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.
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.

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
Leflunomide is contraindicated in conditions like Hepatic impairment, Pregnancy, Serious infections, Breast feeding, Reversal of hypotension from spinal/epidural anaesthesia, Inotropic support, see instruction.
Dosage
Leflunomide's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 100 mg | 100 mg | Every 24h | PO | For 3 days. Then 10-20 mg QD for maintenance. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
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
Interference in Pathology
Leflunomide may interfere in the diagnosis of Tests for ALT, AST, and serum albumin, Monitoring of liver enzymes.
Available Brands
Drug Classification
- 1.2.4 — Disease modifying antirheumatic drugs