Leflunomide (Arava)

A pyrimidine synthesis inhibitor that blocks T cell clonal expansion.

A medication of the DMARD (disease -modifying antirheumatic drug) type, used in active moderate to severe rheumatoid arthritis and psoriatic arthritis.

Oral administration as tablets containing 10, 20, or 100 mg of active drug.

An immunomodulatory drug inhibiting dihydroorotate dehydrogenaseJean.

Antiproliferative activity and anti-inflammatory effect.

Slows progression of the disease and causes remission/relief of symptoms of rheumatoid arthritis and psoriatic arthritis.

Is metabolized to teriflunomide, which is responsible for all of the drug’s activity.

Due to its very long half-life of approximately 2 weeks, a loading dose of 100 mg for 3 days is used in clinical studies to reach steady-state levels quickly, but one study showed fewer adverse effects and good efficacy if no loading dose is used at the beginning of treatment with leflunomide of patients with rheumatoid arthritis.

Daily dosing of 20 mg is recommended for treatment of patients with RA.

Inhibits structural damage as evidenced by X-ray erosions and joint space narrowing and improves physical function, with onset of clinical improvement can be expected after 4 to 6 weeks of continued therapy.

Aspirin, or other nonsteroidal anti-inflammatory agents, and/or low-dose corticosteroids may be continued during treatment with leflunomide.

Concomitant use of methotrexate may lead to severe or even fatal hepatotoxicity, and this combination of medications accounted in the past for most cases of liver toxicity.

ACR response rate in rheumatoid arthritis 45% at 1 year.

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