Guideline for the Use of Tibolone in South Africa: Tibolone Advisory Board (Guideline) (Drug Overview‪)‬

With the recent publication of the Liberate Trial, it was felt appropriate to re-evaluate the role of tibolone as an option in postmenopausal therapy. An International Consensus Group published its clinical recommendations and practical guidelines in 2005, and this is still the fundamental cornerstone of consensus. (1) The aim of the locally convened advisory board was not only to review the published data, but also specifically to give its opinion on the use of tibolone in South Africa. The meeting of the South African advisory board had cumulative input from 10 national experts on menopause. There were a total of 9 presentations from which the final consensus report ultimately emanated. The meeting was sponsored by an unconditional grant provided by Adcock Ingram. The meeting of the advisory board took place at Fairlawns, Sandton, in November 2009 and had cumulative input from 10 national experts on menopause. Tibolone is an analogue of the progestin, norethynodrel. After ingestion it is converted to three metabolites, namely 3-alpha-and 3-beta-hydroxytibolone, which have oestrogenic effects, and delta-4-isomerase, which has progestogenic and androgenic properties. Both the oestrogenic metabolites bind to the alpha-oestrogen receptor but not the beta-oestrogen receptor, while the delta-4 isomer binds to the alpha-and beta-oestrogen, progestogen and androgen receptors. Tibolone is also a sulphatase inhibitor, blocking conversion of oestrone sulphate to oestrone, as well as stimulating local sulphotransferase activity. In contrast to other forms of postmenopausal hormonal therapy, it decreases sex hormone binding globulin and hence increases circulating free testosterone, thereby further adding to its androgenicity. Tibolone significantly decreases vasomotor symptoms, mood disorders, insomnia, bone loss and vaginal atrophy. It has a favourable impact on the cardiovascular system and minimal impact on the endometrium and on mammary tissue. It has been classified as a selective tissue oestrogenic activity regulator (STEAR). (2-4)