在健康的赞比亚人CYP2D6 Halofantrine和氯喹抑制活动。

文章的细节

引用

复制到剪贴板

Simooya OO, Sijumbil G,林纳德女士,塔克GT

在健康的赞比亚人CYP2D6 Halofantrine和氯喹抑制活动。

Br中国新药杂志。1998年3月,45 (3):315 - 7。

PubMed ID

10896408 (在PubMed

]

文摘

目的:确定治疗剂量halofantrine加载的影响和氯喹对CYP2D6活动在健康黑色的赞比亚人。方法:20个健康的黑人男性赞比亚人是表现型CYP2D6活动通过测量debrisoquine / 4-hydroxydebrisoquine比在一个主/ h尿样10毫克剂量的口服后debrisoquine hemi-sulphate。受试者(所有的广泛的代谢表型对CYP2D6)随机分成两组,24 h后一组接受1500毫克盐酸halofantrine和另一组口头/剂量1500毫克磷酸氯喹。所有受试者进一步10毫克剂量的debrisoquine 2 h, 1周和2周后最后剂量的抗疟药物,和表型如上所述。结果:中位数debrisoquine / 4-hydroxydebrisoquine主/ h尿率增加了halofantrine(1.39到6.05;P < 0.01;95%置信区间4.00 - -11.7)和氯喹(1.96到3.91;P < 0.01;95%置信区间1.34 - -2.66)当debrisoquine被2 h后治疗。CYP2D6活动依然显著的减少这两种药物后1周。 Halofantrine was a significantly more potent inhibitor of CYP2D6 than chloroquine (P=0.037). Phenocopying occurred in two subjects taking halofantrine and one taking chloroquine (i.e. the debrisoquine/4-hydroxydebrisoquine ratios became consistent with the poor metabolizer phenotype). CONCLUSIONS: Given in therapeutic loading doses, both halofantrine and chloroquine caused significant inhibition of CYP2D6 activity in healthy black Zambians. With respect to halofantrine, this finding reinforces the recommendation that its combination with other drugs known to prolong the QT interval should be avoided, especially those that are metabolized significantly by CYP2D6.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
氯喹	细胞色素P450 2 d6	蛋白质	人类	未知的	底物 抑制剂	细节
Halofantrine	细胞色素P450 2 d6	蛋白质	人类	未知的	抑制剂	细节