Leflunomide
Leflunomide Brand names, Leflunomide Analogs
Leflunomide Brand Names Mixture
- No information avaliable
Leflunomide Chemical_Formula
C12H9F3N2O2
Leflunomide RX_link
http://www.rxlist.com/cgi/generic3/leflunomide.htm
Leflunomide fda sheet
Leflunomide msds (material safety sheet)
Leflunomide Synthesis Reference
No information avaliable
Leflunomide Molecular Weight
270.207 g/mol
Leflunomide Melting Point
165-166 oC
Leflunomide H2O Solubility
21 mg/L (poorly soluble)
Leflunomide State
Solid
Leflunomide LogP
2.659
Leflunomide Dosage Forms
Tablet
Leflunomide Indication
For the treatment of active rheumatoid arthritis (RA).
Leflunomide 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.
Leflunomide Absorption
Well absorbed, peak plasma concentrations appear 6-12 hours after dosing
Leflunomide side effects and Toxicity
LD50=100-250 mg/kg (acute oral toxicity)
Leflunomide Patient Information
No information avaliable
Leflunomide Organisms Affected
Humans and other mammals
