Leflunomide (Leflunomide)
Overview of Leflunomide
Leflunomide is used for its immunosuppressant properties, in the treatment of moderate to severe active rheumatoid arthritis and in active psoriatic arthritis. The immunosuppressant properties are partly due to the action of its active metabolite A77-1726 in inhibiting pyrimidine synthesis. Leflunomide is under invastiagation for its use in organ and tissue transplantation.
Indication of Leflunomide
Leflunomide is primarily indicated in conditions like Psoriatic arthritis, Sedative in combined anaesthesia.
Contraindication of Leflunomide
Leflunomide is contraindicated in conditions like Hepatic impairment,Pregnancy,Serious infections,Breast feeding,Reversal of hypotension from spinal/epidural anaesthesia,Inotropic support, see instruction.
Side Effects of Leflunomide
The severe or irreversible adverse effects of Leflunomide, which give rise to further complications include Thrombocytopenia, Hepatotoxicity, Hypokalemia, Stevens johnson syndrome, Stevens johnson syndrome, Hepatotoxicity, Bone marrow toxicity.,The symptomatic adverse reactions produced by Leflunomide are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Headache, Alopecia, Anorexia, Diarrhea, Abdominal pain, Rashes, Pruritus, Weight LossX, Asthenia, Nausea and vomiting, Dry skin, Increased BP, Paresthesias, Eczema, Oral mucosal disorders, Rarely taste disrurbances, Alopecia, dizziness.
Precautions of Leflunomide
Renal impairment; impaired bone-marrow function including anaemia, leucopenia, or thrombocytopenia (avoid if significant and due to causes other than rheumatoid arthritis); recent treatment with other hepatotoxic or myelotoxic disease-modifying antirheumatic drugs (avoid concomitant use); history of tuberculosis; exclude pregnancy before treatment; effective contraception essential during treatment and for at least 2 years after treatment in women and atleast 3 months after treatment in men (plasma concentration monitoring required; waiting time before conception may be reduced with washout procedures; monitor full blood count (including differential white cell count and platelet count before treatment and every 2 weeks for 6 months then every 8 weeks; maonitor liver function; monitor blood pressure; washout procedures recommended for serious adverse effects and before transferring to other disease-modifying antirheumatic drugs. HEPATOTOXICITY. Potentially life threatening hepatotoxicity reported usually in the first 6 months; monitor liver function before treatment and at least monthly for first 6 months then every 2 months. Discontinue treatment or reduce dose a/c to liver function abnormality; if liver function abnormality persits after dose reduction, discontinue treatment and institute washout procedure. WASHOUT PROCEDURES: To aid drug elemination in case of serious adverse effect, before starting another disease-modifying antirheumatic drug, or before conception, stop treatment give either colestyramine 8g 3 times daily for 11 days or activated charcoal 50g 4 times daily for 11 days; the concentration of active metabolite after washout should be < 20 micrograms /lit (measured on 2 occasions 14 days apart) in men or women before conception.