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Influence of the defective metabolism of sparteine on its pharmacokinetics.

作者信息

Eichelbaum M, Spannbrucker N, Dengler H J

出版信息

Eur J Clin Pharmacol. 1979 Sep;16(3):189-94. doi: 10.1007/BF00562060.

DOI:10.1007/BF00562060
PMID:499319
Abstract

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 nonmetabolisers 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 beta-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).

摘要

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Addressing phenoconversion: the Achilles' heel of personalized medicine.
应对表型转换:个性化医疗的致命弱点。
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Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I.人类细胞色素P450 2D6的多态性及其临床意义:第一部分。
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Insights into drug metabolism by cytochromes P450 from modelling studies of CYP2D6-drug interactions.通过CYP2D6-药物相互作用的建模研究深入了解细胞色素P450介导的药物代谢
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Eur J Clin Pharmacol. 2003 Jun;59(2):111-6. doi: 10.1007/s00228-003-0595-1. Epub 2003 May 1.
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[The chemistry of sparteins].
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