Treatment of rheumatoid arthritis

Leflunomide possesses immunomodulating activity, possibly via inhibition of T-cell pyrimidine biosynthesis. The mechanism of action of this agent may differ from that of tacrolimus and cyclosporine.

Oral bioavailability: 81%. Leflunomide is metabolized to a primary active metabolite (M1), with the parent drug rarely detectable in plasma. Protein binding: 99.3%. M1 is eliminated by renal and biliary route. The elimination half-life of M1 is 18 ?? 9 days.

Hypersensitivity to leflunomide products; pregnancy or women who may become pregnant

X

Contraindicated

Alopecia, rash, diarrhea, increased liver enzymes, respiratory tract infection, hypertension.

Loading dose, 100 mg ORALLY daily for 3 days; maintenance, 20 mg ORALLY daily; may reduce dose to 10 mg daily if higher dose not tolerated.

Dosage adjustment in hepatic impairment: If ALT elevations >2 times but ≦3 times ULN are noted, reduce dose to 10 mg/day, and monitor closely. If elevations persist or if elevations >3 times ULN are observed, discontinue leflunomide and initiate protocol