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Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions.细胞色素 P450 2C8 在药物代谢和相互作用中的作用。
Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411.
6
An HPLC method with diode array detector for the simultaneous quantification of chloroquine and desethylchloroquine in plasma and whole blood samples from Plasmodium vivax patients in Vietnam, using quinine as an internal standard.一种采用二极管阵列检测器的高效液相色谱法,以奎宁为内标,同时定量检测越南间日疟患者血浆和全血样本中的氯喹和去乙基氯喹。
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7
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8
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CYP2C8基因多态性对疟疾患者氯喹暴露量的影响——一项初步研究

Influence of CYP2C8 Polymorphism on the Exposure to Chloroquine in Patients with Malaria by -A Preliminary Study.

作者信息

Pereira de Sena Luann Wendel, Fuzii Hellen Thais, Villanova Fabiola Elizabeth, Nunes Cardoso Mello Amanda Gabryelle, de Sena Maria Pantoja Moreira, Dias Ferreira Michelle Valéria, Fernandes Vieira José Luiz

机构信息

College of Collective Health, Federal University of the South and Southeast of Para, Cidade Universitaria, Avenida dos Ipês s/n, Maraba 68500000, Para, Brazil.

Tropical Medicine Center, Para Federal University, Generalissimo Deodoro Street 92, Belem 66074740, Para, Brazil.

出版信息

Int J Environ Res Public Health. 2025 Feb 25;22(3):336. doi: 10.3390/ijerph22030336.

DOI:10.3390/ijerph22030336
PMID:40238288
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11941787/
Abstract

AIM

To assess the impact of the CYP2C82 polymorphism on chloroquine and desethylchloroquine concentrations in patients with malaria caused by .

METHODS

A prospective study was conducted on patients with malaria in an endemic area of the Amazon basin. Liquid chromatography was employed to measure the levels of chloroquine and desethylchloroquine, while molecular methods estimated the frequency of the CYP2C82 variant.

RESULTS

This study revealed that plasma levels of chloroquine were higher in patients with the CYP2C82 polymorphism compared to those without this variant. The difference in plasma levels ranged from 5% to 26.5%. Conversely, patients with the CYP2C82 polymorphism exhibited lower levels of desethylchloroquine.

CONCLUSION

The findings of this study confirm the impairment of chloroquine metabolism by the CYP2C82 variant. However, it is noteworthy that in the dose regimen used for malaria treatment, these changes did not lead to toxic concentrations of the drug.

摘要

目的

评估CYP2C82基因多态性对由……引起的疟疾患者体内氯喹和去乙基氯喹浓度的影响。

方法

在亚马逊流域的一个疟疾流行地区对疟疾患者进行了一项前瞻性研究。采用液相色谱法测量氯喹和去乙基氯喹的水平,同时用分子方法估计CYP2C82变体的频率。

结果

本研究表明,与没有该变体的患者相比,具有CYP2C82基因多态性的患者血浆中氯喹水平更高。血浆水平差异在5%至26.5%之间。相反,具有CYP2C82基因多态性的患者去乙基氯喹水平较低。

结论

本研究结果证实CYP2C82变体损害了氯喹代谢。然而,值得注意的是,在用于疟疾治疗的剂量方案中,这些变化并未导致药物的毒性浓度。