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Tibolone prevents bone loss and reduces spinal fractures. One uncontrolled English study has suggested that tibolone increases breast cancer risk but better quality placebo controlled randomised trials do not show that breast cancer rates in healthy women are changed by tibolone.
Raw Tibolone Hormones Trenbolone Steroid To Prevent Bone Loss & Reduces Spinal Fractures
Tibolone (brand name Livial, Tibofem), also known as 7α-methylnoretynodrel, 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.
Tibolone 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. Tibolone has also been investigated as a possible treatment for female sexual dysfunction.
|TIBOLONE; LIVIELLA; LIVIAL;|
|Appearance||white crystalline powder|
What is tibolone?
• Tibolone is a synthetic hormone derived from the Mexican yam.
• Tibolone is used to replace the body’s natural sex hormones. It is converted in the body into three other substances which act like the hormones oestrogen, progesterone or testosterone in different tissues.
• Tibolone acts like oestrogen in the brain (preventing flushes), bone (preventing bone loss) and vaginal tissue (preventing dryness and soreness).
• Tibolone also acts like progesterone in the womb to prevent overgrowth of the endometrium and subsequent bleeding. A woman who has not had a hysterectomy does not need to take a progesterone if she is taking tibolone.
• Tibolone has testosterone-like activity that appears to play a role in enhancing women’s mood and libido, although response is variable.
Tibolone is a 19-nortestosterone derivative and is related structurally to other 19-nortestosterone progestins. It is the 7α-methyl derivative of noretynodrel.
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 may interfere with the effectiveness of breast cancer therapies and its use is contraindicated in women with breast cancer.
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).
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