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1
Plasma and whole blood mefloquine concentrations during treatment of chloroquine-resistant falciparum malaria with the combination mefloquine-sulphadoxine-pyrimethamine.用甲氟喹-磺胺多辛-乙胺嘧啶联合治疗耐氯喹恶性疟期间的血浆和全血中甲氟喹浓度
Br J Clin Pharmacol. 1987 Apr;23(4):477-81. doi: 10.1111/j.1365-2125.1987.tb03079.x.
2
Comparison of the susceptibility of falciparum malaria to mefloquine-sulphadoxine-pyrimethamine and chloroquine in Nigeria.尼日利亚恶性疟原虫对甲氟喹-磺胺多辛-乙胺嘧啶和氯喹敏感性的比较。
Afr J Med Med Sci. 1988 Dec;17(4):195-200.
3
Sensitivity of Plasmodium falciparum to mefloquine-sulphadoxine-pyrimethamine (Fansimef) in vivo and to mefloquine alone in vitro in Nigeria.尼日利亚恶性疟原虫对甲氟喹-磺胺多辛-乙胺嘧啶(Fansimef)的体内敏感性以及对单独甲氟喹的体外敏感性。
Ann Trop Med Parasitol. 1988 Aug;82(4):325-30. doi: 10.1080/00034983.1988.11812253.
4
Double-blind dose finding study of mefloquine-sulfadoxine-pyrimethamine in children with acute falciparum malaria.甲氟喹-磺胺多辛-乙胺嘧啶治疗儿童急性恶性疟的双盲剂量探索研究。
Trans R Soc Trop Med Hyg. 1988;82(4):538-40. doi: 10.1016/0035-9203(88)90496-8.
5
Trials of mefloquine in vivax and of mefloquine plus 'fansidar' in falciparum malaria.氯喹用于间日疟以及氯喹加“Fansidar”用于恶性疟的试验。
Lancet. 1985 Apr 20;1(8434):885-8. doi: 10.1016/s0140-6736(85)91670-8.
6
[A case of malaria tropicameningoencephalitis (neuromalaria) with chloroquine and pyrimethamine/sulfadoxine resistance].1例对氯喹及乙胺嘧啶/磺胺多辛耐药的热带型脑型疟疾(神经型疟疾)
Nervenarzt. 1985 Feb;56(2):101-5.
7
The effect of mefloquine-sulfadoxine-pyrimethamine vs quinine on patients with complicated falciparum malaria.甲氟喹-磺胺多辛-乙胺嘧啶与奎宁对复杂型恶性疟患者的疗效比较
Southeast Asian J Trop Med Public Health. 1987 Jun;18(2):223-5.
8
Sequential treatment with quinine and mefloquine or quinine and pyrimethamine-sulfadoxine for falciparum malaria.采用奎宁与甲氟喹或奎宁与乙胺嘧啶-磺胺多辛序贯治疗恶性疟。
Br Med J. 1977 Jun 25;1(6077):1626-8. doi: 10.1136/bmj.1.6077.1626.
9
Randomized comparison of chloroquine plus sulfadoxine-pyrimethamine versus artesunate plus mefloquine versus artemether-lumefantrine in the treatment of uncomplicated falciparum malaria in the Lao People's Democratic Republic.在老挝人民民主共和国,氯喹加周效磺胺-乙胺嘧啶与青蒿琥酯加甲氟喹以及蒿甲醚-本芴醇治疗非复杂性恶性疟的随机对照研究
Clin Infect Dis. 2004 Oct 15;39(8):1139-47. doi: 10.1086/424512. Epub 2004 Sep 27.
10
RII and RIII type resistance of Plasmodium falciparum to combination of mefloquine and sulfadoxine/pyrimethamine in Indonesia.印度尼西亚恶性疟原虫对甲氟喹和磺胺多辛/乙胺嘧啶联合用药的RII型和RIII型抗性
Lancet. 1985 Nov 9;2(8463):1039-40. doi: 10.1016/s0140-6736(85)90908-0.

