User:Mr. Ibrahem/Roflumilast

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Mr. Ibrahem/Roflumilast
drugb
Clinical data
Trade namesDaxas, Daliresp, others
AHFS/Drugs.comMonograph
MedlinePlusa611034
License data
Pregnancy
category
  • AU: B3
Routes of
administration
By mouth
Drug classPhosphodiesterase-4 inhibitor (PDE-4)[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailability79%[3][2][5][6]
Protein binding99%[3][2][5][6]
MetabolismLiver via CYP1A2 & CYP3A4[3][2][5][6]
Elimination half-life17 hours (30 hours [active metabolite])[3][2][5][6]
ExcretionUrine (70%)[3][2][5][6]
Identifiers
  • 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
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 trade name Daxas among others, is a medication used for the long term management of chronic obstructive pulmonary disease (COPD).[1] It is used in those with severe disease.[1] It is taken by mouth.[1]

Common side effects include diarrhea, nausea, headache, back pain, trouble sleeping, and dizziness.[7] Other side effects can include suicide.[7] It is a selective inhibitor of the enzyme phosphodiesterase-4 (PDE-4) and works by decreasing lung inflammation.[1][4]

Roflumilast was approved for medical use in Europe in 2010 and the United States in 2011.[4][8][7] In the United Kingdom it costs the NHS about £38 per month as of 2021.[9] This amount in the United States costs about 430 USD.[10]

References[edit]

  1. ^ a b c d e f g "Roflumilast Monograph for Professionals". Drugs.com. Archived from the original on 25 February 2021. Retrieved 18 October 2021.
  2. ^ a b c d e f "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.
  3. ^ a b c d e f "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Archived from the original on 25 March 2021. Retrieved 28 September 2020.
  4. ^ a b c "Daxas EPAR". European Medicines Agency. Archived from the original on 12 August 2020. Retrieved 28 September 2020.
  5. ^ a b c d e "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.
  6. ^ a b c d e "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Archived from the original on 12 September 2017. Retrieved 18 November 2013.
  7. ^ a b c d "DailyMed - DALIRESP- roflumilast tablet". dailymed.nlm.nih.gov. Archived from the original on 25 March 2021. Retrieved 18 October 2021.
  8. ^ ""Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"". Archived from the original on 2017-08-24. Retrieved 2021-07-21.
  9. ^ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 286. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  10. ^ "Daliresp Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 11 April 2021. Retrieved 18 October 2021.