roflumilast

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Related to Daxas: Roflumilast

roflumilast

(row-floo-mi-last) ,

Daliresp

(trade name),

Daxas

(trade name)

Classification

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

Indications

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

Action

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.

Pharmacokinetics

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)

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

Contraindications/Precautions

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

Dermatologic

  • rash

Gastrointestinal

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

Metabolic

  • weight loss

Musculoskeletal

  • muscle spasms

Neurologic

  • tremor

Miscellaneous

  • hypersensitivity reactions including angioedema (life-threatening)

Interactions

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.

Route/Dosage

Oral (Adults) 500 mcg once daily.

Availability

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

Implementation

  • 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).

roflumilast

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 ?
The National Institute for Health and Care Excellence (NICE) has rejected AstraZeneca's Daxas (roflumilast) as a treatment for chronic obstructive pulmonary disease (COPD), Pharmafile reported on Monday.
Daxas should be available on prescription at the end of the summer.
AstraZeneca's (LON: AZN) drug Daxas has been rejected by the National Institute for Health and Care Excellence (NICE) as an NHS treatment for certain patients with chronic obstructive pulmonary disease (COPD), Pharma Times reported on Friday.
The deal will include the expansion of rights to roflumilast (marketed as Daliresp in the US and Daxas in other countries), the only approved oral PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD).
The acquisition includes the roflumilast franchise (Daliresp in the United States and the Daxas trade name in Europe), a first-in-class treatment for chronic obstructive pulmonary disease that is expected to be a major source of revenue growth for Takeda.
The expert panel voted 10-5 not to recommend approval for Daxas for chronic obstructive pulmonary disease.
In addition, we are hopeful to obtain FDA approval later this quarter for Daxas (roflumilast), for the treatment of COPD.
Under the terms of the agreement, AstraZeneca will acquire the respiratory business including products Daxas (roflumilast), Alvesco and Omnaris (ciclesonide).
8 December 2011 - The UK's National Institute for Health and Clinical Excellence (NICE) requested more data in order to be able to evaluate the effectiveness of Nycomed's oral respiratory medicine Daxas (roflumilast) and recommended a new clinical trial.
Nycomed and Forest Laboratories have entered into a collaboration and distribution agreement for Daxas in the U.
Nycomed spokeswoman Beatrix Benz said in a statement Daxas had drawn "great interest" from parties proposing to commercialize the drug in the United States.
M2 PHARMA-September 26, 2011-Nycomed's Daxas prevents exacerbations in COPD patients(C)2011 M2 COMMUNICATIONS