Save up -80% on Leflunomide
|Note: this is a drug discount program, not an insurance plan.|
|RX BIN: 015558||RX PCN: HT||Group ID: DDN6600||Card Holder ID: DDN6600|
|Pharmacists and Patients support.|
2019 Price of Arava
|$63.75||30 tablets/20 mg|
|Price with discount in nearest pharmacy. Price may vary.|
We offer free Leflunomide coupons and discounts that may help you save up to 80% off the retail price in your local pharmacy. Just print your coupon! It’s ready to use and never expire. Present your manufacturer copay card in most local pharmacies to get a discount on Leflunomide every time. What are you waiting for? Claim your prescription drug card now!
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Leflunomide volume of distribution
Leflunomide has a low volume of distribution (Vss = 0.13 L/kg) and is extensively bound (>99.3%) to albumin in healthy subjects. Protein binding has been shown to be linear at therapeutic concentrations. The free fraction of M1 is slightly higher in patients with rheumatoid arthritis and approximately doubled in patients with chronic renal failure; the mechanism and significance of these increases are unknown.
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Leflunomide
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs, which are chemically and pharmacologically very heterogeneous. Leflunomide was approved by FDA and in many other countries (e.g., Canada, Europe) in 1999.
Leflunomide mechanism of action
Leflunomide is a prodrug that is rapidly and almost completely metabolized following oral administration to its pharmacologically active metabolite, A77 1726. This metabolite is responsible for essentially all of the drug’s activity in-vivo. The mechanism of action of leflunomide has not been fully determined, but appears to primarily involve regulation of autoimmune lymphocytes. It has been suggested that leflunomide exerts its immunomodulating effects by preventing the expansion of activated autoimmune lymphocytes via interferences with cell cycle progression. In-vitro data indicates that leflunomide interferes with cell cycle progression by inhibiting dihydroorotate dehydrogenase (a mitochondrial enzyme involved in de novo pyrimidine ribonucleotide uridine monophosphate (rUMP)synthesis) and has antiproliferative activity. Human dihydroorotate dehydrogenase consists of 2 domains: an ./.-barrel domain containing the active site and an .-helical domain that forms a tunnel leading to the active site. A77 1726 binds to the hydrophobic tunnel at a site near the flavin mononucleotide. Inhibition of dihydroorotate dehydrogenase by A77 1726 prevents production of rUMP by the de novo pathway; such inhibition leads to decreased rUMP levels, decreased DNA and RNA synthesis, inhibition of cell proliferation, and G1 cell cycle arrest. It is through this action that leflunomide inhibits autoimmune T-cell proliferation and production of autoantibodies by B cells. Since salvage pathways are expected to sustain cells arrested in the G1 phase, the activity of leflunomide is cytostatic rather than cytotoxic. Other effects that result from reduced rUMP levels include interference with adhesion of activated lymphocytes to the synovial vascular endothelial cells, and increased synthesis of immunosuppressive cytokines such as transforming growth factor-. (TGF-.). Leflunomide is also a tyrosine kinase inhibitor. Tyrosine kinases activate signalling pathways leading to DNA repair, apoptosis and cell proliferation. Inhibition of tyrosine kinases can help to treating cancer by preventing repair of tumor cells.
Dosage forms of Leflunomide
|Film-coated tablet||Oral use||10 mg|
|Film-coated tablet||Oral use||100 mg|
|Film-coated tablet||Oral use||20 mg|
5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide 5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide
Humans and other mammals
Indication of Leflunomide
For the management of the signs and symptoms of active rheumatoid arthritis (RA) to improve physical function and to slow the progression of structural damage associated with the disease. Has also been used for the prevention of acute and chronic rejection in recipients of solid organ trasnplants and is designated by the FDA as an orphan drug for this use.
Toxicity of Leflunomide
LD sub50 /sub=100-250 mg/kg (acute oral toxicity)
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