INFLUENCE OF THE DEFECTIVE METABOLISM OF SPARTEINE ON ITS PHARMACOKINETICS

被引:56
作者
EICHELBAUM, M
SPANNBRUCKER, N
DENGLER, HJ
机构
[1] Department of Medicine, University of Bonn, Bonn-Venusberg
关键词
defective metabolism; pharmacogenetic defect; pharmacokinetics; renal excretion; sparteine;
D O I
10.1007/BF00562060
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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). © 1979 Springer-Verlag.
引用
收藏
页码:189 / 194
页数:6
相关论文
共 9 条
[1]  
BINNIG F, 1974, ARZNEIMITTEL-FORSCH, V24, P752
[2]  
DENGLER H J, 1970, Pharmacologia Clinica, V2, P189, DOI 10.1007/BF00404298
[3]   DEFECTIVE N-OXIDATION OF SPARTEINE IN MAN - NEW PHARMACOGENETIC DEFECT [J].
EICHELBAUM, M ;
SPANNBRUCKER, N ;
STEINCKE, B ;
DENGLER, HJ .
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1979, 16 (03) :183-187
[4]   ASSESSMENT OF PHARMACOKINETIC CONSTANTS FROM POSTINFUSION BLOOD CURVES OBTAINED AFTER IV INFUSION [J].
LOO, JCK ;
RIEGELMAN, S .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1970, 59 (01) :53-+
[5]  
PETERS L, 1960, PHARMACOL REV, V12, P1
[6]  
RENNICK BR, 1965, J PHARMACOL EXP THER, V148, P262
[7]  
SPANNBRUCKER N, UNPUBLISHED
[8]  
SPERBER I, 1949, SCAND J CLIN LAB INV, V1, P345
[9]  
SPITELLER M, 1978, BIOL OXIDATION NITRO, P109