DrugInfoSys

Leflunomide

Drug #1760

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.

Primary Characteristics

It is of Synthetic origin and belongs to Pyrimidine synthes inhibitor.

Molecular Weight: 270.23 · Solubility in Water: Soluble · Non-proprietary name: Leflunomide.

Molecular structure of Leflunomide

Pharmacokinetics

Absorption: Leflunomide has an oral bioavailability is 88.5% (±6.5%).

Distribution: Leflunomide has a plasma protein binding is >99.3%.

Elimination: plasma half-life is 2 weeks, renal excretion is 43%.

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Indications

Leflunomide is primarily indicated in conditions like Psoriatic arthritis, Sedative in combined anaesthesia.

Contraindications

Dosage

Leflunomide's dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
100 mg100 mgEvery 24hPOFor 3 days. Then 10-20 mg QD for maintenance.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

2 interactions
Major1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Leflunomide in overdosage may give rise to further complications which include Thrombocytopenia , Hepatotoxicity , Hypokalemia , Stevens johnson syndrome , Stevens johnson syndrome , Hepatotoxicity , Bone marrow toxicity .

Leflunomide is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Alopecia, Anorexia , Asthenia , Diarrhea, Dizziness, Dry skin, Eczema, Headache, Increased BP , Nausea and vomiting, Oral mucosal disorders, Paresthesias, Pruritus , Rarely taste disrurbances, Rashes , Weight LossX.

Warnings / Precautions

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.

Interference in Pathology

Leflunomide may interfere in the diagnosis of Tests for ALT, AST, and serum albumin, Monitoring of liver enzymes.

Available Brands

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Single Ingredient

Multi-Ingredient Combinations

Drug Classification

  1. 1.2.4Disease modifying antirheumatic drugs

Manufacturers