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血吸虫感染对小鼠非那宗清除率的影响。

Effect of schistosomiasis infection on the clearance of phenazone in mice.

作者信息

Metwally A A, Janku I, Kemper F, Khayyal M T, Ebeid F A, Botros S S

机构信息

Theodor Bilharz Research Institute, Pharmacology Department, Warrak El-Hadar, Egypt.

出版信息

Arzneimittelforschung. 1990 Feb;40(2 Pt 1):206-9.

PMID:2110459
Abstract

The disposition phenazone (antipyrine) was used to study the effect of Schistosoma mansoni infection on the activity of drug metabolizing enzymes in mice. Plasma elimination rate constant (Ke), elimination half-life (t1/2e), clearance (CL) and apparent volume of distribution (Vd) were estimated 8 and 12 weeks after infection of mice with 80 S. mansoni cercariae. Liver and kidney function tests were performed simultaneously. Infection increased the levels of glutamic oxalacetic transaminase (GOT), glutamic pyruvic transaminase (GPT), lactic dehydrogenase (LDH), alkaline phosphatase (AP) and total proteins 8 and 12 weeks post infection. At the same time a decrease was recorded in the total cholesterol level. Moreover infection with S. mansoni produced a decrease in phenazone clearance with an increase in the area under the curve (AUC) of the drug 8 and 12 weeks post infection. Elimination half-lives were 57.92 +/- 14.10 and 72.72 +/- 4.14 min 8 and 12 weeks after infection, respectively, compared to 19.29 +/- 3.30 and 26.14 +/- 5.31 min in corresponding controls. No statistically significant change was recorded in the volume of distribution of phenazone in the groups studied. In addition no significant correlation was found between parameters of phenazone disposition and the enzyme levels studied 8 and 12 weeks after infection.

摘要

使用非那宗(安替比林)来研究曼氏血吸虫感染对小鼠药物代谢酶活性的影响。在用80条曼氏血吸虫尾蚴感染小鼠8周和12周后,估算血浆消除速率常数(Ke)、消除半衰期(t1/2e)、清除率(CL)和表观分布容积(Vd)。同时进行肝功能和肾功能检测。感染后8周和12周,感染组小鼠的谷草转氨酶(GOT)、谷丙转氨酶(GPT)、乳酸脱氢酶(LDH)、碱性磷酸酶(AP)水平及总蛋白含量均升高。与此同时,总胆固醇水平下降。此外,感染曼氏血吸虫后8周和12周,非那宗清除率降低,药物曲线下面积(AUC)增加。感染后8周和12周的消除半衰期分别为57.92±14.10分钟和72.72±4.14分钟,而相应对照组分别为19.29±3.30分钟和26.14±5.31分钟。在所研究的组中,非那宗的分布容积没有统计学上的显著变化。此外,在感染后8周和12周,未发现非那宗处置参数与所研究的酶水平之间存在显著相关性。

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