The metabolism of ondansetron.

D A Saynor, C M Dixon
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Abstract

The metabolism of ondansetron has been studied in rat, dog and man. In laboratory animals absorption of the compound across the gastrointestinal tract is rapid and extensive, but due to high first-pass metabolism, the oral systemic bioavailability is low (less than 10%). The high systemic clearance of ondansetron results in a very short half-life in rat and dog. The renal clearance of ondansetron is low, indicating that the major route of systemic clearance is by metabolism. Routes of excretion of drug-related material differ between laboratory animals and man - the major route in the rat and dog is via the bile, while in man the predominant route is via the urine. However, the routes of metabolism are qualitatively similar in all species, indicating that the species used in toxicological testing of ondansetron were appropriate.

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昂丹西酮的代谢。
研究了昂丹司琼在大鼠、狗和人体内的代谢。在实验动物中,化合物通过胃肠道的吸收迅速而广泛,但由于第一过代谢高,口服全身生物利用度低(小于10%)。昂丹司琼的高全身清除率导致在大鼠和狗的半衰期非常短。昂丹司琼的肾脏清除率较低,提示全身清除率主要通过代谢途径。药物相关物质的排泄途径在实验动物和人类之间是不同的——大鼠和狗的主要途径是通过胆汁,而人类的主要途径是通过尿液。然而,所有物种的代谢途径在质量上是相似的,这表明用于昂丹司琼毒理学试验的物种是合适的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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Effect of soybean feeding on experimental carcinogenesis--III. Carcinogenecity of nitrite and dibutylamine in mice: a histopathological study. Abstracts from the second annual meeting of the Danish Society for Cancer Research. 14 April 1989. International Conference on Supportive Care in Oncology. Brussels (Belgium), 23-25 August 1988. Proceedings. Proceedings of the Ondansetron Symposium. London, 30 June 1989. Pharmacological and anti-emetic properties of ondansetron.
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