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.


Adult Dose
Dose: 100 mg
Single Dose: 100 (100)
Frequency: 24 hourly
Route: PO
Instructions: For 3 days. Then 10-20 mg QD for maintenance.
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin and belongs to Pyrimidine synthes inhibitor. . The Molecular Weight of Leflunomide is 270.23.
Contraindications
Leflunomide is contraindicated in conditions like Pregnancy,Serious infections,Hepatic impairment,Breast feeding,Reversal of hypotension from spinal/epidural anaesthesia,Inotropic support, see instruction.
Effects
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.
Indications
Leflunomide is primarily indicated in conditions like Psoriatic arthritis, Sedative in combined anaesthesia.
Interactions
Leflunomide is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementCladribineMumps VaccineConcurrent use may weaken the immune system.RituximabThe use of leflunomide in combination with other immunosuppressive or myelosuppressive agents may increase the risk of infections. Serious infections including sepsis, as well as opportunistic infections like Pneumocystis jiroveci pneumonia, pulmonary and extrapulmonary tuberculosis, and aspergillosis have been reported with the use of leflunomide, particularly in patients on concomitant immunosuppressive therapy.MajorClose monitoring for the development of infection is recommended if leflunomide is used in patients who have recently received or are receiving other immunosuppressive or myelosuppressive agents. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Tests for ALT, AST, and serum albuminMonitoring of liver enzymes
Risks
Drug should not be given to Pregnant Mothers, patients suffering from Kidney dysfunction, and patients suffering from Liver Malfunction.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Warnings
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
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