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Revisiting the Effect of Pharmaceuticals on Transmission Stage Formation in the Malaria Parasite .重新探讨药物对疟原虫传播阶段形成的影响。
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Patient age does not affect mefloquine concentrations in erythrocytes and plasma during the acute phase of falciparum malaria.患者年龄并不影响恶性疟原虫疟疾急性期红细胞和血浆中的甲氟喹浓度。
Braz J Infect Dis. 2016 Sep-Oct;20(5):482-6. doi: 10.1016/j.bjid.2016.07.005. Epub 2016 Aug 16.
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Pharmacokinetic interactions between artesunate-mefloquine and ritonavir-boosted lopinavir in healthy Thai adults.青蒿琥酯-甲氟喹与利托那韦增强型洛匹那韦在泰国健康成年人中的药代动力学相互作用。
Malar J. 2015 Oct 9;14:400. doi: 10.1186/s12936-015-0916-8.
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Interspecies allometric scaling of antimalarial drugs and potential application to pediatric dosing.抗疟药物的种间异速生长标度及其在儿科给药中的潜在应用。
Antimicrob Agents Chemother. 2014 Oct;58(10):6068-78. doi: 10.1128/AAC.02538-14. Epub 2014 Aug 4.
5
Distribution of mefloquine in the blood of Thai patients with acute uncomplicated falciparum malaria following administration of therapeutic doses of artesunate.青蒿琥酯治疗剂量给药后泰国无并发症恶性疟患者血液中的甲氟喹分布。
Eur J Clin Pharmacol. 2011 Jul;67(7):687-91. doi: 10.1007/s00228-011-1058-8. Epub 2011 May 10.
6
Mefloquine treatment of acute falciparum malaria: a prospective study of non-serious adverse effects in 3673 patients.甲氟喹治疗急性恶性疟:3673例患者非严重不良反应的前瞻性研究。
Bull World Health Organ. 1995;73(5):631-42.
7
Mefloquine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy.甲氟喹:其抗疟活性、药代动力学特性及治疗效果综述
Drugs. 1993 Mar;45(3):430-75. doi: 10.2165/00003495-199345030-00009.
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Divided-dose kinetics of mefloquine in man.甲氟喹在人体中的分次给药动力学。
Br J Clin Pharmacol. 1989 Aug;28(2):179-84. doi: 10.1111/j.1365-2125.1989.tb05413.x.
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The disposition of amodiaquine in Zambians and Nigerians with malaria.阿莫地喹在赞比亚和尼日利亚疟疾患者中的处置情况。
Br J Clin Pharmacol. 1990 Jun;29(6):695-701. doi: 10.1111/j.1365-2125.1990.tb03690.x.
10
Clinical pharmacokinetics of mefloquine.甲氟喹的临床药代动力学
Clin Pharmacokinet. 1990 Oct;19(4):264-79. doi: 10.2165/00003088-199019040-00002.

本文引用的文献

1
Recent advances in malaria with special reference to Southeast Asia.疟疾的最新进展,特别提及东南亚地区
Southeast Asian J Trop Med Public Health. 1982 Mar;13(1):1-34.
2
Single dose kinetics of mefloquine in man. Plasma levels of the unchanged drug and of one of its metabolites.甲氟喹在人体中的单剂量动力学。原形药物及其一种代谢物的血浆水平。
Chemotherapy. 1982;28(1):70-84. doi: 10.1159/000238062.
3
On the mechanism for the red-cell accumulation of mefloquine, an antimalarial drug.
Biochim Biophys Acta. 1984 Mar 23;803(3):174-81. doi: 10.1016/0167-4889(84)90007-7.
4
A phase II clinical trial of mefloquine in patients with chloroquine-resistant falciparum malaria in Thailand.甲氟喹在泰国耐氯喹恶性疟患者中的II期临床试验。
Bull World Health Organ. 1983;61(2):299-305.
5
Possible role of drug malabsorption in recrudescence of falciparum malaria.药物吸收不良在恶性疟复发中的可能作用。
Lancet. 1982 Nov 20;2(8308):1157-8. doi: 10.1016/s0140-6736(82)92807-0.
6
Intragastric mefloquine is absorbed rapidly in patients with cerebral malaria.脑型疟患者胃内的甲氟喹吸收迅速。
Am J Trop Med Hyg. 1985 Nov;34(6):1028-36. doi: 10.4269/ajtmh.1985.34.1028.
7
The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.甲氟喹在人体内的药代动力学:甲氟喹对安替比林代谢无影响。
Br J Clin Pharmacol. 1985 Nov;20(5):469-74. doi: 10.1111/j.1365-2125.1985.tb05099.x.
8
Treatment of falciparum malaria with quinne and tetracycline or combined mefloquine/sulfadoxine/pyrimethamine on the Thai-Kampuchean border.
Am J Trop Med Hyg. 1986 Mar;35(2):246-50. doi: 10.4269/ajtmh.1986.35.246.
9
Severe cutaneous reactions among American travelers using pyrimethamine-sulfadoxine (Fansidar) for malaria prophylaxis.使用乙胺嘧啶-磺胺多辛(Fansidar)预防疟疾的美国旅行者中出现的严重皮肤反应。
Am J Trop Med Hyg. 1986 May;35(3):451-8. doi: 10.4269/ajtmh.1986.35.451.
10
Trials of mefloquine in vivax and of mefloquine plus 'fansidar' in falciparum malaria.氯喹用于间日疟以及氯喹加“Fansidar”用于恶性疟的试验。
Lancet. 1985 Apr 20;1(8434):885-8. doi: 10.1016/s0140-6736(85)91670-8.

用甲氟喹-磺胺多辛-乙胺嘧啶联合治疗耐氯喹恶性疟期间的血浆和全血中甲氟喹浓度

Plasma and whole blood mefloquine concentrations during treatment of chloroquine-resistant falciparum malaria with the combination mefloquine-sulphadoxine-pyrimethamine.

作者信息

Karbwang J, Looareesuwan S, Phillips R E, Wattanagoon Y, Molyneux M E, Nagachinta B, Back D J, Warrell D A

出版信息

Br J Clin Pharmacol. 1987 Apr;23(4):477-81. doi: 10.1111/j.1365-2125.1987.tb03079.x.

DOI:10.1111/j.1365-2125.1987.tb03079.x
PMID:3555581
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1386099/
Abstract

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.

摘要

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。