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Disposition and metabolism of carbon 14 labeled tiaramide hydro chloride in man



Disposition and metabolism of carbon 14 labeled tiaramide hydro chloride in man



Drug Metabolism & Disposition 10(3): 241-245



The disposition and metabolism of 14C-tiaramide HCl [an antiinflammatory and antihistaminic agent] was examined in 4 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 and 6.0 .+-. 1.5% in feces. The elimination was rapid with 83.9% of the radioactivity excreted in urine in the first 12 h. The unchanged tiaramide serum concentration curve showed monoexponential elimination with a half-life of 1.3 h. Peak serum levels of 1.6-2.2 .mu.g/ml were attained between 0.5-1.5 h after dosing. Tiaramide was extensively metabolized with < 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.

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Accession: 005170610

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