Cannabaceae

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Roflumilast
Clinical data
Trade namesDaxas, Daliresp, Zoryve, others
AHFS/Drugs.comMonograph
MedlinePlusa611034
License data
Pregnancy
category
  • AU: B3
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 via CYP1A2 & CYP3A4[4][3][8][9]
Elimination half-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
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.210.960 Edit 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 name Daxas among others, is a medication used for the treatment of chronic obstructive pulmonary disease,[4] plaque psoriasis,[5] seborrheic dermatitis,[6] and atopic dermatitis.[5] It acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4).[10] It has anti-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 a generic medication.[13]

Medical uses

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Roflumilast is indicated for the treatment of severe chronic obstructive pulmonary disease (COPD),[4] plaque psoriasis,[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

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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

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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

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  1. ^ a b "Daxas Product information". Health Canada. 20 July 2017. Retrieved 13 July 2024.
  2. ^ "Zoryve Product information". Health Canada. 7 November 2023. Retrieved 13 July 2024.
  3. ^ a b c d e f g h "Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC)". (emc). 11 June 2020. Archived from the original on 19 September 2020. Retrieved 28 September 2020.
  4. ^ a b c d e f g h i j k "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Archived from the original on 25 March 2021. Retrieved 28 September 2020.
  5. ^ a b c d e "Zoryve- roflumilast cream". DailyMed. 16 August 2022. Archived from the original on 21 January 2023. Retrieved 21 January 2023.
  6. ^ a b c "Zoryve- roflumilast aerosol, foam". DailyMed. 20 December 2023. Retrieved 13 July 2024.
  7. ^ a b c d "Daxas EPAR". European Medicines Agency. 17 September 2018. Archived from the original on 12 August 2020. Retrieved 28 September 2020.
  8. ^ a b c d e f g "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Archived (PDF) from the original on 26 June 2016. Retrieved 18 November 2013.
  9. ^ a b c d e f g "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Archived from the original on 12 September 2017. Retrieved 18 November 2013.
  10. ^ a b 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.
  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. Retrieved 30 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. Retrieved 1 August 2022 – via GlobeNewswire.
  15. ^ "FDA Approves Atopic Dermatitis Label Expansion for Arcutis' Zoryve Cream". BioSpace. Retrieved 13 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. Retrieved 10 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. Retrieved 28 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 from the original on 18 January 2017. Retrieved 16 December 2019.

Further reading

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source: https://en.wikipedia.org/wiki/Roflumilast

One thought on “Cannabaceae”

  1. Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
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