Comparative Pharmacology
Head-to-head clinical analysis: ARAVA versus LEFLUNOMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARAVA versus LEFLUNOMIDE.
ARAVA vs LEFLUNOMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Leflunomide inhibits dihydroorotate dehydrogenase (DHODH), a key enzyme in de novo pyrimidine synthesis, thereby reducing T cell proliferation.
Inhibits dihydroorotate dehydrogenase (DHODH), blocking de novo pyrimidine synthesis, thereby reducing lymphocyte proliferation.
100 mg orally once daily for 3 days (loading dose), then 20 mg orally once daily (maintenance); if not tolerated, may reduce to 10 mg orally once daily.
100 mg PO once daily for 3 days (loading dose), then 20 mg PO once daily (maintenance); may reduce to 10 mg PO once daily if not tolerated.
None Documented
None Documented
The terminal elimination half-life of teriflunomide is approximately 18–19 days due to enterohepatic recirculation. This long half-life necessitates a loading dose and may prolong time to steady state (>3 months).
Clinical Note
moderateLeflunomide + Digitoxin
"Leflunomide may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateLeflunomide + Deslanoside
"Leflunomide may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateLeflunomide + Acetyldigitoxin
"Leflunomide may decrease the cardiotoxic activities of Acetyldigitoxin."
Clinical Note
moderateLeflunomide + Ouabain
"Leflunomide may decrease the cardiotoxic activities of Ouabain."
Terminal half-life of teriflunomide is approximately 18-19 days (range 14-58 days) due to enterohepatic recirculation; clinical significance: prolonged washout required before switching to other disease-modifying antirheumatic drugs (DMARDs) or in case of toxicity.
Following oral administration, ~90% of a dose is excreted in feces (primarily as parent drug and M1 metabolite) and ~10% in urine (M1 metabolite). Biliary excretion is a major route for the active metabolite teriflunomide.
Primarily fecal (~48%) and renal (~43%) as metabolites. Teriflunomide, the active metabolite, undergoes enterohepatic recirculation and is eliminated via bile and feces. Less than 1% excreted as unchanged drug.
Category C
Category D/X
DMARD
DMARD