Pros and cons of existing treatment modalities in osteoporosis: a comparison between tibolone, SERMs and estrogen (±progestogen) treatments

@article{Kloosterboer2002ProsAC,
  title={Pros and cons of existing treatment modalities in osteoporosis: a comparison between tibolone, SERMs and estrogen (±progestogen) treatments},
  author={Helenius Jan Kloosterboer and A. G. H Ederveen},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2002},
  volume={83},
  pages={157-165}
}
Tibolone, selective estrogen receptor modulators (SERMs) like tamoxifen and raloxifene, and estrogen (+/-progestogen) treatments prevent bone loss in postmenopausal women. They exert their effects on bone via the estrogen receptor (ER) and the increase in bone mass is due to resorption inhibition. The effect of SERMs on bone mineral density is less than that with the other treatments, but the SERM raloxifene still has a positive effect on vertebral fractures. In contrast to tibolone and… Expand
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References

SHOWING 1-10 OF 71 REFERENCES
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
Tibolone Exerts Its Protective Effect on Trabecular Bone Loss Through the Estrogen Receptor
  • A. Ederveen, H. Kloosterboer
  • Medicine
  • Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research
  • 2001
TLDR
The results indicate that tibolone acts on bone almost entirely through activation of the estrogen receptor, excluding a major role of the androgenic and progestogenic activities of tIBolone in its action against trabecular bone loss. Expand
Comparative effects on bone mineral density of tibolone, transdermal estrogen and oral estrogen/progestogen therapy in postmenopausal women.
TLDR
Since tibolone effected a greater increase in spine BMD than did either conjugated equine estrogen with progestogen or transdermal estradiol alone, it is particularly suitable for older women who often have more advanced osteoporosis and who would not accept a return of cyclical bleeding. Expand
Prevention of Postmenopausal Bone Loss Using Tibolone or Conventional Peroral or Transdermal Hormone Replacement Therapy with 17β‐Estradiol and Dydrogesterone
TLDR
Tibolone can be regarded as an alternative to conventional HRT to prevent postmenopausalBone preservation was observed in all three treatment groups as compared with controls, without significant differences among treatment regimens. Expand
Time-dependent changes in biochemical bone markers and serum cholesterol in ovariectomized rats: effects of raloxifene HCl, tamoxifen, estrogen, and alendronate.
TLDR
The results indicate that for treatment of postmenopausal osteoporosis, raloxifene HCl may have an advantage over the other antiresorptive agents studied in having both non-uterotrophic and hypocholesterolemic effects in addition to its ability to inhibit bone resorption. Expand
Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women.
TLDR
Daily therapy with raloxifene increases bone mineral density, lowers serum concentrations of total and low-density lipoprotein cholesterol, and does not stimulate the endometrium. Expand
A 3-year study of prevention of postmenopausal bone loss: conjugated equine estrogens plus medroxyprogesterone acetate versus tibolone.
TLDR
Tibolone not only prevented cortical and trabecular bone loss, but further increased bone mineral density at the lumbar spine and at the hip throughout the 3 years of treatment, suggesting a sustained positive effect on bone mass. Expand
Raloxifene inhibits bone turnover and prevents further cancellous bone loss in adult ovariectomized rats with established osteopenia.
TLDR
Evidence is provided that raloxifene is a much more potent estrogen agonist on the skeleton and liver than on the uterus, and that estrogen treatment after menopause reduces body weight and serum cholesterol. Expand
Tibolone, a Steroid with a Tissue‐Specific Hormonal Profile, Completely Prevents Ovariectomy‐Induced Bone Loss in Sexually Mature Rats
  • A. Ederveen, H. Kloosterboer
  • Medicine
  • Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research
  • 1999
TLDR
Treatment with tibolone for 4 weeks prevented OVX‐induced bone loss by suppressing both bone resorption and bone turnover in a similar way as EE2, however, the frequency of dosing is more important for EE2 than for tIBolone. Expand
A comparison of tibolone and conjugated equine estrogens effects on coronary artery atherosclerosis and bone density of postmenopausal monkeys.
TLDR
It is suggested that tibolone is a cardiovascular-safe treatment for climacteric symptoms and the prevention of osteoporosis, and there was no increase in CAA despite adverse effects of tIBolone on plasma lipoprotein concentrations. Expand
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