title: Leflunomide in dialysis patients with rheumatoid arthritis--a pharmacokinetic study.
abstract: Pharmacokinetic data of disease modifying antirheumatic drugs during hemodialysis are limited to sulfasalazine, methotrexate, and cyclosporine. Only respective anecdotal data have been reported on leflunomide. We repeatedly measured teriflunomide (A77-1726), the active metabolite of leflunomide, during standard hemodialysis sessions and calculated teriflunomide clearances in five patients with rheumatoid arthritis (RA) and end-stage renal disease. The calculated teriflunomide clearances during a standardized dialysis session of 3-4.5 h at a blood flow rate of 160-300 ml/min were between 0 and 4.3 ml/min, the mean clearances of the total dialysis ranged between 1.1 and 3.4 ml/min. Total amount of teriflunomide removed was 5.8-8.8 μg per dialysis session. Dialytic removal of the active metabolite of leflunomide, teriflunomide (A77-1726), is negligible. Leflunomide can be used for RA patients on chronic dialysis without any dosage modification.
authors.affiliation: Medizinische Klinik A, Klinikum Ludwigshafen, Bremserstraße 79, 67063 Ludwigshafen, Germany. bergnerr@klilu.de
authors.forename: Raoul
authors.initials: R
authors.lastname: Bergner
authors.forename: Lena
authors.initials: L
authors.lastname: Peters
authors.forename: Verena
authors.initials: V
authors.lastname: Schmitt
authors.forename: Christian
authors.initials: C
authors.lastname: Löffler
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D018501:Antirheumatic Agents / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001172:Arthritis, Rheumatoid / Q000150:complications / Q000188:drug therapy*; D003437:Crotonates / Q000097:blood / Q000737:chemistry; D005260:Female; D006801:Humans; D006885:Hydroxybutyrates; D007555:Isoxazoles / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007676:Kidney Failure, Chronic / Q000150:complications / Q000628:therapy*; D000077339:Leflunomide; D008297:Male; D008875:Middle Aged; D008954:Models, Biological; D009570:Nitriles; D006435:Renal Dialysis; D012189:Retrospective Studies; D014052:Toluidines / Q000097:blood / Q000737:chemistry
chemical_list: D018501:Antirheumatic Agents; D003437:Crotonates; D006885:Hydroxybutyrates; D007555:Isoxazoles; D009570:Nitriles; D014052:Toluidines; C527525:teriflunomide; D000077339:Leflunomide