Arava
Brand names,
Arava
Analogs
Arava
Brand Names Mixture
Arava
Chemical_Formula
C12H9F3N2O2
Arava
RX_link
http://www.rxlist.com/cgi/generic3/leflunomide.htm
Arava
fda sheet
Arava
msds (material safety sheet)
Arava
Synthesis Reference
No information avaliable
Arava
Molecular Weight
270.207 g/mol
Arava
Melting Point
165-166 oC
Arava
H2O Solubility
21 mg/L (poorly soluble)
Arava
State
Solid
Arava
LogP
2.659
Arava
Dosage Forms
Tablet
Arava
Indication
For the treatment of active rheumatoid arthritis (RA).
Arava
Pharmacology
Leflunomide is a pyrimidine synthesis inhibitor indicated in adults for the treatment of active rheumatoid arthritis (RA). RA is an auto-immune disease characterized by high T-cell activity. T cells have two pathways to synthesize pyrimidines: the salvage pathways and the de novo synthesis. At rest, T lymphocytes meet their metabolic requirements by the salvage pathway. Activated lymphocytes need to expand their pyrimidine pool 7- to 8-fold, while the purine pool is expanded only 2- to 3-fold. To meet the need for more pyrimidines, activated T cells use the de novo pathway for pyrimidine synthesis. Therefore, activated T cells, which are dependent on de novo pyrimidine synthesis, will be more affected by leflunomide's inhibition of dihydroorotate dehydrogenase than other cell types that use the salvage pathway of pyrimidine synthesis.
Arava
Absorption
Well absorbed, peak plasma concentrations appear 6-12 hours after dosing
Arava
side effects and Toxicity
LD50=100-250 mg/kg (acute oral toxicity)
Arava
Patient Information
No information avaliable
Arava
Organisms Affected
Humans and other mammals