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1977年荷兰欧加农药厂研制出一种新型的类固醇激素Org OD_(14)(简称OD_(14)),应用于临床治疗更年期综合征,显示其具有突出的优点.本文拟对OD_(14)的化学结构、代谢、药理作用及安全性研究、临床应用作一介绍.一、化学结构及代谢OD_(14)的化学名称为(7α,17α)-17羟基-7甲基19去甲基5(10)烯20炔孕酮.药代动力学研究显示口服OD_(14)后吸收迅速,服药1.5~4小时内血中浓度达高峰.在体内主要代谢产物为3α羟OD_(14)、3β羟OD_(14)及其△~4同分异构体.根据受体结合试验与动物试验结果显示这些代谢产物仍具有生物活性.最
In 1977, a new type of steroid hormone, Org OD_ (14) (OD_ (14)), developed by Oujia Pesticide Factory in Holland, was used in the clinical treatment of climacteric syndrome and showed its outstanding advantages.In this paper, Chemical Structure, Metabolism, Pharmacological Action and Safety Study, Clinical Application I. Introduction to Chemical Structure and Metabolism The chemical name of OD_ (14) is (7α, 17α) -17 hydroxy-7 methyl 19 demethyl (10) Ethinyl progesterone.Pharmacokinetics studies showed that oral administration of OD_ (14) rapidly absorbed, peak blood concentrations within 1.5 to 4 hours after taking the drug.The main metabolites in vivo were 3α hydroxyl OD 14, 3β Hydroxyl OD_ (14) and its △ ~ 4 isomers. According to the results of receptor binding assay and animal experiment, these metabolites are still bioactive.