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Comparison of the disposition and of the metabolic pattern of Reboxetine, a new antidepressant, in the rat, dog, monkey and man

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Summary

The purpose of this study was to compare the disposition and the metabolic pattern of Reboxetine in several species, including man.

[14C]-Reboxetine was given orally to the rat, the dog, the monkey (5 mg/kg) and man (2 and 4 mg/kg). Radioactivity was eliminated both by the renal and faecal route in the rat and the dog, mainly in urine in the monkey and man. Reboxetine was extensively metabolized. A number of urinary metabolites were quantified by radio-HPLC and tentatively identified by comparison with the retention times of reference compounds.

Suggested routes of metabolic transformation are: 2-O-dealkylation; hydroxylation of the ethoxyphenoxy ring; oxidation of the morpholine ring; morpholine ring-opening; and combinations of these. Metabolites were partially or completely conjugated with glucuronic acid and/or sulphuric acid.

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Authors and Affiliations

  1. Erbamont Group, R&D Pharmacokinetics and Metabolism, Farmitalia Carlo Erba, Via Imbonati 24, I-20159, Milan, Italy

    G. Cocchiara, R. Battaglia, P. Pevarello & M. Strolin Benedetti

Authors
  1. G. Cocchiara
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  2. R. Battaglia
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  3. P. Pevarello
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  4. M. Strolin Benedetti
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Cocchiara, G., Battaglia, R., Pevarello, P. et al. Comparison of the disposition and of the metabolic pattern of Reboxetine, a new antidepressant, in the rat, dog, monkey and man. European Journal of Drug Metabolism and Pharmacokinetics 16, 231–239 (1991). https://doi.org/10.1007/BF03189965

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  • DOI: https://doi.org/10.1007/BF03189965

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