Urinary metabolites of dl-methadone in maintenance subjects.
Urinary metabolites of dl-methadone in maintenance subjects.
复制标题
维持受试者中 dl-美沙酮的尿液代谢物。
DOI：
10.1021/jm00266a009
复制
发表时间：
1973
影响因子：
7.3
通讯作者：
S. L. Due
中科院分区：
文献类型：
--
作者：
H. Sullivan;S. L. Due
研究对象。三名年龄为23-36岁的美沙酮耐受男性受试者参加了本研究。他们一直在参与美沙酮维持计划，在这个实验室和其他地方尝试用化学方法制备N-去甲基美沙酮，到目前为止总是导致2的分离。在未发表的研究中，我们进行了美沙酮的体外酶促去甲基化，并试图用仲胺捕获剂“捕获”N-去甲基美沙酮。然而，只有2人被隔离。我们认为，去甲基美沙酮足够不稳定，使得其在体内形成后几乎立即转化为2。位于马里兰州的巴尔的摩，为期4个月至5年。每名受试者都有长期的多种药物滥用史，每天接受80-100 mg美沙酮的维持剂量。在每日剂量美沙酮给药后24小时内，在监督下采集尿样。由于吡咯烷代谢物对空气氧化的极端敏感性，并且由于美沙酮尿液在室温下保存容易产生模拟美沙酮N-氧化物行为的伪影，因此立即冷冻每个尿液收集物，并在-10 ℃下冷冻保存直至使用。
MethodsSubjects. Three male, methadone-tolerant subjects, ages 23-36 years, participated in the study. They hadbeen participating in the methadone maintenance program at t Attempts in this laboratory and elsewhereto prepare jV-des-methylmethadone chemically have to date always led to theisolation of 2. In unpublished studies we have carried out the in vitro enzym-atic demethylation of methadone andattempted to “trap” JV-des-methylmethadone with secondary amine trapping agents. Neverthe-less, only 2 was isolated. It is our feeling that Mdesmethylmethadone is sufficiently unstable so that it converts to 2 almost immediately following its in vivo formation.Man Alive Research, Inc., of Baltimore, Md., for a period of 4 months to 5 years. Each subject had a long history of multidrug abuse and was receiving a daily maintenance dosage of 80-100 mg of methadone. Urine samples were collected under supervision for 24 hr following administration of the daily dose of methadone. Each urinecollection was immediately frozen and was kept frozen at-10 until use because of the extreme sensitivity of the pyrrolidine metaboliteto air oxidation andbecause methadone urines kept at room temperature tend to develop artifacts that mimic the behavior of methadone N-oxide.