Springer Nature is making SARS-CoV-2 and COVID-19 research free. View research | View latest news | Sign up for updates

Metabolism of pheneturide in the rat and in man

  • 12 Accesses

  • 3 Citations


The biotransformation of pheneturide was studied in humans and in the rat. Human volunteers received a single oral dose of 10mg/kg of pheneturide and the rats were given repeated doses of 250 mg/kg. Urine from both study groups was extracted with Amberlite XAD-2 and the extracts were separated by preparative HPLC after enzymatic hydrolysis. Five metabolites were isolated in man and their structures were determined using NMR and mass spectrometry. The hydrolysis of the ureide function and the 4-hydroxylation of the benzene ring led to the formation of two major metabolites: 2-(4-hydroxyphenyl)-butyroylurea (37.5%) and 2-phenylbutyric acid (40.6%), and to one minor metabolite: 2-(4-hydroxyphenyl)-butyric acid (11.9%). Seven metabolites were isolated in the rat. The 4-hydroxylation of the benzene ring and the C 3 hydroxylation of the aliphatic chain led to the formation of two major metabolites: 2-(4-hydroxyphenyl)-butyroylurea (70.5%) and 3-hydroxy-2-phenyl-butyroylurea (19.6%), whereas the hydrolysis of the ureide function was less important. Only traces of the parent drug were found in humans as well as in the rat.

This is a preview of subscription content, log in to check access.


  1. 1.

    Vas C.J. and Parsonage M.J. (1967): Treatment of intractable temporal lobe epilepsy with pheneturide. Acta Neurol. Scand.,43, 580–586.

  2. 2.

    Schweingruber R. and Ketz E. (1960): The contribution of the acetylureas to the treatment of epilepsy. Schweiz. Med. Wochenschr.,90, 423–426.

  3. 3.

    Ketz E., Bernoulli C. und Gold-Aubert Ph. (1972): Erfahrungen mit Pheneturide bei therapierefraktären Epilepsien. Schweiz. Rundschau Med. (Praxis),61, 1146–1152.

  4. 4.

    Galeazzi R.L., Egli M. and Wad N. (1979): Pharmacokinetics of Phenylethylacetylurea (Pheneturide), an old anti-epileptic drug. J. of Pharm, and Biopharm.,7, 453–462.

  5. 5.

    Miamoto K, Seino M. and Ikeda Y. (1975): Consecutive determination of the levels of twelve anti-epileptic drugs in blood and cerebrospinal fluid.In: Schneider H., Janz D., Gardner-Thorpe C, Meinardi H. and Sherwin A.L.S. (Eds.) Clinical Pharmacology of Anti-Epileptic Drugs. Springer Verlag, New York, pp. 323–330.

  6. 6.

    Wad N., Rai P.V. und Egli M. (1979): Klinisch-chemische und klinisch-pharmakologische Aspekte von Mephytoin, Methsuximide, Monohydroxy-Carbazepine (GP 47779) und Pheneturide. Jahresbericht Schweiz. Epilepsie-Klinik, pp. 23–34.

  7. 7.

    Tschudi P. (1983): Pheneturide in der Epilepsie-Therapie: Klinische Wirksamkeit und therapeutische Serumkonzentration. Inaugural-Dissertation, Universität Zürich.

  8. 8.

    Glasson B., Lerch P. et Benakis A. (1960): Répartition et élimination du Pheneturide marqué. Thérapie XV, 368–376.

  9. 9.

    Vachta J. and Gold-Aubert Ph. (1982): Febarbamate: Metabolism in the rat. Eur. J. Drug. Metab. Pharmacokin.,7, 147–156.

  10. 10.

    Vachta J., Valter K. and Gold-Aubert Ph. (1983): Febarbamate: Metabolism in man. Eur. J. Drug. Metab. Pharmacokin.,8, 297–308.

  11. 11.

    Lockok R.A. and Couts R.T. (1970): The mass spectra of succinimides, hydantoins, oxazolidinediones and other medicinal anti-epileptic drugs. Org. Mass. Spectr.,3, 735–745.

Download references

Author information

Correspondence to J. Vachta.

Rights and permissions

Reprints and Permissions

About this article

Cite this article

Vachta, J., Valter, K. & Gold-Aubert, P. Metabolism of pheneturide in the rat and in man. European Journal of Drug Metabolism and Pharmacokinetics 11, 195–204 (1986). https://doi.org/10.1007/BF03189847

Download citation


  • Antiepileptics
  • pheneturide
  • metabolism
  • man
  • rat
  • structure determination