DEFECTIVE N-OXIDATION OF SPARTEINE IN MAN - NEW PHARMACOGENETIC DEFECT

被引:609
作者
EICHELBAUM, M
SPANNBRUCKER, N
STEINCKE, B
DENGLER, HJ
机构
[1] Department of Medicine, University of Bonn, Bonn-Venusberg
关键词
autosomal recessive trait; defective metabolism; pharmacogenetic defect; sparteine; sparteine-N-oxidation;
D O I
10.1007/BF00562059
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Sparteine, an antiarrhythmic and oxytocic drug, is metabolised by N1-oxidation. The sparteine-N1-oxide rearranges with loss of water to 2- and 5-dehydrosparteine. 18 (i. e., 5%) out of 360 subjects were unable to metabolise the drug. These persons, who were designated as nonmetabolisers, excreted almost 100% of the administered dose in urine as unchanged drug. The defective metabolism of sparteine was found to have a genetic basis. Sparteine-N1-oxidation appears to be determined by two allelic genes at a single locus where nonmetabolisers are homozygous for an autosomal recessive gene. © 1979 Springer-Verlag.
引用
收藏
页码:183 / 187
页数:5
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