ABSTRACT
Tibolone is a synthetic analogue of the gonadal steroids with combined oestrogenic, progestogenic and androgenic properties (Table 5.6). The parent compound appears to bind preferentially with oestrogen receptors, whereas its metabolites have greater affinity for progesterone and androgen receptors. It prevents experimentally induced oestrogen-deficiency osteoporosis and does not cause endometrial hyperplasia in the doses used in women. It is effective in controlling hot flushes, sweats and mood, and recent studies suggest that it prevents postmenopausal bone loss. It should be used only in women who are at least 1 year postmenopausal. In those women who change from combined HRT to tibolone, cyclical progestogens should be given until the withdrawal bleed ceases. The long-term effects on cardiovascular morbidity have not been evaluated, but tibolone decreases both high-density lipoprotein and VLDL and may increase insulin resistance.
