Effects of tibolone on selectins in postmenopausal women

Long-term effects of tibolone on circulating levels of vascular cell adhesion molecules and E-selectin in postmenopausal women

“…Our results are in accordance with those of Sator and co-workers, who recently, in a randomized placebocontrolled study, demonstrated that postmenopausal women treated with tibolone had a significant decrease for the variables E-selectin, L-selectin, and platelet-endothelial cell adhesion molecule (PECAM-1) after 8 weeks of treatment (20,21). Our results agree also with the data of Register et al (19) who compared the effects of tibolone, E replacement therapy, and E plus progestogen replacement therapy on VCAMs and endothelin-1 concentrations in surgically postmenopausal cynomolgus monkeys.…”

“…The sample size was determined with the use of statistical software (Epistat, Tracy L. Gustafson, M.D., Round Rock, TX), based on an expected 20% reduction in VCAM levels induced by tibolone in postmenopausal women (20,21), a 90% chance of detecting a 20% difference between the groups treated with tibolone and with placebo, and a 90% chance that any difference at the usual level of statistical significance between the two groups would not simply be due to chance.…”

“…In fact, tibolone administration induces a decrease in endothelin levels (15) and an increase in serum nitric oxide levels (16,17). Tibolone also reduces the expression of VCAMs in human isolated endothelial cells (18) and decreases circulating VCAM levels in monkeys (19), as well as in postmenopausal women after 8 weeks of treatment (20,21). To the best of our knowledge, no data exist on the effects of long-term treatment with tibolone on circulating VCAM levels.…”

Cardiovascular Effects of Tibolone: A Selective Tissue Estrogenic Activity Regulator

“…Thus, tibolone caused a rapid and sustained decrease in circulating levels of VCAMs but this effect was lost soon after stopping the treatment. In another clinical study, tibolone significantly decreased endothelial expression of sE-selectin, sL-selectin, and sPECAM-1 after 8 weeks of treatment in healthy postmenopausal women (Sator et al 2006). By reducing leukocyte adhesion molecule expression in endothelial cells, tibolone might, therefore, exert additional, lipid-independent, cardioprotective effects in postmenopausal women.…”

Dissolution rate enhancement of the poorly water-soluble drug Tibolone using PVP, SiO2, and their nanocomposites as appropriate drug carriers

“…It is structurally related to the progestogens, norethindrone and norethynodrel, and it is a known tissue-specific and effective agent that can be used in hormone replacement therapy (HRT) in (post)menopausal woman, for the treatment of menopausal and postmenopausal disorders, including climacteric complaints, vasomotor symptoms, osteoporosis, and vaginal atrophy [17][18][19][20][21][22][23] . The already published papers concerning the dissolution rate enhancement of Tibo are limited 24 .…”