Pain in stomach or abdomen
  • Burning sensation in chest or stomach
  • Indigestion
  • Back pain
  • Pain in side or lower back
  • Muscles spasms
  • Pains around eyes or cheekbones
  • Shaky legs, arms, hands or feet
  • Trembling hands or feet
  • Shortness of breath
  • Tightness in chest or wheezing
  • Bladder pain
  • Clouding or bloody urine
  • Difficult, burning or painful urination
  • Frequent urge to urinate
  • Reduced appetite
  • Upset stomach
  • Tenderness in stomach
  • Dizziness
  • Sneezing
  • Stuffy or runny nose
  • Sweating

If you notice any other side effects not listed here, consult your doctor or report them to the FDA.

Overdose

An overdose of roflumilast could be dangerous. If you think you have taken too much of the drug, call your local poison control center. If the person taking roflumilast has collapsed or isn't breathing, call 911. Symptoms of roflumilast overdose include:

  • Headache
  • Severe dizziness
  • Lightheadedness
  • Fast heartrate
  • Cold, clammy skin

Signs of allergic reaction

Seek emergency medical treatment if you think you are suffering from an allergic reaction roflumilast. Symptoms of an allergy include:

  • Rash
  • Hives
  • Itchiness
  • Red skin
  • Swollen skin
  • Blistered or peeling skin
  • Sudden onset of wheezing, tightness in chest or troubled breathing
  • Tightness in throat
  • Difficulty talking
  • Unusual hoarseness
  • Swollen face, mouth, lips, tongue or throat

Dosage

The recommended dose of roflumilast for adults with COPD is 500 mcg taken once each day, either with or without food. However, this may vary depending on your medical history; always follow your doctor's dosing instructions. The drug has not been thoroughly tested for safety and efficacy in children, so the use and dosage for pediatric doses should be determined by a doctor.

Take roflumilast tablets whole without chewing, breaking or crushing them. You can take them with water if necessary. Try to take them around the same time every day; setting an alarm may help you with this.

If you miss a dose of roflumilast, take it as soon as you remember. If when you remember that you've missed a dose it is almost time for the next one, do not take the missed dose. Instead, simply skip it and return to your normal dosing schedule. Do not double doses to make up for a missed dose, as this could increase the risk of side effects.

Interactions

Roflumilast can interact with other medicines and cause harmful effects. It is very important that your doctor knows about all the medicines you're currently taking, including those prescribed to you and those bought over the counter. You should also tell your doctor about all herbal supplements, vitamin supplements and multivitamins you are taking. Do not take any new medicines once you start taking roflumilast without your doctor's approval.

It is not recommended that patients take riociguat (Adempas) at the same time as roflumilast. Your doctor may choose not to prescribe roflumilast or they might give you an alternative to riociguat.

The following medicines are not recommended to be taken at the same time as roflumilast, but in some instances, it may be necessary. If so, your doctor may adjust the doses of some of your current medicines when they prescribe roflumilast or change the times at which you take your medicines. Always follow your doctor's instructions.

  • Ceritinib (Zykadia)
  • Clarithromycin (Biaxin)
  • Fosphenytoin (Cerebyx)
  • Idelalisib (Zydelig)
  • Phenytoin (Dilantin, Phenytek)
  • Rifampin (Rifadin, Rimactane)

The following medicines might increase the risk of side effects when taken with roflumilast. However, it may still be necessary to take both medicines at the same time. Your doctor may adjust your dosages or the times at which you take the medicines. Follow your doctor's instructions closely.

  • Cimetidine (Tagamet)
  • Enoxacin (Penetrex)
  • Erythromycin (E.E.S., EryPed, Erythrocin Stearate Filmtab, PCE Dispertab)
  • Ethinyl Estradiol
  • Fluvoxamine (Luvox)
  • Gestodene
  • Ketoconazole (Nizoral)

Warnings

Risk of suicide

Some of the side effects associated with roflumilast are related to mental health, and the drug can lead to suicidal thoughts or actions. In individuals with a history of suicidal thoughts or actions, the risk is higher. If you notice sudden changes in your mood, particularly if you feel unusually depressed, nervous, restless, irritable, or have panic attacks, let your doctor know as soon as possible. You should also seek medical care urgently if you have suicidal thoughts or actions.

