Andersen S L, Ager A L, McGreevy P, Schuster B G, Ellis W, Berman J
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, DC 20307-5100.
Antimicrob Agents Chemother. 1994 Aug;38(8):1862-3. doi: 10.1128/AAC.38.8.1862.
The efficacy of the newly marketed azalide azithromycin was compared with that of the clinical agent doxycycline in a murine model of sporozoite-induced malaria. Drug was administered once; Plasmodium yoelii sporozoites were administered 2 h later; survival at day 60 was determined. For parenterally administered drug, 160 mg of azithromycin or doxycycline per kg of body weight was 100% effective; 40 mg of azithromycin per kg was 80% effective, but 40 mg of doxycycline per kg was 40% effective. Orally administered azithromycin was somewhat less effective than parenterally administered drug, consistent with the 37% clinical oral bioavailability of this agent. For orally administered azithromycin, 160 mg/kg was 100% effective and 40 mg/kg was 40% effective. The efficacy of azithromycin in comparison with that of doxycycline and the known prolonged levels of azithromycin in the livers of humans suggest that azithromycin has potential as a clinical causal prophylactic agent for malaria.
在子孢子诱导的疟疾小鼠模型中，将新上市的氮杂内酯类阿奇霉素的疗效与临床用药多西环素进行了比较。药物给药一次；2小时后接种约氏疟原虫子孢子；测定第60天的存活率。对于胃肠外给药，每千克体重160毫克的阿奇霉素或多西环素有效率为100%；每千克体重40毫克的阿奇霉素有效率为80%，但每千克体重40毫克的多西环素有效率为40%。口服阿奇霉素的疗效略低于胃肠外给药，这与该药物37%的临床口服生物利用度一致。对于口服阿奇霉素，每千克体重160毫克有效率为100%，每千克体重40毫克有效率为40%。与多西环素相比，阿奇霉素的疗效以及阿奇霉素在人体肝脏中已知的延长水平表明，阿奇霉素有潜力作为疟疾的临床病因预防药物。
