COMPARISON OF THE METABOLISM AND ELIMINATION OF PYRILAMINE MALEATE INTHE RAT, MOUSE AND FEMALE RHESUS-MONKEY

Elimination and metabolic profiles of the O-glucuronide conjugated pro ducts of pyrilamine and their nonconjugated O-dealkylated and N-desmet hyl pyrilamine products were determined after the oral administration of (C-14)-pyrilamine maleate to Fischer 344 rats, B(6)C(3)F1 mice and female rhesus monkeys by stomach tube or i.v. The total cumulative uri nary and fecal pyrilamine products were determined. The conjugated pyr ilamine metabolites, isolated and identified were the glucuronide prod ucts of O-dealkylated pyrilamine and ring-hydroxylated pyrilamine, and the nonconjugated metabolites were predominately the N-desmethylpyril amine and O-dealkylated pyrilamine and their ring-hydroxylated product s. Statistically significant differences were observed in the percenta ges of the conjugated and nonconjugated metabolites of pyrilamine excr eted by the three species studied.