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阿奇霉素作为体内血液裂殖体杀灭剂对啮齿动物和人类疟原虫的活性。

Activity of azithromycin as a blood schizonticide against rodent and human plasmodia in vivo.

作者信息

Andersen S L, Ager A, McGreevy P, Schuster B G, Wesche D, Kuschner R, Ohrt C, Ellis W, Rossan R, Berman J

机构信息

Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, District of Columbia.

出版信息

Am J Trop Med Hyg. 1995 Feb;52(2):159-61. doi: 10.4269/ajtmh.1995.52.159.

Abstract

We compared the efficacy of azithromycin to the clinical antimalarial doxycycline in Plasmodium berghei-infected mice and in P. falciparum-infected Aotus monkeys. When mice were administered drug orally twice a day for three days, the minimum total dose of azithromycin that cured all mice was 768 mg/kg. Doxycycline at a dose of 1,536 mg/kg cured no mice. The efficacy of fast-acting blood schizonticides (quinine, halofantrine, artemisinin) against P. berghei was augmented by azithromycin. In monkey experiments in which there were two animals per experimental group, azithromycin (100 mg/kg/day for seven days) eliminated parasitemia; azithromycin (30 mg/kg/day) initially cleared 99.8-100% of the parasites with recrudescence in the one completely cleared case. Doxycycline (30 mg/kg/day) cleared 100% of the parasites with recrudescence in both cleared cases. Since azithromycin can be clinically administered at a somewhat higher daily dosage than doxycycline, the data suggest that it may be possible to replace drugs of the tetracycline class with azithromycin in combination with fast-acting blood schizonticides for the treatment of P. falciparum infection.

摘要

我们比较了阿奇霉素与临床抗疟药多西环素对感染伯氏疟原虫的小鼠和感染恶性疟原虫的夜猴的疗效。当小鼠每天口服给药两次,持续三天时,治愈所有小鼠的阿奇霉素最小总剂量为768毫克/千克。剂量为1536毫克/千克的多西环素未能治愈任何小鼠。阿奇霉素增强了速效血内裂殖体杀灭剂(奎宁、卤泛群、青蒿素)对伯氏疟原虫的疗效。在每个实验组有两只动物的猴子实验中,阿奇霉素(100毫克/千克/天,持续七天)消除了寄生虫血症;阿奇霉素(30毫克/千克/天)最初清除了99.8%-100%的寄生虫,在一例完全清除的病例中出现了复发。多西环素(30毫克/千克/天)在两例清除的病例中均清除了100%的寄生虫,但出现了复发。由于阿奇霉素在临床上的每日给药剂量可能比多西环素略高,这些数据表明,在治疗恶性疟原虫感染时,阿奇霉素与速效血内裂殖体杀灭剂联合使用有可能取代四环素类药物。

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