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巧茶(Catha edulis)的使用对氯喹生物利用度、血浆水平及抗疟活性的影响。

Effect of Khat (Catha edulis) Use on the Bioavailability, Plasma Levels and Antimalarial Activity of Chloroquine.

作者信息

Issa Faiza H, Al-Habori Molhem, Chance Michael L

机构信息

Department of Biochemistry & Molecular Biology, Sana'a University, Sana'a, Yemen;

Department of Parasitology, Liverpool School of Tropical Medicine, Liverpool, UK.

出版信息

Sultan Qaboos Univ Med J. 2016 May;16(2):e182-8. doi: 10.18295/squmj.2016.16.02.008. Epub 2016 May 15.

DOI:10.18295/squmj.2016.16.02.008
PMID:27226909
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4868517/
Abstract

OBJECTIVES

This study aimed to evaluate the effect of khat (Catha edulis) on chloroquine (CQ) bioavailability in healthy Yemeni adults and its effect on CQ plasma levels and parasite clearance among malaria patients.

METHODS

This study took place between January and April 2007 in Bajil and Sana'a, Yemen. Two CQ doses (600 mg each) were given to 15 healthy males on separate occasions; the first dose was followed by a khat-chewing session (phase one) while controls abstained from khat-chewing for the second (phase two). Additionally, 103 patients with Plasmodium falciparum-induced malaria, including both regular khat chewers (n = 57) and non-khat chewers (n = 46), were treated with CQ (25 mg/kg) over three days. Pharmacokinetic parameters were analysed among both controls and malaria patients. Parasite clearance was also investigated for the latter group.

RESULTS

The mean area under the concentration-time curve (AUC) was 2,108.9 versus 2,797.4 ng/hour/mL, mean peak plasma concentration (Cmax) was 415.6 versus 508.7 ng/mL and mean time to reach Cmax was 3.8 versus 3.6 hours for controls in phase one versus phase two, respectively; both AUC and Cmax levels were significantly reduced by khat-chewing (P <0.050). For khat- versus non-khat-chewing malaria patients, mean plasma CQ concentrations were 266.4 ng/mL versus 427.5 ng/mL (P <0.001). Furthermore, CQ was effective in 71.7% and 75.4% of non-khat and khat-chewing malaria patients, respectively (P = 0.823).

CONCLUSION

Khat-chewing was found to significantly reduce plasma CQ levels among healthy volunteers and malaria patients. While receiving CQ treatment, patients should be advised not to chew khat.

摘要

目的

本研究旨在评估巧茶(Catha edulis)对健康也门成年人氯喹(CQ)生物利用度的影响,及其对疟疾患者氯喹血浆水平和寄生虫清除的影响。

方法

本研究于2007年1月至4月在也门的巴吉尔和萨那进行。分别在不同时间给15名健康男性服用两种氯喹剂量(各600毫克);第一次服药后进行嚼巧茶环节(第一阶段),而对照组在第二次服药时不嚼巧茶(第二阶段)。此外,103名由恶性疟原虫引起疟疾的患者,包括经常嚼巧茶者(n = 57)和不嚼巧茶者(n = 46),接受了为期三天的氯喹(25毫克/千克)治疗。分析了对照组和疟疾患者的药代动力学参数。还对后一组患者的寄生虫清除情况进行了研究。

结果

第一阶段与第二阶段对照组的平均血药浓度-时间曲线下面积(AUC)分别为2108.9与2797.4纳克/小时/毫升,平均血浆峰浓度(Cmax)分别为415.6与508.7纳克/毫升,平均达峰时间分别为3.8与3.6小时;嚼巧茶使AUC和Cmax水平均显著降低(P <0.050)。对于嚼巧茶与不嚼巧茶的疟疾患者,平均血浆氯喹浓度分别为266.4纳克/毫升与427.5纳克/毫升(P <0.001)。此外,氯喹分别在71.7%的不嚼巧茶疟疾患者和75.4%的嚼巧茶疟疾患者中有效(P = 0.823)。

结论

发现嚼巧茶会显著降低健康志愿者和疟疾患者的血浆氯喹水平。在接受氯喹治疗时,应建议患者不要嚼巧茶。

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