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[人口服塞克硝唑后血清浓度及尿排泄的研究。与替硝唑比较]

[Study of serum concentrations and urinary excretion of secnidazole after oral administration in man. Comparison with tinidazole].

作者信息

Populaire P, Decouvelaere B, Renard A, Pasquier P

出版信息

Pathol Biol (Paris). 1980 Nov;28(9):621-4.

PMID:7003510
Abstract

Secnidazole, a derivative of 5-nitro imidazole exhibits trichomonacid, amoebicid and antimicrobial properties; it has been studied in view of its biological fate in healthy volunteers (man and woman) comparatively with tinidazole. Both products were administered orally to the same volunteers at the single dose level of 2 g. The seric concentrations and the pharmacokinetic profile were determined up to the 72nd hour after drug administration. The whole urinary excretion (unchanged product + metabolites) during the same period was determined in percent of the administered dose level. Secnidazole is particularly different from tinidazole owing to its slower blood clearance. The apparent average half-life in the ten volunteers (5 men and 5 women) is about 17 hours for secnidazole and 13 hours for tinidazole. However, for both drugs, a difference between men and women was demonstrated: in female volunteers, the decrease in blood concentrations occurs a little quicker than in male volunteers. Regarding urinary excretion, it is also a little greater in female volunteers than in male volunteers.

摘要

塞克硝唑是5-硝基咪唑的衍生物,具有抗滴虫、抗阿米巴和抗菌特性;已针对其在健康志愿者(男性和女性)体内的生物转归与替硝唑进行了比较研究。两种药物均以2克的单剂量水平口服给予相同的志愿者。在给药后72小时内测定血清浓度和药代动力学曲线。同时测定同一时期内整个尿液排泄量(原形药物+代谢物)占给药剂量水平的百分比。塞克硝唑与替硝唑有显著差异,因为其血液清除较慢。在十名志愿者(5名男性和5名女性)中,塞克硝唑的表观平均半衰期约为17小时,替硝唑为13小时。然而,对于两种药物,均显示出男性和女性之间的差异:在女性志愿者中,血药浓度下降比男性志愿者略快。关于尿液排泄,女性志愿者的排泄量也比男性志愿者略多。

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[Study of serum concentrations and urinary excretion of secnidazole after oral administration in man. Comparison with tinidazole].[人口服塞克硝唑后血清浓度及尿排泄的研究。与替硝唑比较]
Pathol Biol (Paris). 1980 Nov;28(9):621-4.
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Pharmacokinetics of tinidazole and metronidazole in women after single large oral doses.单次大剂量口服后替硝唑和甲硝唑在女性体内的药代动力学
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Secnidazole. A 5-nitroimidazole derivative with a long half-life.塞克硝唑。一种半衰期较长的5-硝基咪唑衍生物。
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Pharmatherapeutica. 1981;3(1):67-70.

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Secnidazole. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic use in the management of protozoal infections and bacterial vaginosis.塞克硝唑。对其抗菌活性、药代动力学特性以及在原生动物感染和细菌性阴道病治疗中的应用综述。
Drugs. 1996 Apr;51(4):621-38. doi: 10.2165/00003495-199651040-00007.
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Tinidazole in anaerobic infections: a review of its antibacterial activity, pharmacological properties and therapeutic efficacy.替硝唑在厌氧菌感染中的应用:抗菌活性、药理特性及治疗效果综述
Drugs. 1982 Aug;24(2):85-117. doi: 10.2165/00003495-198224020-00001.