Leflunomide

Leflunomid

Information about Leflunomide

Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Liver safety of Leflunomide

Leflunomide therapy is associated with frequent elevations in serum aminotransferase levels and with rare instances of clinically apparent acute liver injury which can be severe and even fatal.

Mechanism of action of Leflunomide

Leflunomide (le floo' noe mide) is an isoxazole derivative that is rapidly converted to its active metabolite teriflunomide (ter" i floo' noe mide: A77-1726) in the gut wall and liver. Leflunomide acts by inhibition of dihydroorotate dehydrogenase, which is a rate limiting step in pyrimidine synthesis necessary for DNA replication of rapidly dividing cells. Activated T lymphocytes are particularly sensitive to the inhibition of pyrimidine synthesis caused by leflunomide. Leflunomide is effective in reducing pain, improving functional status and decreasing the rate of injury in rheumatoid and psoriatic arthritis and is considered a “disease modifying antirheumatic agent (DMARD).” Leflunomide was approved for use in the United States in 1998 and is currently in wide use.

Dosage and administration for Leflunomide

Leflunomide is available in tablets of 10, 20 and 100 mg generically and under the brand name of Arava. The usual recommended dose is 100 mg daily for three days followed by 20 mg daily, reducing the dose of 10 mg daily if tolerance is poor.

Side effects of Leflunomide

Common side effects include fever, rash, alopecia, gastrointestinal upset, nausea and diarrhea.

Antirheumatic Agents

• Gold Preparations

• • Auranofin, Gold salts, Gold sodium thiomalate

• Interleukin receptor antagonists

• • Anakinira, Canakinumab, Rilonacept, Sarilumab, Tocilizumab

• Major immunosuppressive agents

• • Cyclosporine, Mycophenylate, Sirolimus, Tacrolimus

• Monoclonal antibodies

• • Adalimumab, Canakinumab, Certolizumab, Golimumab, Infliximab, Rituximab, Sarilumab, Tocilizumab, Ustekinumab

• Thiopurines

• • Azathioprine, Mercaptopurine, Thioguanine

• Tumor necrosis factor antagonists

• • Adalimumab, Certolizumab, Etanercept, Golimumab, Infliximab

• Tyrosine kinase inhibitors

• • Baricitinib, Tofacitinib

• Miscellaneous

• • Abatacept, Flavocoxid, Hydroxychloroquine, Leflunomide, Methotrexate, Penicillamine

• Dailymed label info on Leflunomide
• FDA Leflunomide