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The elimination half-life is approximately 45 h.In this review we will discuss the results from the randomized, controlled, and double blind trials (RCTs) of tibolone, with respect to its effects on climacteric symptoms, sexual function, endometrial and breast tissue, lipid metabolism, and bone mineral density (BMD).A computerized search of the published literature in diverse electronic databases, including MEDLINE, Gallen II, EMBASE, and Cochrane library, was conducted. Summaries of the study design, duration of the trials, participant demographics, and different outcomes are presented in Tables 1–4Menopause-associated symptoms impair quality of life for many women. Tibolon: eine Alternative zur Oestrogensubstitution?Tibolone: a steroid with a tissue-specific mode of action.Human endometrial 3β-hydroxysteroid dehydrogenase/isomerase can locally reduce intrinsic estrogenic/progestagenic activity ratios of a steroidal drug (Org OD 14).Estrogenic and progestagenic activities coexisting in steroidal drugs: quantitative evaluation by in vitro bioassays with human cells.Placebo-controlled cross-over study of effects of Org OD 14 in menopausal women.Use of a new steroid (Org OD 14) in the climacteric syndrome.Effects of Org OD 14 on pituitary and peripheral β-endorphin in castrated rats and post-menopausal women.Double-blind cross-over study with Org OD 14 and placebo in postmenopausal patients.Long-term placebo-controlled efficacy and safety study of ORG OD 14 in climacteric women.Treatment of climacteric complaints with Org OD 14: a comparative study with oestradiol valerate and placebo.Effect on sexual life–a comparison between tibolone and a continuous estradiol-norethisterone acetate regimen.Defferential effects on the androgen status of postmenopausal women treated with tibolone and continuous combined estradiol and norethindrone acetate replacement therapy.A double-blind, randomised trial comparing the effects of tibolone and continuous combined hormone replacement therapy in postmenopausal women with menopausal symptoms.A randomised placebo controlled trial of the effects of tibolone on blood pressure and lipids in hypertensive women.Effects of long-term Org OD 14 administration on blood coagulation in climacteric women.Coagulation and fibrinolysis in post-menopausal women treated with Org OD 14.Resistance of pelvic arteries and plasma lipids in postmenopausal women: comparative study of tibolone and continuous combined estradiol and norethindrone acetate replacement therapy.Tibolone: influence on markers of cardiovascular disease.The effect of the synthetic steroid Org OD14 on fibrinolysis and blood lipids in postmenopausal women.Effects of two doses of tibolone on trabecular and cortical bone loss in early postmenopausal women: a two-year randomized, placebo-controlled study.Absent correlation between vaginal bleeding and oestradiol levels or endometrial morphology during tibolone use in early postmenopausal women.Tibolone: prevention of bone loss in late postmenopausal women.Clinical review 82: androgens and the postmenopausal woman.Effects of tibolone and continuous combined hormone replacement therapy on parameters in the clotting cascade: a multicenter, double-blind, randomized study.Pharmacokinetics and metabolism of sildenafil in mouse, rat, rabbit, dog and man.The response in spinal bone mass to tibolone treatment is related to bone turnover in elderly women.Prospective double-blind trial of synthetic steroid (Org OD 14) for preventing postmenopausal osteoporosis.Non-linear increase in vertebral density induced by a synthetic steroid (Org OD 14) in women with established osteoporosis.Prevention of bone loss with tibolone in postmenopausal women: results of two randomized, double-blind, placebo-controlled, dose-finding studies.Short-term effects of Org OD 14 and 17β-oestradiol on bone and lipid metabolism in early post-menopausal women.Anti-estrogens, selective estrogen receptor modulators (SERM), tibolone: modes of action.Effects of Org OD14 (Livial) and its metabolites on 17β-hydroxysteroid dehydrogenase activity in hormone-dependent MCF-7 and T-47D breast cancer cells.Concentrations of estrone, estradiol, and estrone sulfate and evaluation of sulfatase and aromatase activities in pre- and postmenopausal breast cancer patients.Effect of tibolone (Org OD14) and its metabolites on estrone sulphatase activity in MCF-7 and T-47D mammary cancer cells.

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