Abstract
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.
DMD articles become freely available 12 months after publication, and remain freely available for 5 years.Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page.
|