TY - JOUR T1 - The disposition and metabolism of 14C-tiaramide . HCl in man. JF - Drug Metabolism and Disposition JO - Drug Metab Dispos SP - 241 LP - 245 VL - 10 IS - 3 AU - L J Klunk AU - P S Riska AU - D E Maynard Y1 - 1982/05/01 UR - http://dmd.aspetjournals.org/content/10/3/241.abstract N2 - The disposition and metabolism of 14C-tiaramide HCl was examined in four healthy male volunteers, after administration of a 200-mg dose in solution. The mean cumulative recovery of administered radioactivity was 91.3 +/- 2.9% (mean +/- SD) in urine an 6.0 +/- 1.5% in feces. The elimination was rapid, with 83.9% of the radioactivity extracted in urine in the first 12 hr. The unchanged tiaramide serum concentration curve showed monoexponential elimination with a half-life of 1.3 hr. Peak serum levels, of 1.6-2.2 micrograms/ml were attained between 0.5 and 1.5 hr after dosing. Tiaramide was extensively metabolized, with less than 1% excreted unchanged. Urinary metabolites (80-95% of the dose) were identified by mass-spectral comparison to authentic standards. Biotransformation resulted in production of the N-acetic acid N-oxide, N-acetic acid, O-glucuronide, N-oxide, and desethanol metabolites of tiaramide. ER -