Veenendaal J R, Parkinson A D, Kere N, Rieckmann K H, Edstein M D
Army Malaria Research Unit, Milpo, Ingleburn, Australia.
Eur J Clin Pharmacol. 1991;41(2):161-4. doi: 10.1007/BF00265910.
Halofantrine is a new blood schizontocidal drug used for the treatment of multidrug-resistant falciparum malaria. The pharmacokinetics of halofantrine (HAL) and its principal metabolite, N-desbutylhalofantrine (BHAL), was investigated in 6 adult male patients of Melanesian origin with uncomplicated falciparum malaria. The patients received 500 mg of halofantrine hydrochloride at times 0, 6 and 12 h (total 1.5 g). All patients responded to treatment with a mean parasite clearance time of 52.7 h and a mean fever clearance time of 33.8 h. The following kinetic parameters (mean values) were determined for HAL and BHAL, respectively: maximum plasma concentration (Cmax) = 896 and 491 ng.ml-1; time to reach the Cmax (tmax) = 15 and 56 h; elimination half-life (t1/2) = 91 and 79 h and the mean residence time (MRT) = 71 and 102 h. Based on the clinical response the plasma concentrations of HAL and BHAL were adequate for the treatment of uncomplicated falciparum malaria in the 6 patients.
卤泛群是一种新型的血液裂殖体杀灭药物，用于治疗耐多药恶性疟。在6名美拉尼西亚裔成年男性非复杂性恶性疟患者中研究了卤泛群（HAL）及其主要代谢产物N-去丁基卤泛群（BHAL）的药代动力学。患者在0、6和12小时分别接受500mg盐酸卤泛群（总计1.5g）。所有患者治疗有效，平均疟原虫清除时间为52.7小时，平均退热时间为33.8小时。分别测定了HAL和BHAL的以下动力学参数（平均值）：最大血浆浓度（Cmax）=896和491ng.ml-1；达到Cmax的时间（tmax）=15和56小时；消除半衰期（t1/2）=91和79小时，平均驻留时间（MRT）=71和102小时。基于临床反应，HAL和BHAL的血浆浓度足以治疗这6例患者的非复杂性恶性疟。
