Roflumilast

Roflumilast
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
ATC code R03DX07 (WHO)
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
PubChem (CID) 449193
IUPHAR/BPS 6962
ChemSpider 395793 N
UNII 0P6C6ZOP5U YesY
ChEBI CHEBI:47657 N
ChEMBL CHEMBL193240 N
Chemical and physical data
Formula C17H14Cl2F2N2O3
Molar mass 403.207 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)

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, 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 2695611Freely accessible. 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 2567892Freely accessible. PMID 18660825.


This article is issued from Wikipedia - version of the 6/7/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.