Karbwang J, Looareesuwan S, Phillips R E, Wattanagoon Y, Molyneux M E, Nagachinta B, Back D J, Warrell D A
Br J Clin Pharmacol. 1987 Apr;23(4):477-81. doi: 10.1111/j.1365-2125.1987.tb03079.x.
Mefloquine-sulphadoxine-pyrimethamine (MSP) in combination has proved effective against multiple-drug-resistant falciparum malaria, but nothing is known about mefloquine absorption when it is given in this formulation. Nine Thai patients, aged 15-51 years with uncomplicated chloroquine-resistant falciparum malaria, took 11.2-16.7 mg of mefloquine base per kilogram bodyweight as MSP tablets. All patients responded to treatment with fever and parasite clearance times of 61 +/- 29 h (mean +/- s.d.) and 52 +/- 24 h, respectively. The mean apparent absorption half-time (t1/2abs) of mefloquine was 4.89 h (range 2.25-9.72) and mean peak plasma concentration was 1815 ng ml-1 (range 725-3368). Peak plasma mefloquine concentrations in three patients who vomited within 2 h of treatment were 725, 956 and 1972 ng ml-1. There was no significant difference between plasma and whole blood mefloquine concentrations during the first 48 h of treatment. Based on the elimination of parasitaemia, the plasma mefloquine concentrations are adequate for therapy of uncomplicated falciparum malaria although the relationship between plasma concentrations and therapeutic efficacy of mefloquine requires further study.
甲氟喹-磺胺多辛-乙胺嘧啶(MSP)联合用药已被证明对多重耐药性恶性疟有效,但对于以该配方给药时甲氟喹的吸收情况却一无所知。9名年龄在15至51岁之间、患有非复杂性氯喹耐药性恶性疟的泰国患者,按每公斤体重服用11.2至16.7毫克甲氟喹碱的MSP片剂。所有患者对治疗均有反应,发热和寄生虫清除时间分别为61±29小时(平均值±标准差)和52±24小时。甲氟喹的平均表观吸收半衰期(t1/2abs)为4.89小时(范围为2.25至9.72),平均血浆峰值浓度为1815纳克/毫升(范围为725至3368)。在治疗后2小时内呕吐的3名患者的血浆甲氟喹峰值浓度分别为725、956和1972纳克/毫升。在治疗的前48小时内,血浆和全血中甲氟喹浓度之间没有显著差异。基于疟原虫血症的消除情况,尽管血浆浓度与甲氟喹治疗效果之间的关系需要进一步研究,但血浆中甲氟喹浓度对于非复杂性恶性疟的治疗是足够的。