Clin Osteol 2008; 13(1): 12-16
Tibolone in the prevention and treatment of postmenopausal osteoporosisShort communications
For over 20 years, tibolone has been used for the treatment of vasomotor symptoms and for the prevention of osteoporosis in postme nopausal women. Thanks to its unique, tissue-specific metabolism, it was included in the group of selective tissue estrogenic activity regulators (STEARs). Tibolone decreases bone turnover to an extent similar to that in hormonal therapy and increases bone mineral density in both younger and older postmenopausal women. This was confirmed by a large clinical study that informed about statisti cally significant reduction in the risk of new vertebral fractures in elderly osteoporotic women treated with a daily dose of 1.25 mg of ti bolone. However, in this population of elderly women, prolonged use of tibolone was related to a higher risk of stroke. Because of its high effectiveness in reducing menopausal problems and symptoms connected with urogenital atrophy, tibolone remains a suitable al ternative for preventing osteoporosis in patients with acute menopausal syndrome and an increased risk of osteoporosis. Despite ex cellent results in lowering the risk of fractures, tibolone has not been indicated for further use in the treatment of osteoporosis.
Keywords: tibolone, STEARs, osteoporosis, menopause
Published: June 11, 2008 Show citation
References
- Kloosterboer HJ. Tibolone: a steroid with a tissue-specific mode of action. J Ste roid Biochem Mol Biol 2001;76:231-238.
Go to original source... - De Gooyer ME, Deckers GH, Schoonen WGEJ, Verheul HAM. Receptor profiling and endocrine interactions of tibolone. Steroids 2002;68:21-30.
Go to original source... - Barkhem T, Carlsson B, Nilsson Y, Enmark E, Gustafsson J-J, Nilsson S. Diffe rential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists. Mol Pharmacol 1998;54:105-112.
Go to original source... - De Gooyer ME, Overklift Vaupel Kleyn GT, Smits KC, Ederveen AGH, Verheul AM, Kloosterboer HJ. Tibolone: a compound with tissue-specific inhibitory effects on sulfatase. Mol Cell End 2001;183:55-62.
Go to original source... - De Gooyer ME, Oppers-Tiemissen HM, Leysen D, Verheul HAM, Kloosterboer HJ: Tibolone is not converted by human aromatase to 7-methyl-17-ethynylestradiol (7-MEE), analysis with sensitive bioassays for estrogens and androgens and LC-MSMS. Steroids 2003;68:233-241.
Go to original source... - Tang B, Markiewicz L, Kloosterboer HJ, Gurpide E: Human endometrial 3-hydroxysteroid dehydrogenase/isomerase can locally reduce intrinsic estrogenic/progestagenic activity ratios of a steroidal drug (Org OD14). J Steroid Biochem Mol Biol 1993; 45:345-351.
Go to original source... - Ederveen AGH, Kloosterboer HJ. Tibolone exerts its protective effect on trabecu lar bone loss through the estrogen receptor. J Bone Miner Res 2001;16:1651-1657.
Go to original source... - Ederveen AGH, Kloosterboer HJ. Tibolone, a steroid with tissuespecific hormone profile, completely prevents ovariectomy-induced bone loss in sexually mature rats. J Bone Miner Res 1999;14:1963-1970.
Go to original source... - Ederveen AGH, Spanjers CPM, Quaytaal JHM, Kloosterboer HJ: Effect of 16 months of treatment with tibolone on bone mass, turnover, and biomechanical quality in mature ovariectomized rats. J Bone Miner Res 2001;16:1674-1681.
Go to original source... - Clarkson TB, Anthony MS, Wagner JD: A comparison of tibolone and conjuga ted equine estrogens effects on coronary artery atherosclerosis and bone density of postmenopausal monkeys. J Clin Endocrinol Metab 2001;86:5396-5404.
Go to original source... - Lindsay R., Hart DMcK, Kraszewski A Prospective double-blind trial of synthe tic steroid (Org OD14) for preventing postmenopausal osteoporosis. Br Med J 1980;280:1207-1209.
Go to original source... - Geusens P, Dequeker J, Gielen J, Schot LPC. Non-linear increase in vertebral den sity induced by a synthetic steroid (Org OD14) in women with established osteo porosis, Maturitas 13 (1991) 151-159.
