Proguanil metabolism in relation to S-mephenytoin oxidation in a Turkish population

被引：14

作者：

Basci, NE ^{[1
]}

Bozkurt, A ^{[1
]}

Kortunay, S ^{[1
]}

Isimer, A ^{[1
]}

Sayal, A ^{[1
]}

Kayaalp, SO ^{[1
]}

机构：

[1] GULHANE MIL MED ACAD,DEPT PHARMACOL,ANKARA,TURKEY

来源：

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY | 1996年 / 42卷 / 06期

关键词：

proguanil; mephenytoin; oxidation polymorphisms; Turkish population;

D O I：

10.1046/j.1365-2125.1996.00500.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The oxidation of proguanil was studied in 89 unrelated healthy Turkish volunteers after administration of proguanil (single dose, 200 mg, orally). Based on the distribution of the ratio of proguanil to cycloguanil excreted in urine, and using an antimode value of 15, the prevalence of poor metabolizers in a Turkish population was estimated to be 5.6% (95% confidence interval 2.0%-17.3%) which was similar to that in the other Caucasian populations. The relationship between the oxidative capacities of CYP2C19 for the two substrates, proguanil and mephenytoin, was studied in 39 subjects (two poor and 37 extensive metabolizers of proguanil). The two poor metabolizers of proguanil were also identified as poor metabolizers of S-mephenytoin and no misclassification by the two phenotyping methods was observed. The correlation between the metabolic ratio of proguanil to cycloguanil and the S/R-mephenytoin ratio as assessed by Spearman's rank test, was statistically significant (r(s) = 0.50, P < 0.001).

引用

页码：771 / 773

页数：3

共 17 条

[1] IN-VITRO PROGUANIL ACTIVATION TO CYCLOGUANIL BY HUMAN LIVER-MICROSOMES IS MEDIATED BY CYP3A ISOFORMS AS WELL AS BY S-MEPHENYTOIN HYDROXYLASE [J].