Karbwang J, Bangchang K N, Bunnag D, Harinasuta T
Department of Clinical Tropical Medicine, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Bull World Health Organ. 1991;69(2):207-12.
A double-blind randomized comparative study of the pharmacokinetics and pharmacodynamics of a single oral dose of 750 mg or 1250 mg of mefloquine was carried out on 20 Thai male patients with acute uncomplicated falciparum malaria. In the 750-mg group, one patient exhibited an RII response, while the others responded to the treatment with a mean fever clearance time of 50.2 +/- 28.2 hours and a mean parasite clearance time of 70.2 +/- 17.3 hours. The main adverse effects were dizziness, nausea, vomiting, abdominal pain, and diarrhoea. Electrocardiogram monitoring detected sinus bradycardia in three patients and sinus arrhythmia in three others. In the 1250-mg group, one patient exhibited an RII response, while the others responded to the treatment with a mean fever clearance time of 43.4 +/- 36.6 hours and a mean parasite clearance time of 73.4 +/- 25.2 hours. However, during the follow-up period, two patients recrudesced on day 23 and on day 31 (RI response). Dizziness, nausea, vomiting, abdominal pain, and diarrhoea were the major adverse effects, with dizziness being more frequent compared with the 750-mg group. Sinus bradycardia occurred in four patients and sinus arrhythmia in four others. The pharmacokinetics of the two regimens were similar, with the absorption of mefloquine increasing linearly with the dose; however, vomiting within an hour of taking the drug reduced the whole blood mefloquine concentrations. The results do not indicate that there is any advantage in using a single dose of 1250 mg of mefloquine rather than 750 mg.
对20名患有急性非复杂性恶性疟的泰国男性患者进行了一项双盲随机对照研究，比较单次口服750毫克或1250毫克甲氟喹的药代动力学和药效学。在750毫克组中，1名患者出现RII反应，其他患者对治疗有反应，平均退热时间为50.2±28.2小时，平均寄生虫清除时间为70.2±17.3小时。主要不良反应为头晕、恶心、呕吐、腹痛和腹泻。心电图监测发现3例患者出现窦性心动过缓，另外3例出现窦性心律失常。在1250毫克组中，1名患者出现RII反应，其他患者对治疗有反应，平均退热时间为43.4±36.6小时，平均寄生虫清除时间为73.4±25.2小时。然而，在随访期间，2例患者分别在第23天和第31天复发（RI反应）。头晕、恶心、呕吐、腹痛和腹泻是主要不良反应，与750毫克组相比，头晕更为常见。4例患者出现窦性心动过缓，另外4例出现窦性心律失常。两种治疗方案的药代动力学相似，甲氟喹的吸收随剂量呈线性增加；然而，服药后1小时内呕吐会降低甲氟喹全血浓度。结果并未表明使用1250毫克单剂量甲氟喹比750毫克有任何优势。
