甲硝唑及其主要代谢产物的药代动力学及其对阴道加德纳菌的活性。
Pharmacokinetics of metronidazole and its principal metabolites and their activity against Gardnerella vaginalis.
作者信息
Easmon C S, Ison C A, Kaye C M, Timewell R M, Dawson S G
出版信息
Br J Vener Dis. 1982 Aug;58(4):246-9. doi: 10.1136/sti.58.4.246.
Abstract
The hydroxy metabolite of metronidazole was found to be more active against 21 strains of Gardnerella vaginalis than the parent compound and less affected by culture in carbon dioxide. After 400 mg oral metronidazole (Flagyl) plasma concentrations of the two agents were below the minimum inhibitory concentrations (MICs) for most G vaginalis strains tested. With 2 g metronidazole the plasma concentrations exceeded the MICs of the more sensitive strains. Even with the lower dose of metronidazole clinically useful concentration of metronidazole and its hydroxy metabolite were present in the urine. Urinary excretion of these compounds may contribute to the efficacy of metronidazole in the treatment of vaginitis associated with G vaginalis.
摘要
已发现甲硝唑的羟基代谢物对21株阴道加德纳菌的活性比母体化合物更强，且受二氧化碳培养的影响较小。口服400毫克甲硝唑（灭滴灵）后，两种药物的血浆浓度低于大多数测试阴道加德纳菌菌株的最低抑菌浓度（MICs）。服用2克甲硝唑时，血浆浓度超过了较敏感菌株的MICs。即使使用较低剂量的甲硝唑，尿液中也存在临床上有用浓度的甲硝唑及其羟基代谢物。这些化合物的尿排泄可能有助于甲硝唑治疗与阴道加德纳菌相关的阴道炎的疗效。
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