Pharmacokinetics leflunomide

Pharmacokinetics Leflunomide is well absorbed after oral administration. It is extensively bound to albumin (>90 percent), and has a half-life of 14 to 18 days. [Note Because of its long half-life, loading doses are necessary (see p. 19).] Leflunomide is rapidly converted to the active metabolite. The metabolites are excreted in the urine and the feces. The active metabolite undergoes biliary recycling. 

D. Pharmacokinetics and Clinical Use Sulfasalazine, hydroxychloroquine, methotrexate, cyclosporine, penicillamine and leflunomide are given orally. Infliximab and etanercept are given by injection. Gold compounds are available for parenteral use (gold sodium thiomalate and au-rothioglucose) and for oral administration (auranofin). 

Leflunomide was given to healthy women taking a triphasic oral contraceptive containing 30 micrograms of ethinylestradiol. During the study it was found that the leflunomide had no effect on the activity of the oral contraceptive and the pharmacokinetics of the active metabolite of leflunomide (A771726) were not changed to a clinically relevant extent. No special precautions would therefore appear to be needed on concurrent use. 

Weinblatt ME, Kremer Coblyn JS, Maier AL, Helfgott SM, Mcnell M, Byrne VM, Kay-makcianMV, Sttand V. Pharmacokinetics, safety, and efficacy of combination treatment with methottexate and leflunomide in patients widi active rheumatoid arthritis. Ar iritis Rheum... 

Gates BJ, Nguyen TT, Setter SM, devies NM (2005) Meloxicam a reappraisal of pharmacokinetics, efficacy and safety. Expert Opin Pharmacother 6 2117-2140 Veber DF, Johnson SR, Cheng HY, Smith BR, Ward KW, Kopple KD (2002) Molecular properties that influenee the oral bioavailability of drug candidates. J Med Chem 45 2615-2623 Prakash A, Jarvis B (1999) Leflunomide a review of its use in active rheumatoid arthritis. Drugs 58 1137-1164... 

Rozman B. Clinical pharmacokinetics of leflunomide. Clin Pharmacokinet 2002 41 421 30. 

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