Roflumilast

Roflumilast
Systematic (IUPAC) name
3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
Clinical data
Trade names Daxas,Daliresp
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a611034
License data
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
administration
Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability 79%[1][2][3][4]
Protein binding 99%[1][2][3][4]
Metabolism Hepatic via CYP1A2 & CYP3A4[1][2][3][4]
Biological half-life 17 hours (30 hours [active metabolite])[1][2][3][4]
Excretion Urine (70%)[1][2][3][4]
Identifiers
CAS Number 162401-32-3 N
ATC code R03DX07 (WHO)
PubChem CID 449193
IUPHAR/BPS 6962
ChemSpider 395793 N
UNII 0P6C6ZOP5U YesY
ChEBI CHEBI:47657 N
ChEMBL CHEMBL193240 N
Chemical data
Formula C17H14Cl2F2N2O3
Molar mass 403.207 g/mol
 NYesY (what is this?)  (verify)

Roflumilast (trade names Daxas, Daliresp) is a drug that acts as a selective, long-acting inhibitor of the enzyme PDE-4 (Phosphodiesterase-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, Daxas was approved in the EU for severe COPD associated with chronic bronchitis.[9] In March 2011, Daliresp 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]

References

  1. 1 2 3 4 5 6 7 "DALIRESP (roflumilast) tablet [Forest Laboratories, Inc.]" (PDF). DailyMed. Forest Laboratories, Inc. August 2013. Retrieved 18 November 2013.
  2. 1 2 3 4 5 6 7 "DAXAS 500 micrograms film-coated tablets". electronic Medicines Compendium. Takeda UK Ltd. 9 September 2013. Retrieved 18 November 2013.
  3. 1 2 3 4 5 6 7 "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Retrieved 18 November 2013.
  4. 1 2 3 4 5 6 7 "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". 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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