Tiflamizole elimination from plasma in rheumatoid arthritis.
Tiflamizole is a fluorinated diarylamidazole sulfone nonsteroidal anti-inflammatory drug not metabolized or excreted in urine. Its mean (+/- SD) elimination t 1/2 from plasma was 21.6 +/- 9 days (range 11.8 to 49.5 days) in 17 subjects with rheumatoid arthritis, and appeared to be first order in most of them. Plasma elimination t 1/2 was loosely related (r = -0.67) to stool frequency in eight subjects for whom stool frequency data were available. In one, cholestyramine decreased t 1/2 to 4.1 days. In two patients, synovial fluid total tiflamizole concentrations were approximately one-third of simultaneous plasma concentrations, but elimination t 1/2s from synovial fluid were of the same order as those from plasma. Even with infrequent dosing, the longer t 1/2 may help sustain the anti-inflammatory effects of this drug.
D000328:Adult; D000368:Aged; D001172:Arthritis, Rheumatoid / Q000188:drug therapy / Q000378:metabolism*; D002792:Cholestyramine Resin / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D004347:Drug Interactions; D005243:Feces / Q000032:analysis; D005260:Female; D006207:Half-Life; D006801:Humans; D007093:Imidazoles / Q000009:adverse effects / Q000097:blood / Q000378:metabolism* / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D013582:Synovial Fluid / Q000032:analysis; D005466:Fluorocarbons
D002792:Cholestyramine Resin; D007093:Imidazoles; C041583:tiflamizole; D005466:Fluorocarbons