Influence of CYP2C8 Polymorphism on the Exposure to Chloroquine in Patients with Malaria by Plasmodium vivax—A Preliminary Study

Abstract

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