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Influence of the defective metabolism of sparteine on its pharmacokinetics

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Summary

Sparteine is metabolized by N1-oxidation, which in some subjects is defective. The defect has a pronounced effect on the kinetics of the drug. In non-metabolisers elimination of sparteine proceeds entirely via renal excretion by a capacity-limited process, 99,9% of the dose being excreted as unchanged drug. In metabolisers the drug is mainly eliminated by metabolic degradation. Pronounced differences in β-phase half-life and total plasma clearance were observed between metabolisers (156 min; 535 ml · min−1) and nonmetabolisers (409 min; 180 ml · min−1).

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References

  1. Binnig, F.: Zur Chemie des Sparteins. Arzneim. Forsch. (Drug Res.)24, 752–753 (1974)

    Google Scholar 

  2. Dengler, H. J., Eichelbaum, M., Hengstmann, J., Wieber, J.: (1970) Pharmacokinetic studies in man with sparteine. Pharmacol. Clin.2, 189–195 (1970)

    Google Scholar 

  3. Eichelbaum, M., Spannbrucker, N., Steincke, Dengler, H. J.: Defective N-oxidation of sparteine in man: a new pharmacogenetic defect. Eur. J. Clin. Pharmacol.16, 183–187 (1979)

    Google Scholar 

  4. Loo, J. C. K., Riegelman, S.: Assessment of pharmacokinetic constants from postinfusion blood curves obtained after i. v. infusion. J. Pharm. Sci.59, 53 (1970)

    Google Scholar 

  5. Peters, L.: Renal tubular excretion of organic bases. Pharmacol. Rev.12, 1–35 (1960)

    Google Scholar 

  6. Rennick, P. R., Lyons, R. H., Hoobler, S. W., Nelighi, R.: Absorption and renal excretion of the tetraethylammonium ion. J. Pharmacol. Exp. Ther.148, 262–269 (1965)

    Google Scholar 

  7. Spannbrucker, N., Eichelbaum, M., Dengler, H. J.: Untersuchungen zum in vitro Metabolismus von Spartein. Arzneim. Forsch. (submitted for publication)

  8. Sperber, J.: The excretion of some organic bases and some phenols and phenol derivatives. Scand. J. Clin. Lab. Invest.1, 345–346 (1949)

    Google Scholar 

  9. Spiteller, M., Spiteller, G.: Structural elucidation of sparteine metabolites. In: Biological Oxidation of Nitrogen. Gorrod, J. (ed.), pp. 109–112. Amsterdam: Elsevier 1978

    Google Scholar 

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Eichelbaum, M., Spannbrucker, N. & Dengler, H.J. Influence of the defective metabolism of sparteine on its pharmacokinetics. Eur J Clin Pharmacol 16, 189–194 (1979). https://doi.org/10.1007/BF00562060

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  • DOI: https://doi.org/10.1007/BF00562060

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