[苯并咪唑衍生物的药代动力学]。

Voprosy meditsinskoi khimii Pub Date : 2002-05-01
A A Spasov, L A Smirnova, I N Iezhitsa, S A Sergeeva, A A Ozerov
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引用次数: 0

摘要

综述了具有抗精神病、保动、抗心律失常、抗溃疡、抗过敏、抗尿、驱虫药活性的苯并咪唑类药物的药动学性质。在兽医实践中作为驱虫药使用的苯并咪唑衍生物的药代动力学也被考虑。苯并咪唑衍生物的特点是多室和不明确的药代动力学模型。苯并咪唑的衍生物在肝脏中进行第一次代谢,因此,它们被转化为活性和非活性代谢物。有必要考虑到苯并咪唑与其他药物的共同给药。观察了苯并咪唑的肝十二指肠循环和未改变药物及其代谢物在肠道内的反复吸附。许多苯并咪唑衍生物的特点是在口服时绝对生物利用度相当低(从2%到60%)。苯并咪唑衍生物可与血液中的蛋白质和细胞成分结合。通常,苯并咪唑的药代动力学谱在低剂量时是线性的,但在高剂量时就失去了线性。动物和人的药代动力学模型几乎总是相同的。
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[Pharmacokinetics of benzimidazole derivatives].

Pharmacokinetic properties of benzimidazole derivatives drug possessing antipsychotic, actoprotector, antiarrhythmic, antiulcerogenic, antiallergic, uricosuric, anthelmintic activities have been summarized. Pharmacokinetics of benzimidazole derivatives used in veterinary practice as anthelmintic drugs is also considered. Benzimidazoles derivatives are characterised by multicompartment and ambiguous pharmacokinetic models. The derivatives of benzimidazoles are subjected to the first pass metabolism in the liver, and, therefore, they are converted to both active, and inactive metabolites. It is necessary to take into account for coadministration of benzimidazoles with other drugs. Hepatoduodenal circulation and repeated adsorption of unchanged drug and its metabolites in the gut is observed for benzimidazole. Many derivatives of benzimidazoles are characterised by rather low absolute bioavailability during peroral intake (from 2 up to 60%). Benzimidazsole derivative may bind to proteins and cell elements of blood. More often pharmacokinetic profile of benzimidazoles is linear for low doses, however, at high doses the linearity is lost. For animals and men pharmacokinetic models are always nearly identical.

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