Tibolone: the way to beat many a postmenopausal ailments

@article{Lazovi2008TiboloneTW,
  title={Tibolone: the way to beat many a postmenopausal ailments},
  author={G. Lazovi{\'c} and U. Radivojevic and J. Marinkovi{\'c}},
  journal={Expert Opinion on Pharmacotherapy},
  year={2008},
  volume={9},
  pages={1039 - 1047}
}
Objective: The effects of tibolone on climacteric symptoms, osteoporosis, cardiovascular disease, breasts and the endometrium are summarised, and its role in clinical practice is reviewed in this article. Background: Tibolone has tissue-specific effects on receptors and enzymes that influence the synthesis and metabolism of endogenous sexual steroid hormones. Methods: This evaluation was based on the findings from several randomised studies, which addressed the basic and clinical research on… Expand
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Effects of Human Sulfotransferase 2A1 Genetic Polymorphisms 3 on the Sulfation of Tibolone
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Kinetic analysis revealed that different SULT2A1 allozymes exhibited differential substrate affinity and catalytic efficiency toward the two substrates tested, which provided useful information concerning the differential metabolism of tibolone through sulfation in individuals with different Sult2A 1 genotypes. Expand
15 Pharmacology of Hormone Replacement Therapy in Menopause

References

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Pharmacokinetics of tibolone in early and late postmenopausal women.
TLDR
The pharmacokinetics of tibolone are similar in early (age 45-55 years) and late (65-75 years) postmenopausal women and the two formulations were bioequivalent with respect to the dose-normalized AUC (0, infinity) and the AUC(0,t(fix) values for the 3alpha- and 3beta-hydroxy t Tibolone. Expand
Tibolone: a steroid with a tissue-specific mode of action
  • H. Kloosterboer
  • Medicine, Biology
  • The Journal of Steroid Biochemistry and Molecular Biology
  • 2001
TLDR
It is concluded that tibolone acts as a tissue-specific compound by mediating its effects via steroid receptors and enzymatic pathways, and avoids stimulation of the endometrium and breast tissue. Expand
Tissue-selectivity: the mechanism of action of tibolone.
TLDR
Tibolone appears to regulate estrogenic activity in the various tissues by influencing the availability of estrogenic compounds for the estradiol receptor in a tissue-selective manner and has direct oestrogenic effects on the cardiovascular system. Expand
Tibolone: influence on markers of cardiovascular disease.
TLDR
The overall effect on hemostatic factors of the present doses of tibolone in healthy, late postmenopausal women tends towards increased fibrinolysis and unchanged coagulation, which may be beneficial and might theoretically counterbalance the potentially negative effect of the decrease in high density lipoprotein cholesterol. Expand
Effects of tibolone on human breast cancer cells and human vascular coronary cells
TLDR
The data suggest that tibolone does have tumour cell-growth promoting effects in vitro, however, tiberolone can positively influence the synthesis of markers in cell cultures of human female coronary artery, which modulate vascular tone and which play a decisive role in the various stages of atherosclerosis. Expand
Endometrial effects of tibolone.
TLDR
The Tibolone Histology of the Endometrium and Breast Endpoints Study results confirm previous findings that tibolone does not induce endometrial hyperplasia or carcinoma in postmenopausal women, and it is associated with a better vaginal bleeding profile than CEE/MPA. Expand
Effects of tibolone and continuous combined conjugated equine estrogen/medroxyprogesterone acetate on the endometrium and vaginal bleeding: results of the OPAL study.
TLDR
Compared with conjugated equine estrogen/medroxyprogesterone acetate, tibolone has a better tolerability profile with respect to vaginal bleeding but with a similar endometrial safety. Expand
Tibolone and its metabolites inhibit invasion of human mammary carcinoma cells in vitro.
TLDR
Tibolone and its 3beta-OH metabolite have an anti-invasive effect on the tested breast cancer cell lines in vitro, but this effect on invasion is not correlated with an effect on cell-cell adhesion or motility but coincides with a decreased release of pro-MMP-9 in the medium. Expand
Tissue-selective effects of tibolone on the breast.
TLDR
Clinical studies have shown that tibolone users experience less breast tenderness and do not show an increase in mammographic density as found with continuous combined EPT, and the data concerning tibolin and breast cancer risk are inconclusive and require further investigation. Expand
A pilot study of hormone replacement therapy with tibolone in women with mastopathic breasts.
TLDR
This pilot study showed decreases in breast density as well as an attendant significant alleviation of breast discomfort in women with baseline mastopathic changes treated with tibolone for 6 months, which may be due to the inhibitory effect of tIBolone on the enzymes involved in the biosynthesis of estradiol demonstrated in previous trials. Expand
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