Beneficial effect of tibolone on mood, cognition, well-being, and sexuality in menopausal women

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Authors: Andrea Riccardo Genazzani, Nicola Pluchino, Francesca Bernardi, Manolo Centofanti, Michele Luisi

Published Date October 2006 Volume 2006:2(3) Pages 299 - 307

DOI: http://dx.doi.org/10.2147/NDT.S

Andrea Riccardo Genazzani, Nicola Pluchino, Francesca Bernardi, Manolo Centofanti, Michele Luisi

Department of Reproductive Medicine and Child Development, Division of Obstetrics and Gynecology, University of Pisa, Italy

Abstract: Tibolone is a synthetic molecule used extensively for the management of menopausal symptoms, with the proposed additional advantage of enhanced mood and libido. Tibolone, after oral administration, is rapidly converted into 3 major metabolites: 3α-hydroxy tibolone and 3β-hydroxy tibolone, which have estrogenic effects, and the ∆4-isomer, which has progestogenic and androgenic effects. The tissue-selective effects of tibolone are the result of metabolism, of enzyme regulation, and of receptor activation which vary in different tissues. Tibolone seems to be effective on estrogen-withdrawal symptoms such as hot flushes, sweating, insomnia, headache, and vaginal dryness, with results generally comparable to the effects exerted by estrogen-based treatments, and the additional property of a progestogenic activity on the endometrium. As well as relieving vasomotor symptoms, tibolone has positive effects on sexual well-being and mood, and improves dyspareunia and libido. These effects may depend on both estrogenic and androgenic actions exerted at the genital level and in thecentral nervous system, and on a reduction of sex-hormone-binding globulin and an increase of free testosterone, without affecting ∆-5 androgens levels. Based on the evidence available, tibolone is a valuable treatment option to relieve menopausal complaints, especially in women suffering persistent fatigue, blunted motivation, and loss of sexual desire despite an adequate estrogen replacement.

Keywords: tibolone, menopause, mood, well-being and sexuality

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