Roflumilast

About Roflumilast

Roflumilast and its active metabolite inhibit phosphodiesterase 4 (PDE4), which raises cyclic AMP in lung cells and damps airway inflammation. The label approves it to reduce the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations; it is not a bronchodilator and is not for relief of acute bronchospasm, and safety and effectiveness in children have not been established. The maintenance dose is 500 mcg once a day, with or without food. Treatment may start with 250 mcg once a day for four weeks, which the label says may reduce the chance of stopping early in some patients; the 250 mcg tablet is a starting dose only and is not the dose that works. In the trials it was added to inhaled maintenance treatment; it is not a bronchodilator.

There is no boxed warning. Roflumilast is contraindicated in moderate to severe liver impairment (Child-Pugh B or C). Its main warnings are psychiatric: insomnia, anxiety and depression were reported in trials, and there were suicide-related events in people taking it, so the prescriber weighs the risk in anyone with depression or past suicidal thoughts, and patients and families are asked to report mood or behavior changes at once. It also causes weight loss in some people, so weight is checked regularly and the drug may be stopped if the loss is unexplained or significant. The most common side effects are diarrhea, weight loss, nausea, headache, back pain, flu, insomnia, dizziness and decreased appetite; diarrhea and nausea were the usual reasons for stopping.

What is distinctive is the interaction profile. Strong CYP450 inducers such as rifampin, phenobarbital, carbamazepine and phenytoin lower roflumilast levels and are not recommended with it. CYP3A4 inhibitors and dual CYP3A4 and CYP1A2 inhibitors, including erythromycin, ketoconazole, fluvoxamine, enoxacin and cimetidine, raise its levels and may add side effects, so the prescriber weighs that risk; some oral contraceptives do the same. The label advises against use by nursing women, since the drug is likely to pass into milk, and there are no randomized clinical studies in pregnant women. It is not a controlled substance.

Taking Roflumilast

How to take it

Take one tablet by mouth once a day, with or without food, at about the same time each day. Keep taking it even when you feel well; it controls COPD but does not cure it, and it will not relieve a sudden attack of breathlessness, so keep your rescue inhaler.

If you miss a dose

Take it as soon as you remember, unless it is almost time for the next dose; then skip the missed dose. Do not take a double dose.

Storage

In the original tightly closed container at room temperature, away from heat and moisture (not in the bathroom), out of reach of children.

Interactions to know about

Rifampin, phenobarbital, carbamazepine and phenytoin lower its level and are not recommended with it. Erythromycin, ketoconazole, fluvoxamine, enoxacin and cimetidine raise its level, as do some oral contraceptives containing gestodene with ethinyl estradiol, which may add side effects. Tell the pharmacist about every medicine, including nonprescription products and supplements.

This summarizes the official prescribing information. Your prescriber’s and pharmacist’s instructions, and the leaflet that comes with your medicine, take priority.

Why the cash price for Roflumilast differs from pharmacy to pharmacy

Roflumilast 500 mcg has many generic makers, so quotes for the same thirty tablets can differ widely between pharmacies depending on which maker they buy from and whether it sits on a flat-price generic list. The 250 mcg starting strength is dispensed for only four weeks, so it is often quoted separately.

A prescription written for Daliresp with a brand-only instruction is priced as a brand, and the brand costs far more than the generics. The dose is one tablet a day, so a ninety-day fill is a small bottle with one dispensing fee instead of three.

Ways to pay less for Roflumilast without insurance

• Ask the prescriber to write roflumilast generically and allow substitution; a rated generic can be dispensed for Daliresp unless the prescription says otherwise.
• Ask whether the pharmacy has roflumilast on a flat-price generic list, and compare more than one pharmacy for the same strength and count.
• Once you have moved to the 500 mcg maintenance dose and are tolerating it, ask the prescriber about a ninety-day supply.
• If you are prescribed the brand, ask the maker whether its savings or patient assistance program applies to someone paying cash; many copay cards require commercial insurance.
• Upload the prescription to Script Unlock so licensed pharmacies can quote their cash price. You pay the pharmacy directly.

Questions to ask your pharmacist about Roflumilast

1. 1.Do any of my medicines, such as rifampin, carbamazepine, an antibiotic or an antifungal, change how my roflumilast works?
2. 2.Which mood or sleep changes should my family and I watch for, and when should I call my doctor?
3. 3.How often should I weigh myself while taking roflumilast, and how much weight loss should I report?
4. 4.Can I keep using my rescue inhaler and my daily inhalers with roflumilast, and does it replace any of them?

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