Amitriptyline metabolites in human urine. Identification of phenols, dihydrodiols, glycols, and ketones
Prox, A.; Breyer-Pfaff, U.
Drug Metabolism and Disposition the Biological Fate of Chemicals 15(6): 890-896
1987
ISSN/ISBN: 0090-9556 PMID: 2893718 Document Number: 292480
From the urine patients being treated with amtitriptyline, drug metabolites were extracted by adsorption to polystyrene. Nonconjugated compounds and agylcones liberated by enzymaic hydrolysis were purified separately by repeated TLC and characterized by physicochemical and chemical methods. Besides the known E- and Z-10-hydroxy derivatives of amitriptyline (AT), nortriptyline (NT), and their primary amine analogue, two isomeric 10,11-dihydroxy compounds could be identified in each series. Metabolites with an oxo function in position 10 occurred in minor quantities. The phenols 2-hydroxy-NT and 2,11-dihydroxy-NT, as well as the 1,2-dihydrodiol derived from NT, were regularly present, while the corresponding tertiary amines as well as 3-hydroxy-AT and -NT were detected occasionally in very small amounts.