Concept

Tibolone

Summary
Tibolone, sold under the brand name Livial among others, is a medication which is used in menopausal hormone therapy and in the treatment of postmenopausal osteoporosis and endometriosis. The medication is available alone and is not formulated or used in combination with other medications. It is taken by mouth. Side effects of tibolone include acne and increased hair growth among others. Tibolone is a synthetic steroid with weak estrogenic, progestogenic, and androgenic activity, and hence is an agonist of the estrogen, progesterone, and androgen receptors. It is a prodrug of several metabolites. The estrogenic effects of tibolone may show tissue selectivity in their distribution. Tibolone was developed in the 1960s and was introduced for medical use in 1988. It is marketed widely throughout the world. The medication is not available in the United States. Tibolone is used in the treatment of menopausal symptoms like hot flashes and vaginal atrophy, postmenopausal osteoporosis, and endometriosis. It has similar or greater effectiveness compared to older menopausal hormone therapy medications, but shares a similar side effect profile. It has also been investigated as a possible treatment for female sexual dysfunction. Tibolone reduces hot flashes, prevents bone loss, improves vaginal atrophy and urogenital symptoms (e.g., vaginal dryness, dyspareunia), and has positive effects on mood and sexual function. The medication may have greater benefits on libido than standard menopausal hormone therapy, which may be related to its androgenic effects. It is associated with low rates of vaginal bleeding and breast pain. A 2015 network meta-analysis of randomized controlled trials found that tibolone was associated with a significantly decreased risk of breast cancer ( () = 0.317). The decrease in risk was greater than that observed with most of the aromatase inhibitors and selective estrogen receptor modulators that were included in the analysis. However, paradoxically, other research has found evidence supporting an increased risk of breast cancer with tibolone.
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