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Related to roflumilast: indacaterol, PDE4 inhibitor


(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).
Drug Guide, © 2015 Farlex and Partners


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.
Segen's Medical Dictionary. © 2012 Farlex, Inc. All rights reserved.
References in periodicals archive ?
Roflumilast inhibits the release of chemokines and TNF-a from human lung macrophages stimulated with lipopolysaccharide.
* Management of exacerbation-prone patients with COPD includes vaccinations, addition of a phosphodiesterase-4 inhibitor, roflumilast and daily azithromycin and NAC.
"One of the most promising new treatments for COPD is Roflumilast, a first-in-class phosphodiesterase (PDE4) inhibitor that is the only licensed oral therapy that targets COPD-specific inflammation," said Dr Osama Al-Nawasany, medical affairs director, Takeda Pharmaceuticals.
Takeda said the acquisition includes the roflumilast franchise, a market-leading treatment for chronic lung disease, which is expected to be a major source of revenue growth for the Japanese firm.
--By Risk & Insurance and Healthesystems 2011 New Drug Products Likely to Impact Work Comp Gralise[R] Neuropathic pain (gabapentin extended-release) Viibryd[R] Antidepressant (vilazodone) Abstral[R] Opioid Analgesic (fentanyl sublingual tablet) Edarbi[R] High Blood Pressure (azilsartan) Daliresp[R] Chronic obstructive (roflumilast) disease (COPD)
The pill, Roflumilast, tested by patients at University Hospital Aintree, treats one of the world's biggest killers - chronic obstructive pulmonary disease (COPD), a term for chronic bronchitis and emphysema.
Announcing the Cork project as part of its 2003 investment programme, Altana said the Roflumilast tablet-producing factory in Cork was to be its biggest investment for the year.
(2) For group D patients, initial therapy with LABA/LAMA and escalation to LABA/LAMA/ICS or switching to ICS/LABA is recommended, with subsequent addition of roflumilast or a macrolide if frequent exacerbations persist.
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.
Coinhalation of roflumilast and fluticasone, which reduces the counts of both neutrophils and eosinophils in BALF, could significantly improve the inflammatory condition in OVA-induced mice compared with the combination of formoterol and fluticasone [80].