Pharmacokinetics of a Five-day Oral Dihydroartemisinin Monotherapy Regimen in Patients with Uncomplicated Falciparum Malaria
Pharmacokinetics of a Five-day Oral Dihydroartemisinin Monotherapy Regimen in Patients with Uncomplicated Falciparum Malaria
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DOI：
10.2133/dmpk.23.158
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发表时间：
2008-01-01
影响因子：
2.1
通讯作者：
Kesara Na-Bangchang
中科院分区：
文献类型：
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作者：
Diem Thuy Le Thi;Ngoc Hung Le;Kesara Na-Bangchang
在 10 名患有无并发症的恶性疟疾的越南成年患者中，研究了 5 天口服单一疗法中双氢青蒿素 (DHA) 的药代动力学。从第 0 天到第 4 天，患者接受总剂量为 900 mg DHA 的治疗，每日单次剂量为 300、300、100、100 和 100 mg。治疗前两天内 DHA 浓度没有差异。然而，疟疾急性期 DHA 的药代动力学与恢复期显着不同。与第一天获得的结果相比，治疗最后一天观察到半衰期 (T-1/2z) 缩短和浓度曲线下面积 (AUC(无穷大)) 值降低。观察到 T-1/2z 和 AUC（无穷大）的降低与药物清除率 (CL/F) 的增加一致。此外，第 4 天达到最大血浆 DHA 浓度 (T-max) 所需的时间比第 0 天短。 总之，这些研究结果表明，DHA 药代动力学的变化与疟疾患者在疾病急性期和恢复期之间的生理变化有关。
The pharmacokinetics of dihydroartemisinin (DHA) in a 5-day oral monotherapy regimen was investigated in ten adult Vietnamese patients with uncomplicated falciparum malaria. The patients were treated with a total dose of 900 mg DHA divided as single daily doses of 300, 300, 100, 100, and 100 mg from day 0 through day 4. There were no differences in the concentrations of DHA within the first two days of treatment. The pharmacokinetics of DHA in the acute phase, however, was significantly different from that in the convalescent phase of malaria. Reduced half-life (T-1/2z) and lower area under concentration curve (AUC(infinity)) values were observed on the final day of treatment in comparison to those obtained on the first day. These decreases in T-1/2z and AUC(infinity) were observed in concordance with increased drug clearance (CL/F). Furthermore, the time required to reach maximum plasma DHA concentration (T-max) on day 4 was shorter than that on day 0. Together, these findings suggest that the change in pharmacokinetics of DHA is related to the physiological change in malaria patients between the acute and convalescent phases of the disease.