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Influence of the defective metabolism of sparteine on its pharmacokinetics

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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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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Key words

  • sparteine
  • pharmacogenetic defect
  • defective metabolism
  • pharmacokinetics
  • renal excretion