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阿维菌素类药物抗丝虫寄生虫的疗效:简要综述。

Efficacy of the avermectins against filarial parasites: a short review.

作者信息

Campbell W C

出版信息

Vet Res Commun. 1982 May;5(3):251-62. doi: 10.1007/BF02214991.

DOI:10.1007/BF02214991
PMID:7051527
Abstract

The avermectins are macrocyclic lactones produced by Streptomyces avermitilis. One of them has been chemically modified and given the non-proprietary name ivermectin. The compounds have shown efficacy against various stages of filarial parasites. With respect to pre-adult stages in the mammalian host, activity has been observed against Dirofilaria immitis in ferrets and dogs, and Dipetalonema viteae and Litomosoides carinii in jirds (Meriones); but activity has not been observed against the developing stages of Brugia spp. in jirds or Onchocerca spp. in cattle. The compounds have not shown activity against adult filarial worms, except in the case of Setaria equina in horses and possibly Dipetalonema viteae in jirds. With respect to the first state larva (microfilaria) in the mammalian host, efficacy has been observed against Dirofilaria immitis in dogs, Brugia malayi in multimammate rats (Mastomys), Dipetalonema viteae and Litomosoides carinii in jirds and Onchocerca spp. in horses and cattle; but activity has not been observed against microfilariae of Brugia pahangi in jirds or cats. Efficacy against filarial parasites has been observed following oral or parenteral administration of drug, sometimes at extremely low dosage. For example, a single oral dosage of 0.05 mg/kg was highly active against the third and fourth larval stages and microfilariae of D. immitis in dogs.

摘要

阿维菌素是由阿维链霉菌产生的大环内酯类化合物。其中一种已进行化学修饰,并被赋予通用名称伊维菌素。这些化合物已显示出对丝虫寄生虫各个阶段的疗效。对于哺乳动物宿主体内未成熟阶段的寄生虫,已观察到其对雪貂和犬体内的犬恶丝虫、沙鼠(子午沙鼠)体内的魏氏棘唇线虫和卡里尼丝虫有活性;但未观察到其对沙鼠体内布鲁线虫属的发育阶段或牛体内盘尾丝虫属的发育阶段有活性。除马体内的马丝状线虫以及可能沙鼠体内的魏氏棘唇线虫外,这些化合物对成虫阶段的丝虫没有活性。对于哺乳动物宿主体内的第一期幼虫(微丝蚴),已观察到其对犬体内的犬恶丝虫、多乳鼠(非洲巨鼠)体内的马来布鲁线虫、沙鼠体内的魏氏棘唇线虫和卡里尼丝虫以及马和牛体内的盘尾丝虫属有活性;但未观察到其对沙鼠或猫体内的彭亨布鲁线虫微丝蚴有活性。口服或肠胃外给药后已观察到对丝虫寄生虫有疗效,有时剂量极低。例如,0.05毫克/千克的单次口服剂量对犬体内犬恶丝虫的第三和第四幼虫阶段以及微丝蚴有高度活性。

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J Neurochem. 1980 Feb;34(2):351-8. doi: 10.1111/j.1471-4159.1980.tb06604.x.
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Immunization of ferrets against Dirofilaria immitis by means of chemically abbreviated infections.
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Resolving the origins of secretory products and anthelmintic responses in a human parasitic nematode at single-cell resolution.单细胞分辨率解析人体寄生线虫的分泌产物和驱虫反应的起源。
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J Med Chem. 1980 Oct;23(10):1134-6. doi: 10.1021/jm00184a014.
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