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