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Pharmacokinetics and metabolism of [3H]-pipethiaden in healthy volunteers

  • Z. Plecitá
  • M. Španěl
  • I. ULČ
  • V. Rejholec
  • R. Lapka
Article
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Summary

Six healthy volunteers participated in a single-dose study of pharmacokinetics and metabolism of oral administration of [3H]-pipethiaden (1 mg). Plasma levels of total radioactivity, urinary excretion and metabolism were analyzed by liquid scintillation counting and radio-TLC. The mean peak plasma concentration of radioactive metabolites was 4.9 ng eq/ml, and the mean elimination half life was 11.5 h. 34% of radioactivity was recovered in 4 days in urine, with only 0.4% present as unchanged drug. Pipethiaden was extensively metabolized by S-oxidation, N-demethylation, and N-oxidation.

Keywords

[3H]-Pipethiaden pharmacokinetics metabolism 

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References

  1. 1.
    Rajšner M., Metyš J., Protiva M. (1967): Neurotrope and Psychotrope Substanzen. XV. 4,9-Dihydrothieno [2,3-b] benzo[e]thiepin-Derivative. Collect Czech. Chem. Commun., 32, 2854–2866.Google Scholar
  2. 2.
    Metyš J., Metyšová J., Valchát M, Dlabac A. (1979): Pharmacological characteristics of several new antimigraine compounds. Cs. Fysiol., 28, 270–271.Google Scholar
  3. 3.
    Metyšová J., Metyš J. (1979): Comparative studies of new anti-migraine drugs. I. Action on central nervous system in rodents. Activ. Nerv. Sup. (Praha), 21, 174–175.Google Scholar
  4. 4.
    Lapka R., Franc Z., Šmolík S. (1985): Pharmacokinetics of [3H]-pipethiaden after single oral and intravenous administration in rats. Arzneimittelforsch., 35, 486–488.PubMedGoogle Scholar
  5. 5.
    Meier J., Schreier E. (1976): Human plasma levels of some anti-migraine drugs. Headache, 16, 96–104.CrossRefPubMedGoogle Scholar
  6. 6.
    Yamaoka K., Tanigawara Y., Nakagawa T., Uno T. (1981): A pharmacokinetic analysis program (MULTI) for microcomputer. J. Pharm. Dyn., 4, 879–885.Google Scholar
  7. 7.
    Yamaoka K., Nakagawa T., Uno T. (1978): Statistical moments in pharmacokinetics. J. Pharmacokinet. Biopharm., 6, 547–588.CrossRefPubMedGoogle Scholar
  8. 8.
    Metyš J., Dlohožková N., Soucek R., et al. (1989) Pharmacological properties of the metabolites of pipethiaden, a novel anti-migraine prophylactic agent. Cs. Fysiol., 38, 160.Google Scholar

Copyright information

© Springer-Verlag 1992

Authors and Affiliations

  • Z. Plecitá
    • 2
  • M. Španěl
    • 1
  • I. ULČ
    • 1
  • V. Rejholec
    • 2
  • R. Lapka
    • 2
  1. 1.Research Institute for Pharmacy and BiochemistryPlzeňCzechoslovakia
  2. 2.Research Institute for Pharmacy and BiochemistryPragueCzechoslovakia

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