- Lefluno 10mg Tablet Contains
- Lefluno 20mg Tablet Contains
What is Lefluno Used For?
Lefluno is Indicated in adults for the treatment of active rheumatoid arthritis (RA) to reduce signs and symptoms and to retard structural damage as evidenced by X-ray erosions and joint space narrowing.
Aspirin (e.g. Ascard), nonsteroidal anti-inflammatory agents and/or low dose corticosteroids may be continued during treatment with Lefluno Tablets. The combined use of Lefluno with anti-malarial drugs, intramuscular or oral gold, D penicillamine, azathioprine, or methotraxate has not been adequately studied.
How Lefluno Works?
Lefluno is an isoxazole immunomodulatory agent which inhibits dihydroorotate dehydrogenase (an enzyme involved in de novo pyrimidine synthesis) and has anti-proliferative activity. Several in vivo and in vitro experimental models have demonstrated an anti-inflammatory effect.
Following oral administration, Lefluno Tablet (leflurtomide) is metabolized to an active metabolite A77 1726 (hereafter referred to as M1) which is responsible for essentially all of its activity in vivo. Plasma levels of Lefluno are occasionally seen at very low levels. Studies of the pharmacokinetics of leflunomide have primarily examined the plasma concentrations of this active metabolite.
Recommended Dosage of Lefluno Tablets
- Loading Dose
Due to the long half-life in patients with Rheumatoid Arthritis and recommended dosing interval (24 hours), a loading dose is needed to provide steady-state concentrations more rapidly. It is recommended that therapy with Lefluno Tablets be initiated with a loading dose of 100 mg tablet per day for 3 days.
- Maintenance Therapy
Daily dosing of 20 mg is recommended for treatment of patients with Rheumatoid Arthritis. Doses higher than 20 mg/day are not recommended. If dosing at 20 mg/day is not well tolerated clinically, the dose may be decreased to 10 mg daily. Liver enzymes should be monitored and dose adjustments may be necessary. Due to the prolonged half-life of the active metabolite of Lefluno (leflunomide), patients should be carefully observed after dose reduction, since it may take several weeks for metabolite levels to decline.
Side Effects of Lefluno
Most common side effects associated with Lefluno therapy include diarrhea, elevated liver enzymes, alopecia and rash.
Lefluno during Pregnancy and Lactation
Pregnancy should be avoided during treatment with Lefluno. If pregnancy is planned, follow the drug elimination procedure.
Lefluno should not be used by nursing mothers. It is not known whether leflunomide is excreted in human milk. Many drugs are excreted in human milk and there is a potential for serious adverse reactions in nursing infants from Lefluno. Therefore, a decision should be made whether to proceed with nursing or to initiate treatment with Lefluno, taking into account the importance of the drug to the mother.
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