Masimirembwa C M, Gustafsson L L, Dahl M L, Abdi Y A, Hasler J A
Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden.
Br J Clin Pharmacol. 1996 Apr;41(4):344-6. doi: 10.1046/j.1365-2125.1996.30713.x.
The effects of chloroquine (CHQ) on debrisoquine hydroxylase (CYP2D6) and S-mephenytoin hydroxylase (CYP2C19) were assessed in 11 black Zimbabwean and 12 white Swedish healthy volunteers. The activity of CYP2D6 was measured as the urinary debrisoquine to 4-hydroxydebrisoquine metabolic ratio and that of CYP2C19 as the urinary S- to R-mephenytoin enantiomer ratio (S/R). There were no statistically significant differences in either metabolic ratio as a result of prophylactic or loading doses of CHQ. This indicates that CHQ does not inhibit CYP2D6 or CYP2C19 in vivo and is unlikely to compromise the metabolism of substrates for these two enzymes. It is, therefore, also unlikely that residual CHQ in populations under study will interfere with phenotyping of either CYP2D6 or CYP2C19.
在11名津巴布韦黑人健康志愿者和12名瑞典白人健康志愿者中评估了氯喹（CHQ）对异喹胍羟化酶（CYP2D6）和S-美芬妥英羟化酶（CYP2C19）的影响。CYP2D6的活性以尿中异喹胍与4-羟基异喹胍的代谢比来衡量，CYP2C19的活性以尿中S-美芬妥英与R-美芬妥英对映体比（S/R）来衡量。预防性或负荷剂量的CHQ对两种代谢比均无统计学上的显著差异。这表明CHQ在体内不抑制CYP2D6或CYP2C19，并且不太可能损害这两种酶底物的代谢。因此，在研究人群中残留的CHQ也不太可能干扰CYP2D6或CYP2C19的表型分析。
