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不同严重程度血吸虫病患者中安替比林的药代动力学

The pharmacokinetics of antipyrine in patients with graded severity of schistosomiasis.

作者信息

el-Raghy I, Back D J, Osman F, Nafeh M A, Orme M L

出版信息

Br J Clin Pharmacol. 1985 Oct;20(4):313-6. doi: 10.1111/j.1365-2125.1985.tb05069.x.

Abstract

The pharmacokinetics of antipyrine have been studied in patients with schistosomiasis. In comparison to a control group of subjects (n = 6), patients with early (active) schistosomiasis (passing live ova in urine or stools without clinical and laboratory evidence of liver involvement; n = 6) exhibited similar pharmacokinetic parameters. Of seven patients with hepatosplenic schistosomiasis (exhibiting hepatic fibrosis, splenomegaly, at least one episode of haematemesis, ascites), five showed markedly enhanced antipyrine half-life and reduced clearance. Compared to controls, the mean half-life of this group was increased from 10.9 +/- 2.4 to 19.9 +/- 9.5 h (mean +/- s.d.; P less than or equal to 0.05) and clearance reduced from 3.81 +/- 0.74 to 2.18 +/- 0.80 l h-1 (P less than or equal to 0.01). There was no change in the apparent volume of distribution. Liver biopsy was performed on all patients diagnosed as having hepatosplenic schistosomiasis in the 2 weeks prior to the antipyrine study. The results of this study indicate that hepatic microsomal metabolism is impaired in patients with advanced hepatosplenic schistosomiasis.

摘要

已对血吸虫病患者的安替比林药代动力学进行了研究。与对照组受试者(n = 6)相比,早期(活动期)血吸虫病患者(尿或粪便中排出活虫卵但无肝脏受累的临床及实验室证据;n = 6)表现出相似的药代动力学参数。在7例肝脾型血吸虫病患者(表现为肝纤维化、脾肿大、至少一次呕血、腹水)中,5例安替比林半衰期显著延长,清除率降低。与对照组相比,该组的平均半衰期从10.9±2.4小时增加到19.9±9.5小时(均值±标准差;P≤0.05),清除率从3.81±0.74升/小时降低到2.18±0.80升/小时(P≤0.01)。分布表观容积无变化。在安替比林研究前2周,对所有诊断为肝脾型血吸虫病的患者进行了肝活检。本研究结果表明,晚期肝脾型血吸虫病患者的肝微粒体代谢受损。

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