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Metabolism of oxyfedrine

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Summary

Pharmacokinetic studies with orally administered 14C-oxyfedrine were carried out in rats and also in men.

  1. 1.

    In the rat tissue concentrations of oxyfedrine (determined by UV absorption) and 14C-radioactivity reached a maximum within 15 min. Recovery of oxyfedrine equaled that of 14C-activity (14C-oxyfedrine + 14C-labelled metabolites) in the heart and lung tissues, but differed somewhat in the liver and kidney extracts.

  2. 2.

    In experiments with bile fistula rats, 3 metabolites were recovered in the bile: a main metabolite, as an unlabeled, ninhydrin-positive substance (M1) besides two 14C-labeled minor metabolites*.

  3. 3.

    Approximately 40 to 50% of the oxyfedrine applied appeared in the urine as metabolites of oxyfedrine, mainly norephedrine, in rats and men.

  4. 4.

    The pharmacological significance of these findings is discussed.

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Authors and Affiliations

  1. Research Division of Cardiovascular Pharmacology Research Laboratories, Chugai Pharmaceutical Co., Tokyo, Japan

    K. Sakai & S. Sugano

  2. Research Division of Biochemistry Research Laboratories, Chugai Pharmaceutical Co., Tokyo, Japan

    I. Watanabe, M. Fukushima, S. Takanashi & Y. Nishii

Authors
  1. K. Sakai
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  2. S. Sugano
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  3. I. Watanabe
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  4. M. Fukushima
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  5. S. Takanashi
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  6. Y. Nishii
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Additional information

By chemical and pharmacodynamic tests M1 proved to be identical with norephedrine.

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Sakai, K., Sugano, S., Watanabe, I. et al. Metabolism of oxyfedrine. Naunyn-Schmiedeberg's Arch. Pharmacol. 275, 323–337 (1972). https://doi.org/10.1007/BF00500060

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  • DOI: https://doi.org/10.1007/BF00500060

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