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Tibolone: a tissue-specific approach to the menopause

S. Palacios*

Palacios Institute of Women's Health, Madrid, Spain

* Correspondence: Dr S. Palacios, Palacios Institute of Women's Health, Jorge Juan 36, 28001 Madrid, Spain.

Abstract

Tibolone, a synthetic steroid that is used for hormone replacement in menopausal women, is metabolized to three primary active agents: 3-alpha-hydroxy-tibolone; 3-betahydroxy-tibolone; and -tibolone. It can exhibit oestrogenic, progestogenic or androgenic activity, depending primarily on the target tissue involved; for this reason, tibolone is said to have tissue-specific activity. Oestrogenic effects on vasomotor symptoms, the vagina and bone mean that tibolone is effective in the management of climacteric symptoms and bone loss. However, it does not cause oestrogenic stimulation of the endometrium or breast tissue, thus reducing the risk for side effects such as bleeding and breast tenderness.

Key Words: Hormone replacement therapy • menopause • tibolone • tissue-specific activity


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