title: Metabolism of doxylamine succinate in Fischer 344 rats. Part III: Conjugated urinary and fecal metabolites.
abstract: Elimination and metabolic profiles of the glucuronide products of doxylamine and its N-demethylated metabolites were determined after the oral administration of (14C)-doxylamine succinate (13.3 and 133 mg/kg doses) to male and female Fischer 344 rats. The cumulative urinary and fecal eliminations of these conjugated doxylamine metabolites at the 13.3 mg/kg dose were 44.4 +/- 4.2% and 47.3 +/- 8.1% of the total recovered dose for male and female rats, respectively. The cumulative urinary and fecal eliminations of conjugated doxylamine metabolites at the 133 mg/kg dose were 55.2 +/- 2.6% and 47.9 +/- 2.5% of the total recovered dose for male and female rats, respectively. The conjugated doxylamine metabolites that were isolated, quantitated, and identified are doxylamine O-glucuronide, N-desmethyl-doxylamine O-glucuronide, and N,N-didesmethyldoxylamine O-glucuronide.
authors.affiliation: Food and Drug Administration, National Center for Toxicological Research, Jefferson, Arkansas 72079.
authors.forename: C L
authors.initials: CL
authors.lastname: Holder
authors.forename: P H
authors.initials: PH
authors.lastname: Siitonen
authors.forename: W
authors.initials: W
authors.lastname: Slikker
authors.forename: C J
authors.initials: CJ
authors.lastname: Branscomb
authors.forename: W A
authors.initials: WA
authors.lastname: Korfmacher
authors.forename: H C
authors.initials: HC
authors.lastname: Thompson
authors.forename: C E
authors.initials: CE
authors.lastname: Cerniglia
authors.forename: A B
authors.initials: AB
authors.lastname: Gosnell
authors.forename: J O
authors.initials: JO
authors.lastname: Lay
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004319:Doxylamine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000378:metabolism* / Q000652:urine; D005243:Feces / Q000032:analysis*; D005260:Female; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000378:metabolism* / Q000652:urine; D008297:Male; D013058:Mass Spectrometry / Q000379:methods; D015394:Molecular Structure; D011725:Pyridines / Q000378:metabolism*; D051381:Rats; D011916:Rats, Inbred F344; D012737:Sex Factors
chemical_list: D006634:Histamine H1 Antagonists; D011725:Pyridines; D004319:Doxylamine; C035385:doxylamine succinate