The disposition and metabolism of 14C-tiaramide . HCl in man.
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.
D000293:Adolescent; D000893:Anti-Inflammatory Agents / Q000097:blood / Q000378:metabolism* / Q000652:urine; D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D005243:Feces / Q000032:analysis; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D010879:Piperazines / Q000097:blood / Q000378:metabolism* / Q000652:urine
D000893:Anti-Inflammatory Agents; D052160:Benzothiazoles; D002250:Carbon Radioisotopes; D010879:Piperazines; C003468:tiaramide