Leflunomide is an isoxazole immunomodulatory agent which inhibits de novo pyrimidine synthesis and has anti-proliferative activity. Following oral administration, it is rapidly metabolized to A771726, which is active in vitro and is presumed to be the active drug in vivo. Leflunomide has demonstrated prophylactic and therapeutic effects in animal models of autoimmune disease. In addition, leflunomide has exhibited anti-inflammatory and weak analgesic and antipyretic activity. In a model of experimental septicemia, leflunomide did not alter the resistance of mice to bacterial pathogens.
ORAL Rheumatoid arthritis; Psoriatic arthritis: Adult: 100 mg daily for 3 days as a loading dose. Maintenance: 10-20 mg daily.
Cholestyramine and activated charcoal may decrease plasma concentration of active metabolite. Concurrent use of methotrexate and other hepatotoxic drugs may increase the risk of hepatotoxicity. Rifampicin increases serum levels of the active metabolite.
Significant hepatic impairment, compromised immune function including bone marrow dysplasia or severe uncontrolled infection; concurrent vaccination w/ live vaccines. Pregnancy, lactation. Renal & hepatic impairment; women w/ childbearing potential. Monitor blood counts & BP regularly. Avoid alcohol.
Thrombocytopenia, anaphylaxis, eosinophilia, leukopenia, pancytopenia. Headache, dizziness, weakness, bronchitis, urinary tract infection, alopecia, rash, dry skin, eczema, pruritus, hypokalaemia, wt loss, arthralgia, joint disorder, leg cramps, rhinitis, sinusitis, hypertension, diarrhoea, nausea, abdominal pain, synovitis, tenosynovitis, paraesthesia, pharyngitis, anorexia, vomiting, oral thrush, stomatitis.Hepatotoxicity.
leflunomide was found to be embryotoxic and teratogenic. Women treated with leflunomide are advised to avoid pregnancy; those who become pregnant are advised to reduce fetal exposure through a cholestyramine drug elimination procedure. leflunomide are contraindicated during pregnancy and lactation.
There is no human experience regarding leflunomide over dosage. In the event of a significant overdose or toxicity, cholestyramine or charcoal administration is recommended to accelerate elimination.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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