Risk of weight loss

Weight loss is a common side effect associated with roflumilast. Your doctor may request that your weight is monitored on a regular basis. If you experience clinically significant weight loss, your doctor may consider discontinuation of the medicine. Consult your doctor if you feel that you are losing weight rapidly and without explanation.

Preventative nature of medicine

It's important to note that roflumilast prevents symptoms of COPD and doesn't provide relief from acute symptoms, such as bronchospasm. You should take the medicine on a daily basis (or as prescribed by your doctor), even when you do not have symptoms of COPD.

Use inhaled medicines, as prescribed by your doctor, to manage acute flareups. If you do not have medicines of this nature and feel that you could benefit from a treatment for acute flareups, consult your doctor. Do not stop taking roflumilast without your doctor's approval, even if you feel well.

Liver disease

Roflumilast may be harmful to individuals with liver disease or impairment. For individuals with mild liver impairment, doctors will carefully weigh up the risks and benefits of the drug before prescribing it to you. The drug is contraindicated for patients with moderate to severe liver impairment.

Pregnancy and breastfeeding

Roflumilast is an FDA pregnancy category C drug, which means it should only be used during pregnancy if the benefits of the drug far outweigh potential risks to the mother or the fetus. Drugs are categorized as C when there have been no adequate studies into the drug performed on pregnant women, and there have either been no appropriate animal studies conducted, or animal studies have proven adverse effects.

It is not known whether roflumilast is excreted in human breast milk and, if it is, what effects it might have on nursing infants. For this reason, the potential risks should be carefully weighed against the benefits of the drug to the nursing mother. It may be safer to avoid breastfeeding while taking this medicine.

Allergies

Make sure your doctor knows about all the allergies you suffer from and any allergic reactions you have had to medicines in the past. You should mention all allergies, including pollen, animal, drug, food and chemical allergies.

Storage

Roflumilast should be stored in a closed container, preferably with a childproof cap, at room temperature. It should be kept from freezing and away from direct light, heat and moisture. Do not store the medicine in a bathroom. Keep it up and away from the ground so that it is not within reach of children or pets.

Do not keep unused roflumilast tablets. Instead, dispose of them appropriately. Don't flush unused medicine down the toilet. Consult your healthcare provider for disposal instructions; they may have a medicine take-back program, or they may be able to recommend a local recycling program which provides a medicine take-back service.

Summary

Roflumilast is a preventative treatment for chronic obstructive pulmonary disease (COPD) symptoms. It is administered orally in tablet form, and should be taken daily for extended periods of time, even if symptoms of COPD are mild or not present. It shouldn't be used for acute flareups of COPD and patients should continue to use inhaled medicines where appropriate to manage acute symptoms such as wheezing, breathlessness and chest tightness.

In the US, roflumilast is known by the brand name Daliresp and is only available with a prescription. Patients can expect to have regular doctor's appointments to monitor their condition and see how well the medicine is working. Their weight may also be monitored closely since unexplained weight loss is a common side effect of the drug. If clinically significant weight loss occurs, your doctor may discontinue roflumilast.

The recommended dose of roflumilast is 500 mcg taken once each day either with or without food. The tablets should be swallowed whole at roughly the same time each day. Missed doses should be taken as soon as remembered unless it is time for the next dose, in which case the missed dose should be skipped and the normal dosing schedule resumed.

Some patients may experience reduced appetite, pain or discomfort in the stomach, abdomen, side or back, mild dizziness, upset stomach, or indigestion, among other minor side effects. These usually don't require medical attention unless they become persistent.

The most serious side effects associated with the drug are suicidal thoughts or actions, depression, anxiety, irritability and general unusual mood changes. These should be reported to a doctor as soon as possible.

 

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Last Reviewed:
January 28, 2018
Last Updated:
April 05, 2018
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