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卤泛群在肯尼亚非重症和重症疟疾儿童中的药代动力学

Halofantrine pharmacokinetics in Kenyan children with non-severe and severe malaria.

作者信息

Watkins W M, Winstanley P A, Mberu E K, Kokwaro G, Murphy S A, Newton C J, Mwangi I, Forster D, Marsh K

机构信息

Kenya Medical Research Institute, CRC. Kilifi Research Unit.

出版信息

Br J Clin Pharmacol. 1995 Mar;39(3):283-7. doi: 10.1111/j.1365-2125.1995.tb04450.x.

DOI:10.1111/j.1365-2125.1995.tb04450.x
PMID:7619670
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1365005/
Abstract
  1. Kenyan children with uncomplicated malaria given oral halofantrine (HF; non-micronised suspension; 8 mg base kg-1 body weight 6 hourly for three doses) showed wide variation in the disposition of HF and desbutylhalofantrine (HFm). 2. Eight Kenyan children with severe (prostrate) falciparum malaria who were receiving intravenous quinine, were given the same HF regimen by nasogastric tube. One patient had undetectable HF and two had undetectable HFm at all times after drug administration. 3. The mean AUC(0,24 h) of HF in prostrate children was half (7.54 compared with 13.10 micrograms ml-1 h) (P = 0.06), and that for HFm one-third (0.84 compared with 2.51 micrograms ml-1 h) (P < 0.05) of the value in children with uncomplicated malaria. 4. Oral HF may be appropriate for some cases of uncomplicated falciparum malaria in Africa, but in patients with severe malaria, the bioavailability of HF and HFm may be inadequate.
摘要
  1. 给患有非复杂性疟疾的肯尼亚儿童口服卤泛群(HF;非微粉化混悬液;8毫克碱基/千克体重,每6小时一次,共三剂),结果显示HF和去丁基卤泛群(HFm)的处置存在很大差异。2. 八名患有严重(极度虚弱)恶性疟原虫疟疾且正在接受静脉注射奎宁治疗的肯尼亚儿童,通过鼻胃管给予相同的HF治疗方案。一名患者在给药后的所有时间内HF均检测不到,两名患者的HFm始终检测不到。3. 极度虚弱儿童中HF的平均AUC(0,24 h) 为非复杂性疟疾儿童的一半(分别为7.54与13.10微克·毫升⁻¹·小时)(P = 0.06),HFm的平均AUC(0,24 h) 为非复杂性疟疾儿童的三分之一(分别为0.84与2.51微克·毫升⁻¹·小时)(P < 0.05)。4. 口服HF可能适用于非洲一些非复杂性恶性疟原虫疟疾病例,但对于重症疟疾患者,HF和HFm的生物利用度可能不足。

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Efficacy of multiple-dose halofantrine in treatment of chloroquine-resistant falciparum malaria in children in Kenya.
Lancet. 1988 Jul 30;2(8605):247-50. doi: 10.1016/s0140-6736(88)92538-x.
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Pharmacokinetics of halofantrine in man: effects of food and dose size.卤泛群在人体中的药代动力学:食物和剂量大小的影响。
Br J Clin Pharmacol. 1989 Jul;28(1):71-7. doi: 10.1111/j.1365-2125.1989.tb03507.x.