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骨质疏松(osteoporosis)
骨质疏松(osteoporosis)
Osteoporosis control drugs have two broad categories: inhibition of bone absorption and bone formation. Inhibit bone absorption of drugs have double phosphonic acid salt, on behalf of the drug is Allen phosphonic acid sodium fosamax, calcitonin, selective estrogen receptor modulators, Renault yesterday Finn, estrogen, vitamin D and its derivatives, and calcium supplements; Promoting bone formation drugs include fluoride, parathyroid hormone, vitamin D and its derivatives and anabolic steroids. On the selection of drugs, experts recommend a comprehensive balance between improving the quality of life, reducing the occurrence of fracture and the ratio of cost/benefit to the patient according to the patients condition.
Benzothiophenes (benzothiophenes)
Renault yesterday Finn (Raloxifene hydrochloride, Ⅵ) is developed by Eli Lillys second generation of SERMs representative compounds. Used to prevent osteoporosis in postmenopausal women. The 60mg tablet, which was listed in the United States in 1998, is called Evista. The product of the same specification, listed in Argentina, is called Loxifen, which is used to treat climacteric syndrome. Raloxifene has been approved in 59 countries for treatment of osteoporosis in postmenopausal women.
In vitro receptor binding test results showed that lenoxifene had high affinity to the ER of rats, and half of the inhibitory concentration IC50 was 1.85 + + 0.28 nM (17 beta - estradiol was 0.345 + 0.69 nM and tamoxifen was 272nM). Renoirs selective regulation of ER shows that it is an ER agonist for bone and blood lipids, and ER antagonists for the breast and uterus.
The beneficial effect of renaulcifen on bone tissue has been confirmed by several clinical studies. A study of 7, 705 postmenopausal women 36 months of multicenter, randomized, double-blind clinical research results show that the daily use 60 mg or 120 mg of Renault yesterday, can reduce the incidence of spinal fractures by 30% to 50%, can make the spine
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