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Roflumilast

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Roflumilast
File:Roflumilast structure.svg
File:Roflumilast ball-and-stick model.png
drugb
Names
Trade namesDaxas, Daliresp, others
  • 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
Clinical data
Drug classPhosphodiesterase-4 inhibitor (PDE-4)[1]
Main usesChronic obstructive pulmonary disease (COPD)[1]
Side effectsDiarrhea, nausea, headache, back pain, trouble sleeping, dizziness[2]
Pregnancy
category
  • AU: B3
  • US: N (Not classified yet)
Routes of
use		By mouth
Typical dose0.5 mg OD[1]
External links
AHFS/Drugs.comMonograph
MedlinePlusa611034
Legal
License data
Legal status
Pharmacokinetics
Bioavailability79%[5][4][6][7]
Protein binding99%[5][4][6][7]
MetabolismLiver via CYP1A2 & CYP3A4[5][4][6][7]
Elimination half-life17 hours (30 hours [active metabolite])[5][4][6][7]
ExcretionUrine (70%)[5][4][6][7]
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

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.[2] Other side effects can include suicide.[2] It is a selective inhibitor of the enzyme phosphodiesterase-4 (PDE-4) and works by decreasing lung inflammation.[1][3]

Roflumilast was approved for medical use in Europe in 2010 and the United States in 2011.[3][8][2] 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]

Medical uses

Its primary use is in the prevention of exacerbations in severe chronic obstructive pulmonary disease (COPD).[5][4][6][7][3] It is however unclear if benefits are greater than harms.[11]

Dosage

It is taken at a dose of 0.5 mg per day.[1] Some people may be started at half the that dose for the first month.[2]

Side effects

Common (1–10% incidence) adverse effects include:[5][4][6][7][12]

  • Diarrhea
  • Weight loss
  • Nausea
  • Headache
  • Insomnia
  • Decreased appetite
  • Abdominal pain
  • Rhinitis
  • Sinusitis
  • Urinary tract infection
  • Depression

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 "Roflumilast Monograph for Professionals". Drugs.com. Archived from the original on 25 February 2021. Retrieved 18 October 2021. Archived 25 February 2021 at the Wayback Machine
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "DailyMed - DALIRESP- roflumilast tablet". dailymed.nlm.nih.gov. Archived from the original on 25 March 2021. Retrieved 18 October 2021. Archived 25 March 2021 at the Wayback Machine
  3. ↑ 3.0 3.1 3.2 3.3 "Daxas EPAR". European Medicines Agency. Archived from the original on 12 August 2020. Retrieved 28 September 2020. Archived 12 August 2020 at the Wayback Machine
  4. ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 4.7 "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. Archived 19 September 2020 at the Wayback Machine
  5. ↑ 5.0 5.1 5.2 5.3 5.4 5.5 5.6 5.7 "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Archived from the original on 25 March 2021. Retrieved 28 September 2020. Archived 25 March 2021 at the Wayback Machine
  6. ↑ 6.0 6.1 6.2 6.3 6.4 6.5 6.6 "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. Archived 26 June 2016 at the Wayback Machine
  7. ↑ 7.0 7.1 7.2 7.3 7.4 7.5 7.6 "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Archived from the original on 12 September 2017. Retrieved 18 November 2013. Archived 12 September 2017 at the Wayback Machine
  8. ↑ ""Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"". Archived from the original on 2017-08-24. Retrieved 2021-07-21. Archived 2017-08-24 at the Wayback Machine
  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. Archived 11 April 2021 at the Wayback Machine
  11. ↑ Ton, Joey (31 October 2011). "#55 Roflumilast – COPD relief at last?". CFPCLearn. Archived from the original on 28 March 2023. Retrieved 18 June 2023. Archived 28 March 2023 at the Wayback Machine
  12. ↑ 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.

External links

External sites:
Identifiers:

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