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   Drugs and Chemicals /  R   Raloxifene (Evista, Keoxifene)

A second generation selective estrogen receptor modulator used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.


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   Related Disorders   


Postmenopausal Osteoporosis
Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.
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 Pharmacologic Action
  • Selective Estrogen Receptor Modulator
    A structurally diverse group of compounds distinguished from estrogens by their ability to bind and activate the estrogen receptor, but act as either an estrogen agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the endometrium or second generation based on their patterns of tissue specificity.




Free Full Text 20 Jul 2008
A systematic review and economic evaluation of alendronate, etidronate, risedronate, raloxifene and teriparatide for the prevention and treatment of postmenopausal osteoporosis
Objectives:
To establish the clinical effectiveness and cost-effectiveness of selective oestrogen receptor modulators, bisphosphonates and parathyroid hormone (subject to licensing) for the prevention and treatment of osteoporosis and the prevention of osteoporotic fractures in postmenopausal women.
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Women's Health - Prevention of osteoporosis and osteoporotic fractures in postmenopausal women
For women with severe osteoporosis (osteoporosis plus at least 1 fragility fracture), there is good to fair evidence to recommend the use of alendronate, risedronate, parathyroid hormone (limited duration), raloxifene, etidronate and oral pamidronate therapy (grade A to B recommendation). If none of these drugs is tolerated, hormone replacement therapy (HRT) or calcitonin can be considered.
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Mechanisms of action of antiresorptive therapies of postmenopausal osteoporosis
Estrogens and raloxifene (a selective estrogen receptor modulator that acts as an estrogen agonist in bone) suppress bone remodeling to the premenopausal range, maintaining the function of osteoblasts and osteocytes. In the placebo-controlled osteoporosis treatment trials, all the above treatments reduced the risk of fractures.
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Book Reviews 20 Jul 2008

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Categorization derived from National Library of Medicine.
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