Roflumilast

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]

Roflumilast
Clinical data
Trade namesDaxas, Daliresp
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611034
License data
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    administration    		Oral
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability79%[1][2][3][4]
    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]
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.210.960
    Chemical and physical data
    FormulaC17H14Cl2F2N2O3
    Molar mass403.207 g/mol g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    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

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

    Adverse effects

    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

    References
    1. "DALIRESP (roflumilast) tablet [Forest Laboratories, Inc.]" (PDF). DailyMed. Forest Laboratories, Inc. August 2013. Retrieved 18 November 2013.
    2. "DAXAS 500 micrograms film-coated tablets". electronic Medicines Compendium. Takeda UK Ltd. 9 September 2013. Retrieved 18 November 2013.
    3. "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Retrieved 18 November 2013.
    4. "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. ISSN 1178-2005. 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 & Experimental Allergy. 38 (5): 847–56. doi:10.1111/j.1365-2222.2008.02950.x. ISSN 1365-2222. PMID 18307529.
    7. Hohlfeld, JM; Schoenfeld, K; Lavae-Mokhtari, M; Schaumann, F; Mueller, M; Bredenbroeker, D; Krug, N; Hermann, R (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. ISSN 1094-5539. 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. ISSN 1354-3784. 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. ISSN 1476-5381. PMC 2567892. PMID 18660825.


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