PMID: 8583393Sep 1, 1995Paper

Rat tissue concentrations of chlorimipramine, chlorpromazine and their N-demethylated metabolites after a single oral dose of the parent compounds

The Journal of Pharmacy and Pharmacology
G SgaragliL Della Corte

Abstract

A single oral dose of 90 mg kg-1 chlorimipramine or chlorpromazine, corresponding to 54.5 or 55.9 mumol, respectively, was given to male Sprague-Dawley rats and concentrations of parent drugs and their N-desmethyl metabolites measured by gas chromatography in plasma and major organs (brain, liver, lung, kidney, heart, spleen and peritoneal fat). In the case of chlorimipramine, N-desmethyl metabolite levels were consistently higher than those of the parent drug for the entire observation period of 24 h in all tissues except fat, while lower N-desmethyl metabolite/parent compound ratios were observed for chlorpromazine. N-Desmethyl metabolite kinetics of chlorimipramine appeared to be elimination-rate limited, while those of chlorpromazine were formation-rate limited. In all analysed organs, the maximu detectable drug+metabolite concentrations accounted for only 2.3 and 4.6% of the initial dose of chlorimipramine and chlorpromazine. Chlorpromazine treatment gave rise to an area under the total amount-time curve (AUC0-24) for parent drug+metabolites, 3.9-fold that for chlorimipraine. Closer scrutiny discloses a conversion ratio of parent compound to N-desmethyl metabolite of 1.1 for chlorpromazine and of 2.2 for chlorimipramine, i...Continue Reading

References

Feb 1, 1977·Archives of General Psychiatry·S H Snyder, H I Yamamura
Dec 1, 1976·European Journal of Pharmacology·M Weinstock, D Cohen
Jul 1, 1977·Clinical Pharmacokinetics·L F Gram
Apr 1, 1979·The British Journal of Psychiatry : the Journal of Mental Science·L Della CorteA Pazzagli
Apr 1, 1978·British Journal of Pharmacology·K Shein, S E Smith
Aug 1, 1978·Computers and Biomedical Research, an International Journal·C Gomeni, R Gomeni
Apr 1, 1977·Clinical Pharmacology and Therapeutics·S G Dahl, R E Strandjord
Aug 1, 1977·The British Journal of Psychiatry : the Journal of Mental Science·O T PhillipsonA F Healey
Jul 1, 1990·Journal of Biochemistry·S Imaoka, Y Funae
Jan 1, 1990·Pharmacology & Therapeutics·D E Ryan, W Levin
Mar 1, 1970·The Journal of Pharmacy and Pharmacology·S H Curry
Mar 1, 1970·The Journal of Pharmacy and Pharmacology·I C Campbell, A Todrick
Jun 15, 1971·Life Sciences. Pt. 1: Physiology and Pharmacology·A A ManianS R Harris
Jan 1, 1971·Acta Pharmacologica Et Toxicologica·A Ryrfeldt, E Hansson
May 1, 1970·Proceedings of the Society for Experimental Biology and Medicine·S H CurryH M Maling
Jul 1, 1971·British Journal of Pharmacology·S H CurryG P Mould
Nov 16, 1965·Psychopharmacologia·C Kornetsky, G Bain
Jan 1, 1984·Annual Review of Pharmacology and Toxicology·L Rivera-Calimlim, L Hershey
Sep 1, 1980·Clinical and Experimental Pharmacology & Physiology·F A MendelsohnJ Csicsmann
Mar 1, 1980·Naunyn-Schmiedeberg's Archives of Pharmacology·R OrtmannA Delini-Stula
Jan 1, 1980·Progress in Neuro-psychopharmacology·L E EvansT Van Hees
Sep 1, 1980·Clinical and Experimental Pharmacology & Physiology·R F Moulds
Nov 1, 1963·Proceedings of the Society for Experimental Biology and Medicine·L G HART, J R FOUTS
Mar 1, 1980·Acta Psychiatrica Scandinavica·L MaîtreP C Waldmeier

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Citations

Sep 7, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·H WeigmannC Hiemke
Nov 12, 1998·The Journal of Pharmacy and Pharmacology·M ValotiG Sgaragli
Oct 7, 2008·Basic & Clinical Pharmacology & Toxicology·Jun-Sheng WangC Lindsay Devane
Jan 23, 2015·Frontiers in Behavioral Neuroscience·Georgia BalsevichMathias V Schmidt
Feb 12, 2008·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Melanie StruweUlla Plappert-Helbig
Jan 13, 2009·Academic Emergency Medicine : Official Journal of the Society for Academic Emergency Medicine·Martyn HarveyKerry Hoggett
Jan 3, 2021·International Journal of Antimicrobial Agents·Marion PlazeRaphaël Gaillard
Nov 3, 2020·Journal of Clinical Psychopharmacology·Ángel Ruiz de Pellón Santamaría
May 20, 2020·L'Encéphale·Marion PlazeRaphaël Gaillard
Nov 17, 1999·Journal of Pharmaceutical Sciences·S D YooK C Lee

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