Abstract
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.
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Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Basco L. K., Ramiliarisoa O., Le Bras J. In vitro activity of pyrimethamine, cycloguanil, and other antimalarial drugs against African isolates and clones of Plasmodium falciparum. Am J Trop Med Hyg. 1994 Feb;50(2):193–199. doi: 10.4269/ajtmh.1994.50.193. [DOI] [PubMed] [Google Scholar]
- Davidson D. E., Jr, Ager A. L., Brown J. L., Chapple F. E., Whitmire R. E., Rossan R. N. New tissue schizontocidal antimalarial drugs. Bull World Health Organ. 1981;59(3):463–479. [PMC free article] [PubMed] [Google Scholar]
- Kuschner R. A., Heppner D. G., Andersen S. L., Wellde B. T., Hall T., Schneider I., Ballou W. R., Foulds G., Sadoff J. C., Schuster B. Azithromycin prophylaxis against a chloroquine-resistant strain of Plasmodium falciparum. Lancet. 1994 Jun 4;343(8910):1396–1397. doi: 10.1016/s0140-6736(94)92526-7. [DOI] [PubMed] [Google Scholar]
- Schlesinger P. H., Krogstad D. J., Herwaldt B. L. Antimalarial agents: mechanisms of action. Antimicrob Agents Chemother. 1988 Jun;32(6):793–798. doi: 10.1128/aac.32.6.793. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Shmuklarsky M. J., Boudreau E. F., Pang L. W., Smith J. I., Schneider I., Fleckenstein L., Abdelrahim M. M., Canfield C. J., Schuster B. Failure of doxycycline as a causal prophylactic agent against Plasmodium falciparum malaria in healthy nonimmune volunteers. Ann Intern Med. 1994 Feb 15;120(4):294–299. doi: 10.7326/0003-4819-120-4-199402150-00006. [DOI] [PubMed] [Google Scholar]