What to Know About Daliresp (Roflumilast)

Daliresp (roflumilast) is a type of oral medication used to treat chronic obstructive pulmonary disease (COPD) and other lung diseases. It is part of a category of drugs called phosphodiesterase-4 inhibitors (PDE4 inhibitor), which work to suppress inflammation in the airways of people who are resistant to standard COPD treatments. Approved by the U.S. Food and Drug Administration (FDA) in 2011, Daliresp and the generic form, roflumilast, are the only two PDE4 inhibitors currently licensed for use in the United States.

Uses

Daliresp is primarily used in people with severe COPD. It works by blocking PDE4, an enzyme that breaks down an inflammation-regulating molecule called cyclic adenosine monophosphate (cyclic AMP). By suppressing PDE4, cyclic AMP levels are increased and inflammation levels are decreased.

By reducing inflammation related to COPD, PDE4 inhibitors cause airways to dilate (bronchodilation) and, thus, reduce exacerbations. Daliresp may also decrease the mucus overproduction that's characteristic of the disease and decrease airway remodeling.

It's important to note that Daliresp does not repair the lungs or cure COPD. Instead, its effect on inflammation helps prevent further damage and symptom flares.

Daliresp may also be used to treat asthma, psoriasis, and psoriatic arthritis.

Before Taking

Daliresp is generally used to improve lung function in people with stable COPD who are resistant to standard treatment. Since Daliresp and PDE4 drugs work on chronic inflammation, they aren't useful for acute attacks of COPD or asthma, but rather for chronic maintenance of the disease.

This drug appears to be of most benefit to people with chronic bronchitis (a form of COPD) who have frequent exacerbations of their disease.

Your healthcare provider will consider this drug if this describes your case and after other first-line treatments for COPD have been exhausted.

Precautions and Contraindications

The effect of PDE4 inhibitors may be significantly increased when used with corticosteroid drugs. If you're using a corticosteroid inhaler, check with your healthcare provider about whether you need to alter your inhaler usage when you start taking Daliresp.

Because Daliresp has been shown to have severe psychological side effects, you may want to avoid taking the drug if you have pre-existing depression (even though it's not technically contraindicated as such by the manufacturer).

Additionally, if you have liver disease or liver complications (hepatic insufficiency), you shouldn't take Daliresp.

Tell your healthcare provider if you're pregnant or breastfeeding before taking Daliresp. If you're planning on becoming pregnant while taking Daliresp, be sure to also communicate this to your healthcare provider, as it's unknown how the medication will affect a fetus.

Dosage

Daliresp is taken once daily by mouth with or without food. It is available as an oral table in two different doses: 250-micrograms (mcg) and 500 mcg.

The 250-mcg dose is the starting dose; you will take it daily for four weeks before increasing to the 500-mcg dose. Alternatively, you may start on the 500-mcg dose straightaway. Your healthcare provider will determine which dosing regimen is right for you.

How to Take and Store

Daliresp may be taken with or without food, and should only be taken once daily. If you miss a dose, take the skipped dose as soon as you remember, unless it's nearly time for your next scheduled dose. Taking an extra dose of Daliresp may result in a dangerous overdose that should be treated at a poison control center.

Symptoms of Daliresp overdose may include:

• Dizziness
• Lightheadedness
• Headache
• Cold, clammy skin
• Rapid heartbeat

As with most medications, Daliresp should be stored at room temperature away from heat and moisture. Avoid storing in in the bathroom or your glove compartment. Don't share your medication with anyone else. Be sure to keep up with every scheduled healthcare provider's appointment while you're taking Daliresp.

Side Effects

There are several side effects to taking Daliresp. It's important to be aware of them and discuss them with your healthcare provider before taking this medication.

Common

The main side effects of PDE4 inhibitors include diarrhea, nausea, and headaches, as well as back pain, dizziness, flu-like symptoms, and decreased appetite.

Daliresp may cause weight loss in two out of three patients, so weight should be monitored during treatment. You may need to stop taking Daliresp if you lose too much weight.

Severe

Daliresp has also caused major psychological symptoms for some people, including suicidal thoughts and behavior, trouble sleeping (insomnia), anxiety, depression, and other changes in behavior and mood.

In fact, depression, anxiety, and insomnia occur twice as often in users of Daliresp compared to people with COPD who don't use the drug, according to a 2014 review published in American Family Physician.

If you start to notice any of these symptoms, tell your healthcare provider right away.

Warnings and Interactions

Due to their metabolism by a liver enzyme called cytochrome P-450, PDE4 inhibitors may interfere with how other medications are also metabolized, either increasing or decreasing their blood concentration.

Among the drugs known to interact with Daliresp are:

• Erythromycin
• Cimetidine
• Birth control pills
• Some seizure medications

In some cases, a dose adjustment may be needed to counteract the interaction. In others, a drug substitution may be needed. Others still, like cimetidine, don't require any changes in the majority of cases.

Be sure to inform your healthcare provider if you're taking any of these medications, as an interaction between PDE4 inhibitors may result in undesired side effects or ineffective treatment.