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Roflumilast structure.svg
Roflumilast ball-and-stick model.png
Clinical data
Trade namesDaxas, Daliresp
AHFS/Drugs.comConsumer Drug Information
License data
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding99%[1][2][3][4]
MetabolismHepatic via CYP1A2 & CYP3A4[1][2][3][4]
Elimination half-life17 hours (30 hours [active metabolite])[1][2][3][4]
ExcretionUrine (70%)[1][2][3][4]
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.210.960 Edit this at Wikidata
Chemical and physical data
Molar mass403.207 g/mol g·mol−1
3D model (JSmol)
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Roflumilast (trade names Daxas, Daliresp) is a drug that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).[5][6][7][8]

In June 2010, it was approved in the EU for severe COPD associated with chronic bronchitis.[9] In March 2011, it gained FDA approval in the US for reducing COPD exacerbations.[10]

Medical uses[edit]

Its primary clinical use is in the prevention of exacerbations (lung attacks) in severe COPD.[1][2][3][4]

Adverse effects[edit]

Common (1–10% incidence) adverse effects include:[1][2][3][4][11]

  • Diarrhea
  • Weight loss
  • Nausea
  • Headache
  • Insomnia
  • Decreased appetite
  • Abdominal pain
  • Rhinitis
  • Sinusitis
  • Urinary tract infection
  • Depression


  1. ^ a b c d e f g "DALIRESP (roflumilast) tablet [Forest Laboratories, Inc.]" (PDF). DailyMed. Forest Laboratories, Inc. August 2013. Retrieved 18 November 2013.
  2. ^ a b c d e f g "DAXAS 500 micrograms film-coated tablets". electronic Medicines Compendium. Takeda UK Ltd. 9 September 2013. Retrieved 18 November 2013.
  3. ^ a b c d e f g "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Retrieved 18 November 2013.
  4. ^ a b c d e f g "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Retrieved 18 November 2013.
  5. ^ Boswell-Smith V, Spina D (2007). "PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast". International Journal of Chronic Obstructive Pulmonary Disease. 2 (2): 121–9. PMC 2695611. PMID 18044684.
  6. ^ Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK (May 2008). "Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma". Clinical and Experimental Allergy. 38 (5): 847–56. doi:10.1111/j.1365-2222.2008.02950.x. PMID 18307529.
  7. ^ Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, et al. (August 2008). "Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial" (PDF). Pulmonary Pharmacology & Therapeutics. 21 (4): 616–23. doi:10.1016/j.pupt.2008.02.002. PMID 18374614.
  8. ^ Field SK (May 2008). "Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma". Expert Opinion on Investigational Drugs. 17 (5): 811–8. doi:10.1517/13543784.17.5.811. PMID 18447606.
  9. ^ "Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"
  10. ^ "FDA approves new drug to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration (FDA). March 1, 2011.
  11. ^ Spina D (October 2008). "PDE4 inhibitors: current status". British Journal of Pharmacology. 155 (3): 308–15. doi:10.1038/bjp.2008.307. PMC 2567892. PMID 18660825.