title: Dose-dependent pharmacokinetics of metabolites of dipyrone in saliva.
abstract: Metabolites of dipyrone have been determined in the saliva of 18 volunteers following the oral intake of 0.5 g, 1.0 g, 1.5 g, 2.0 g and 2.5 g dipyrone. High concentrations were measured for N-methyl-aminoantipyrine (MAA), the other analgetic active metabolite, 4-aminoantipyrine was found in minor quantities only. N-formyl-antipyrine was not present in the saliva of some volunteers after low doses but could be determined following the intake of doses from 1.5 g - 2.5 g in saliva of all volunteers. N-acetyl-antipyrine appears late in saliva, acetylation rates varied greatly interindividually. Concentrations of the metabolites in saliva mimic the respective non-protein bound fraction in plasma found by other authors.
authors.affiliation: Institut für Pharmazeutische Chemie der Westfälischen Wilhelms-Universität Münster, Federal Republic of Germany.
authors.forename: E
authors.initials: E
authors.lastname: Neddermann
authors.forename: P
authors.initials: P
authors.lastname: Rohdewald
mesh_terms: D000328:Adult; D000632:Aminopyrine / Q000031:analogs & derivatives*; D000675:Ampyrone / Q000031:analogs & derivatives / Q000378:metabolism; D001711:Biotransformation; D002855:Chromatography, Thin Layer; D004177:Dipyrone / Q000031:analogs & derivatives / Q000378:metabolism / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D047069:Pyrazolones; D011721:Pyrenes / Q000378:metabolism; D012463:Saliva / Q000378:metabolism*
chemical_list: D047069:Pyrazolones; D011721:Pyrenes; D000632:Aminopyrine; D000675:Ampyrone; C049354:N-formyl-1-aminopyrene; D004177:Dipyrone; C010403:N-acetylaminoantipyrine; C008667:noramidopyrine