14的新陈代谢C-labelled甲基多巴在正常和高血压人体。
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非盟王寅,西湖LG、司DG、艾萨克P,威廉姆斯RT
14的新陈代谢C-labelled甲基多巴在正常和高血压人体。
j . 1972年8月,129 (1):1 - 10。doi: 10.1042 / bj1290001。
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4646774 (在PubMed]
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1。命运的口头管理(14)C-labelled l-alpha-methyldopa一直在检查三个正常男人和八个高血压患者服药和三个不。2。(14)C的输出在2天的尿和粪便中4天不是很不同的科目。法线排出约40%的剂量在尿液和粪便的60%,反应者52%(35 - 60%范围)和45%,无42%和41%。大部分的尿(14)C放射性剂量后在24小时中就被淘汰了。3所示。主要的尿液中代谢物是自由和共轭alpha-methyldopa(正常男性,23%;反应者,37%;无,25%的剂量)。 Free and conjugated 3-O-methyl-alpha-methyldopa was about 4% in all subjects, total amines (alpha-methyldopamine and 3-O-methyl-alpha-methyldopamine) about 6% and ketones (mainly 3,4-dihydroxyphenylacetone) about 3%. 4. The output of alpha-methyldopamine (2-4% of dose), 3-O-methyl-alpha-methyldopamine (0.3%) and 3,4-dihydroxyphenylacetone (3-5%) was similar in the one normal and two responders examined. 5. The faecal (14)C in all subjects was unchanged l-alpha-methyldopa. 6. In general, the amounts of the metabolites in the urine in normal men and in responding and non-responding patients were quantitatively similar, except in one non-responding patient who converted nearly two-thirds of the absorbed drug into amines and ketones. There appeared to be no correlation between metabolites in the urine and response or lack of response to the drug. 7. In two normal subjects 70-80% of d-alpha-methyldopa was excreted unchanged in the faeces. Of the absorbed compound most (9-14% of the dose) was excreted as the free and conjugated drug together with a small amount (1-2%) of 3-O-methyl-alpha-methyldopa. No amines and only traces of ketone were excreted.
