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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク Tibolone ： ウィキペディア英語版 Tibolone Tibolone (INN, USAN, BAN) (brand name Livial, Tibofem) is a synthetic steroid drug with estrogenic, progestogenic, and weak androgenic actions which was introduced in 1988 and is used widely in Europe, Asia, Australasia, and, with the exception of the United States (where it is not available), the rest of the world. It is used mainly for treatment of endometriosis, as well as hormone replacement therapy in post-menopausal women. Tibolone has similar or greater efficacy compared to older hormone replacement drugs, but shares a similar side effect profile. It has also been investigated as a possible treatment for female sexual dysfunction. Tibolone is a 19-nortestosterone derivative and is related structurally to other 19-nortestosterone progestins. ==Pharmacology== Tibolone possesses a complex pharmacology. Its two major active metabolites, 3α-hydroxytibolone and 3β-hydroxytibolone, act as potent, fully activating agonists of the estrogen receptor (ER), with a high preference for ERα.〔 Tibolone and its metabolite Δ4-tibolone act as agonists of the progesterone and androgen receptors,〔 while 3α-hydroxytibolone and 3β-hydroxytibolone, conversely, act as antagonists of these receptors.〔 Lastly, tibolone, 3α-hydroxytibolone, and 3β-hydroxytibolone act as antagonists of the glucocorticoid and mineralocorticoid receptors, with preference for the mineralocorticoid receptor.〔 Tibolone has tissue-selective estrogenic effects, with desirable effects in bone, the brain, and the vagina, and lack of undesirable action in the endometrium and breasts.〔 Its tissue selectivity is the result of metabolism, enzyme modulation (e.g., of estrogen sulfatase and estrogen sulfotransferase), and receptor modulation that vary in different target tissues, and differs mechanistically from that of selective estrogen receptor modulators (SERMs) such as tamoxifen, which produce their tissue-selectivity via means of modulation of the ER.〔〔 As such, to distinguish it from SERMs, tibolone has been described as a "selective tissue estrogenic activity regulator" (STEAR),〔 and also as a "selective estrogen enzyme modulator" (SEEM). 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Tibolone」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.