Go to original source... - Berning B, Van Kuijk C, Kuiper JW, Coelingh Bennink HJT, Kicovic PM, Fauser BJCM. Effects two doses of tibolone on trabecular and cortical bone loss in early postmenopausal women: a 2-year randomized, placebo-controlled study. Bone 1996;19:395-399.
Go to original source... - Gallagher JC, Baylink DJ, Freeman R, McClung M. Prevention of bone loss with ti bolone in postmenopausal women: results of two randomized, double-blind, place bo-controlled, dose-finding studies. J Clin Endocrinol Metab 2001;86:4717-4726.
Go to original source... - Studd J, Arnala I, Kicovic PM, Zamblera D, Kroger H, Holland N. A randomized study of tibolone on bone mineral density in osteoporotic postmenopausal women with previous fractures. Obstet Gynecol 1998;92:574-579.
Go to original source... - Rymer J. 10 Years of treatment with tibolone 2.5 mg daily: effects on bone loss in postmenopausal women. Climacteric 2002;5:390-398.
Go to original source... - Bjarnason NH, Bjarnason K, Haarbo J, Christiansen C.Tibolone: prevention of postmenopausal bone loss in elderly women. J Clin Endocrinol Metab 1996;81: 2419-2422.
Go to original source... - Bjarnason NH, Bjarnason K, Hassager C, Christiansen C.The response in spinal bone mass to tibolone treatment is related to bone turnover in elderly women. Bo ne 1997;20:151-155.
Go to original source... - Lindsay PC, Shaw RW, Coelingh Bennink HJ, Kovic P. The effect of addback tre atment with tibolone (Livial) on patients treated with the gonadotrophin-releasing hormone agonist triptorelin (Decapeptyl). Fertil Steril 1996;65:342-348.
Go to original source... - Banks EE, Beral V, Reeves G, Balkwill A, Barnes I, for the MillionWomen Study Collaborators. Fracture incidence in relation to the pattern of hormone therapy in postmenopausal women. JAMA 2004;291:2212-2220.
Go to original source... - Cummings SR. LIFT study is discontinued. BMJ 2006; 332:667.
Go to original source... - Volker W, Coelingh Bennink HJT, Helmond FA Effects of tibolone on the endo metrium. Climacteric 2001;4:203-8.
Go to original source... - Wender MC, Edelweiss MI, Campos LS, et al. Endometrial assessment in women using tibolone or placebo: 1-year randomized trial and 2-year observational study. Menopause 2004;11:423-9.
Go to original source... - Langer RD, Landgren BM, Rymer J. Helmond FA; OPAL Investigators: Effects of tibolone and continuous combined conjugated equine estrogen/medroxyprogesterone acetate on the endometrium. Am J Obstet Gynecol 2006;195:1320-7.
Go to original source... - Archer DF, Hendrix S, Gallagher JC, Rymer J, Skouby S, Ferenczy A, den Hollander W, Stathopoulos V, Helmond FA for the Tibolone Histology of the Endometrium and Breast Endpoints (THEBES) Study Group, Endometrial Effects of Tibolone. J Clin Endocrinol Metab 2007;92:911-8.
Go to original source... - Colacurci N, Mele D, De Franciscis P,et al.. Effects of tibolone on the breast. Eur J Obstet Gynecol Reprod Biol;1998;80:235-8.
Go to original source... - Million Women Study Collaborators: Breast cancer and hormone-replacement therapy in the Million Women Study. Lancet 2003; August 9, Vol. 36:419-427.
Go to original source... - Štěpán JJ, Pospíchal J, Presl J et al. Prospective trial of ossein-hydroxyapatite compound (OHC) in surgically induced postmenopausal women. Bone 1989;10: 179-185.
Go to original source... - Salpater SR, Walsh JME, Greyber E. Mortality Associated with Hormone Repla cement Therapy in Younger and Older Women, A Metaanalysis. J Gen Intern Med 2004;19:791-804.
Go to original source... - Ettinger B. Tibolone for Prevention and treatment of postmenopausal osteoporo sis. Maturitas 2007; 57:35-38.
Go to original source...

