文章基本信息

标题：COMPARISON OF THE FIRST-PASS METABOLISM OF ETHENZAMIDE AND SALICYLAMIDE IN RATS
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作者：JUICHIRO SHIBASAKI ; RYOJI KONISHI ; MITSUKO TAKEMURA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1984
卷号：7
期号：11
页码：804-810
DOI：10.1248/bpb1978.7.804
出版社：The Pharmaceutical Society of Japan
摘要：The first-pass metabolism of ethenzamide (ETB), which is considered to be a prodrug of salicylamide (SAM), was studied in rats in order to compare with that of SAM. The extent of first-pass metabolism after oral ETB estimated by oral and intravenous administration was as much as 82% and remaining 18% ETB entered into systemic circulation. Further, it has been confirmed that the first-pass metabolism of ETB is not due to the intestine but entirely due to the liver in which de-ethylation to SAM occurred at first, followed by exclusive conjugation with sulfuric acid and little SAM enters into the systemic circulation. On the other hand, it was previously demonstrated in rats that per se administered SAM is subjected to first-pass metabolism both in the gut and liver as much as about 60% and the remaining 40% entered the systemic circulation. Thus, the behavior of SAM is considerably different depending upon whether it is per se administered or formed from ETB through metabolism. The fact that little SAM appears in the systemic circulation after oral administration of ETB suggests that the pharmacological activity of ETB comes from its own attributes but not from SAM.
关键词：biliary excretion