COMMON BRAND NAME(S): Arava
GENERIC NAME(S): LEFLUNOMIDE
Description: Leflunomide is an immunomodulating agent and DMARD that inhibits pyrimidine synthesis. It inhibits dihydroorotate dehydrogenase enzyme activity resulting in antiproliferative and anti-inflammatory effects.
Absorption: Bioavailability: Approx 82-95%. Time to peak plasma concentration (active metabolite): 6-12 hr.
Distribution: Volume of distribution: 0.13 L/kg. Plasma protein binding (active metabolite): 99% (mainly albumin).
Metabolism: Rapidly converted to active metabolite A77 1726 in GI mucosa and the liver.
Excretion: Via urine (approx 43% as glucuronides) and faeces (approx 48%). Elimination half-life (active metabolite): Approx 14-18 days.