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Related to Daxas: Roflumilast


(row-floo-mi-last) ,


(trade name),


(trade name)


Therapeutic: copd agents
Pharmacologic: phosphodiesterase inhibitors
Pregnancy Category: C


To ↓ the risk of exacerbations in severe COPD patients that have a history of chronic bronchitis with exacerbations.


Roflumilast and one active metabolite (roflumilast N-oxide) act as selective inhibitors of phosphodiesterase 4 (PDE4), responsible for breaking down 3', 5'-adenosine monophosphate (cAMP). Resulting intracellular accumulation of cAMP in lung tissue.
Reduces cells (neutrophils, eosinophils and total cells) in sputum.

Therapeutic effects

↓ exacerbations in COPD patients.


Absorption: Well absorbed following oral administration.
Distribution: Parent drug and metabolites probably enter breast milk.
Protein Binding: Roflumilast—99%; roflumilast N-oxide—97%.
Metabolism and Excretion: Mostly metabolized (87.5%), primarily by CYP3A4 and CYP1A2 enzyme systems One metabolite, roflumilast N-oxide in pharmacologically active. Inactive metabolites excreted in urine.
Half-life: Roflumilast—17 hr; roflumilast N-oxide—30 hr.

Time/action profile (blood levels)

PO unknown1 (4–13†)24 hr
†For roflumilast N-oxide.


Contraindicated in: Acute bronchospasm;Moderate to severe hepatic impairment;Concurrent use of strong inducers of CYP3A4 and CYP1A2 enzymes; Lactation: Avoid breast-feeding.
Use Cautiously in: History of depression/suicidal thoughts; Obstetric: Use only if potential maternal benefit justifies potential risk to the fetus; Pediatric: Safety and effectiveness not established.

Adverse Reactions/Side Effects

Central nervous system

  • suicidal thoughts (life-threatening)
  • anxiety
  • depression
  • dizziness
  • headache
  • insomnia


  • rash


  • diarrhea (most frequent)
  • abdominal pain
  • ↓ appetite
  • dyspepsia
  • gastritis
  • nausea
  • vomiting


  • weight loss


  • muscle spasms


  • tremor


  • hypersensitivity reactions including angioedema (life-threatening)


Drug-Drug interaction

Strong inducers of the CYP3A4 and CYP1A2 enzyme systems, including rifampicin, phenobarbital, carbamazepine, and phenytoin ↓ blood levels and effectiveness; concurrent use should be avoided.Blood levels and risk of adverse reactions ↑ by concurrent use of inhibitors of the CYP3A4 enzyme system and dual inhibitors of the CP3A4 and CYP1A2 enzyme systems including erythomycin, ketoconazole, fluvoxamine, and cimetidine.Gestodene and ethinyl estradiol may also ↑ levels and risk of adverse reactions; risk should be considered.


Oral (Adults) 500 mcg once daily.


Tablets: 500 mcg

Nursing implications

Nursing assessment

  • Assess respiratory status periodically during therapy.
  • Monitor weight regularly. If unexplained or clinically significant weight loss occurs, evaluate weight loss and consider discontinuation of roflumilast.
  • Assess mental status (orientation, mood, behavior) before and periodically during therapy. Assess for suicidal tendencies.
  • Monitor for signs and symptoms of hypersensitivity reactions (angioedema, urticaria, rash). Discontinue therapy and treat symptomatically if symptoms occur.

Potential Nursing Diagnoses

Ineffective airway clearance


  • Oral: Administer without regard to food.

Patient/Family Teaching

  • Instruct patient to take roflumilast as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill; new information may be available.
  • Inform patient that roflumilast is not a bronchodilator and should not be used for treating sudden breathing problems.
  • Advise patient to monitor weight regularly. If weight loss occurs, notify health care professional; may require discontinuation of therapy.
  • Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide, trouble sleeping, new or worse depression, new or worse anxiety, acting on dangerous impulses, or other unusual changes in behavior or mood or signs and symptoms of hypersensitivity reactions occur.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of Rx, OTC, and herbal products without consulting health care professional.
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

  • ↓ in the number of flare-ups or the worsening of COPD symptoms (exacerbations).


A selective inhibitor the phosphodiesterase type 4 (PDE4), which is used as maintenance therapy of severe chronic obstructive pulmonary disease with a forced expiratory volume at one second < 50% of predicted in a background of chronic bronchitis.
References in periodicals archive ?
Daxas will be available from a doctor or via a prescription as a once-daily oral tablet.
Additional sales resources will be necessary in order to adequately support Viibryd, as well as our currently marketed products Teflaro, Savella[R], Bystolic[R], Namenda and Lexapro and the anticipated launch of Daxas (roflumilast), pending FDA approval in calendar 2011.
Nycomed and Goldman have declined to comment on their relations but people familiar with the situation said the bank's primary role was to find a partner for Daxas.
and our co-promotion partner Altana Pharma filed Daxas in the E.
Products that should add significantly to revenues include hepatitis C virus (HCV) drug Victrelis, fertility drug Elonva, Saphris (acute treatment of schizophrenia and bipolar I disorder in adults), Simponi (treatment of certain inflammatory diseases), Dulera (asthma), and Daxas (chronic obstructive pulmonary disease) among others.
6]] Daxas, a once-a-day tablet, is the first drug in a new class of treatment for severe COPD associated with chronic bronchitis and the first oral anti-inflammatory treatment specifically developed for COPD patients.
A sale of the business would not come as great surprise to many in the pharmaceutical industry, since Nycomed is developing an interesting experimental lung drug called Daxas and also has a business in emerging markets that could attract big players.
Daxas, a phosphodiesterase-4 inhibitor in co-development with Altana
With the recent approval of Teflaro[TM], the resubmission of Daxas, and the continuing evolution of our pipeline products, as well as the strong performance of our currently marketed products, this is an appropriate time to retire and pursue personal and academic interests.
In the quarter, the company also launched three new medicines: the intravenous (IV) formulation of BRINAVESS (vernakalant) for the treatment of atrial fibrillation in adults in the European Union (EU), Iceland and Norway; DULERA (mometasone furoate and formoterol fumarate dihydrate) for the treatment of asthma in the United States; and DAXAS (roflumilast) for the treatment of symptomatic COPD in Canada and certain European markets, through a partnership.
The new data analyses presented at ERS include a post hoc analysis of the Daxas (roflumilast) phase III trials showing that fewer patients using Daxas suffered from frequent exacerbations compared to placebo and that time to first, second and third exacerbations was significantly extended.