口服避孕用新型孕激素。

Contraceptive delivery systems Pub Date : 1982-01-01
E De Jager
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引用次数: 0

摘要

去索孕酮(13-乙基-11-亚甲基- 18,19 -dinor-17 -孕酮-4-en-20-yn-17-ol)是一种适用于联合口服避孕药(OC)的新型强效孕激素。目前已经开发了两种产品,一种含有150微克地格孕酮加30微克炔雌醇(EE)/片(Marvelon),另一种是含有50微克EE(7片)的正相产品,然后是125微克地格孕酮加50微克EE(15片)。在大规模多中心试验中没有出现片剂失效的报道。经受体研究证实的临床研究表明,在使用剂量下,地索孕酮缺乏雄激素原性。此外,脂质代谢研究显示,地索孕酮并不能消除ee诱导的高密度脂蛋白胆固醇升高。由于低水平的高密度脂蛋白胆固醇与缺血性心脏病的风险增加有关,这可以被认为是去索孕酮的一个有利方面。鉴于对更安全的OCs的需求日益增加,可以得出结论,应优先考虑含有该孕激素的OCs。
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A new progestagen for oral contraception.

Desogestrel (13-ethyl-11-methylene-18, 19-dinor-17alpha-pregn-4-en-20-yn-17-ol) is a new potent progestagen suitable for incorporation into combined oral contraceptives (OC)s. 2 products have thus far been developed, 1 containing 150 mcg desogestrel plus 30 mcg ethinyl estradiol (EE)/tablet (Marvelon) and the other a normophasic product containing 50 mcg EE (7 tablets) followed by 125 mcg desogestrel plus 50 mcg EE (15 tablets). No tablet failures were reported in large-scale multicenter trials. Clinical studies, confirmed by receptor studies, showed that desogestrel lacks androgenicity in the dosages used. Also, studies on lipid metabolism revealed that desogestrel does not abolish EE-induced rises in HDL cholesterol. Since low levels of HDL cholesterol have been associated with an increased risk of ischemic heart disease, this can be regarded as a favorable aspect of desogestrel. In view of increasing demands for safer OCs, it can be concluded that preference should be given to OCs containing this progestogen.

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