Mr. Ibrahem/Leflunomide
Clinical data
Trade namesArava, Lefumide, Arabloc, others
AHFS/Drugs.comMonograph
MedlinePlusa600032
License data
Pregnancy
category
  • AU: X (High risk)
Routes of
administration
By mouth (tablets)
Legal status
Legal status
Pharmacokinetic data
Bioavailability80%[1]
Protein binding>99%[1]
MetabolismGI mucosa and liver[1]
Onset of actionWithin 6 wks[2]
Elimination half-life14–18 days[1]
ExcretionFaeces (48%), urine (43%)[1]
Identifiers
  • 5-methyl-N-[4-(trifluoromethyl) phenyl]-isoxazole-4-carboxamide
Chemical and physical data
FormulaC12H9F3N2O2
Molar mass270.211 g·mol−1
3D model (JSmol)
  • O=C(Nc1ccc(cc1)C(F)(F)F)c2c(onc2)C
  • InChI=1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18) checkY
  • Key:VHOGYURTWQBHIL-UHFFFAOYSA-N checkY
  (verify)

Leflunomide, sold under the brand name Arava among others, is a medication used to treat rheumatoid arthritis and psoriatic arthritis and to prevent rejection following organ transplantation.[3][2] It is taken by mouth.[3] Onset is generally within 6 weeks.[2]

Common side effects include diarrhea, liver inflammation, hair loss, and rash.[3] Other side effects may include infections, low platelets, low white blood cells, and cancer.[3] Use during pregnancy may harm the baby.[3] It is an disease-modifying antirheumatic drug (DMARD) and immunosuppressant.[3][2] It works by blocking dihydroorotate dehydrogenase which decreases lymphocytes.[2]

Leflunomide was approved for medical use in the United States in 1998 and Europe in 1999.[3][2] It is available as a generic medication.[4] In the United Kingdom it costs the NHS about £5 as of 2021.[4] In the United States this amount costs about 100 USD.[5]

References edit

  1. ^ a b c d e "Arava (leflunomide) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Archived from the original on 31 May 2019. Retrieved 11 March 2014.
  2. ^ a b c d e f g h "Arava". Archived from the original on 30 March 2021. Retrieved 21 November 2021.
  3. ^ a b c d e f g h i "Leflunomide Monograph for Professionals". Drugs.com. Archived from the original on 2021-04-04. Retrieved 2021-11-21.
  4. ^ a b BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1146. ISBN 978-0857114105.
  5. ^ "Leflunomide Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 6 March 2021. Retrieved 21 November 2021.