Information about Leflunomide
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.