Tiflamizole elimination from plasma in rheumatoid arthritis

Clin Pharmacol Ther. 1984 Jul;36(1):92-8. doi: 10.1038/clpt.1984.145.

Abstract

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.

Publication types

  • Case Reports
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Aged
  • Arthritis, Rheumatoid / drug therapy
  • Arthritis, Rheumatoid / metabolism*
  • Cholestyramine Resin / pharmacology
  • Chromatography, High Pressure Liquid
  • Drug Interactions
  • Feces / analysis
  • Female
  • Half-Life
  • Humans
  • Imidazoles / adverse effects
  • Imidazoles / blood
  • Imidazoles / metabolism*
  • Imidazoles / therapeutic use
  • Male
  • Middle Aged
  • Synovial Fluid / analysis

Substances

  • Imidazoles
  • Cholestyramine Resin
  • tiflamizole