Roflumilast

From WikiProjectMed
Jump to navigation Jump to search
Roflumilast
Roflumilast structure.svg
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
US NLMRoflumilast
MedlinePlusa611034
Legal
License data
Legal status
Pharmacokinetics
Bioavailability79%[4][3][6][7]
Protein binding99%[4][3][6][7]
MetabolismLiver via CYP1A2 & CYP3A4[4][3][6][7]
Elimination half-life17 hours (30 hours [active metabolite])[4][3][6][7]
ExcretionUrine (70%)[4][3][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
 ☒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.[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][5]

Roflumilast was approved for medical use in Europe in 2010 and the United States in 2011.[5][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 clinical use is in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[4][3][6][7][5]

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:[4][3][6][7][11]

  • 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. Retrieved 18 October 2021.
  2. 2.0 2.1 2.2 2.3 2.4 "DailyMed - DALIRESP- roflumilast tablet". dailymed.nlm.nih.gov. Retrieved 18 October 2021.
  3. 3.0 3.1 3.2 3.3 3.4 3.5 3.6 3.7 "Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC)". (emc). 11 June 2020. Retrieved 28 September 2020.
  4. 4.0 4.1 4.2 4.3 4.4 4.5 4.6 4.7 "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Retrieved 28 September 2020.
  5. 5.0 5.1 5.2 5.3 "Daxas EPAR". European Medicines Agency. Retrieved 28 September 2020.
  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. Retrieved 18 November 2013.
  7. 7.0 7.1 7.2 7.3 7.4 7.5 7.6 "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Retrieved 18 November 2013.
  8. "Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"
  9. BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 286. ISBN 978-0-85711-369-6.CS1 maint: date format (link)
  10. "Daliresp Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 18 October 2021.
  11. 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: