Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Roflumilast

From Wikipedia, the free encyclopedia
Medication

Pharmaceutical compound
Roflumilast
Clinical data
Trade namesDaxas, Daliresp, Zoryve, others
AHFS/Drugs.comMonograph
MedlinePlusa611034
License data
Pregnancy
category
Routes of
administration
By mouth,topical
Drug classPDE4 inhibitor
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability79%[4][3][8][9]
Protein binding99%[4][3][8][9]
MetabolismHepatic viaCYP1A2 &CYP3A4[4][3][8][9]
Eliminationhalf-life17 hours (30 hours [active metabolite])[4][3][8][9]
ExcretionUrine (70%)[4][3][8][9]
Identifiers
  • 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard(EPA)
ECHA InfoCard100.210.960Edit this at Wikidata
Chemical and physical data
FormulaC17H14Cl2F2N2O3
Molar mass403.21 g·mol−1
3D model (JSmol)
  • C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
  • InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24) ☒N
  • Key:MNDBXUUTURYVHR-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Roflumilast, sold under the brand nameDaxas among others, is a medication used for the treatment ofchronic obstructive pulmonary disease,[4]plaque psoriasis,[5]seborrheic dermatitis,[6] andatopic dermatitis.[5] It acts as a selective, long-actinginhibitor of the enzyme phosphodiesterase-4 (PDE-4).[10] It hasanti-inflammatory effects.[10][11][12]

It was approved for medical use in the European Union in 2010,[7] in the United States in 2011,[4] and in Canada in 2017.[1] It is available as ageneric medication.[13]

Medical uses

[edit]

Roflumilast isindicated for the treatment of severe chronic obstructive pulmonary disease (COPD),[4] plaquepsoriasis,[5][14] seborrheic dermatitis,[6] and atopic dermatitis,[5][15]

It is used in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[3][4][7][8][9]

Adverse effects

[edit]

Common (1–10% incidence) adverse effects include diarrhea, weight loss, nausea, headache, insomnia, decreased appetite, abdominal pain, rhinitis, sinusitis, urinary tract infection, and depression.[4][3][8][9][16]

Society and culture

[edit]

Legal status

[edit]

In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis.[7][17] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations.[18][19]

References

[edit]
  1. ^ab"Daxas Product information".Health Canada. 20 July 2017. Retrieved13 July 2024.
  2. ^"Zoryve Product information".Health Canada. 7 November 2023. Retrieved13 July 2024.
  3. ^abcdefgh"Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC)".(emc). 11 June 2020.Archived from the original on 19 September 2020. Retrieved28 September 2020.
  4. ^abcdefghijk"Daliresp- roflumilast tablet".DailyMed. 12 March 2020.Archived from the original on 25 March 2021. Retrieved28 September 2020.
  5. ^abcde"Zoryve- roflumilast cream".DailyMed. 16 August 2022.Archived from the original on 21 January 2023. Retrieved21 January 2023.
  6. ^abc"Zoryve- roflumilast aerosol, foam".DailyMed. 20 December 2023. Retrieved13 July 2024.
  7. ^abcd"Daxas EPAR".European Medicines Agency. 17 September 2018.Archived from the original on 12 August 2020. Retrieved28 September 2020.
  8. ^abcdefg"Daliresp : EPAR - Product Information"(PDF).European Medicines Agency. Takeda GmbH. 26 September 2013.Archived(PDF) from the original on 26 June 2016. Retrieved18 November 2013.
  9. ^abcdefg"roflumilast (Rx) - Daliresp".Medscape Reference. WebMD.Archived from the original on 12 September 2017. Retrieved18 November 2013.
  10. ^abBoswell-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.
  11. ^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.S2CID 19050454.
  12. ^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.S2CID 73241684.
  13. ^"2022 First Generic Drug Approvals".U.S.Food and Drug Administration (FDA). 3 March 2023.Archived from the original on 30 June 2023. Retrieved30 June 2023.
  14. ^"FDA Approves Arcutis' Zoryve (Roflumilast) Cream 0.3% For the Treatment of Plaque Psoriasis in Individuals Age 12 and Older" (Press release). Arcutis Biotherapeutics. 29 July 2022.Archived from the original on 1 August 2022. Retrieved1 August 2022 – via GlobeNewswire.
  15. ^"FDA Approves Atopic Dermatitis Label Expansion for Arcutis' Zoryve Cream".BioSpace. Retrieved13 July 2024.
  16. ^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.
  17. ^""Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"".Archived from the original on 24 August 2017. Retrieved10 July 2010.
  18. ^"Drug Approval Package: Daliresp Tablets (roflumilast) NDA #022522".U.S.Food and Drug Administration (FDA). 24 December 1999.Archived from the original on 27 October 2020. Retrieved28 September 2020.
  19. ^"FDA approves new drug to treat chronic obstructive pulmonary disease" (Press release). U.S.Food and Drug Administration (FDA). 1 March 2011. Archived fromthe original on 18 January 2017. Retrieved16 December 2019.

Further reading

[edit]
Adrenergics,inhalants
Short-acting β2 agonists
Long-acting β2 agonists
Ultra-long-acting β2 agonists
Other
Glucocorticoids
Anticholinergics/
muscarinic antagonist
Mast cell stabilizers
Xanthines
Eicosanoid inhibition
Leukotriene antagonists
Arachidonate 5-lipoxygenase inhibitors
Thromboxane receptor antagonists
Non-xanthinePDE4 inhibitors
Others/unknown
Combination products
PDE1
PDE2
PDE3
PDE4
PDE5
PDE7
PDE9
PDE10
PDE11
Non-selective
Unsorted
Products
Predecessors and
acquired companies
People
Portal:
Retrieved from "https://en.wikipedia.org/w/index.php?title=Roflumilast&oldid=1235492503"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp