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选择性雌激素受体调节剂(SERMs)对骨骼的影响。

Skeletal effects of selective oestrogen receptor modulators (SERMs).

作者信息

Díez J L

机构信息

School of Medicine, University of Seville, Spain.

出版信息

Hum Reprod Update. 2000 May-Jun;6(3):255-8. doi: 10.1093/humupd/6.3.255.

DOI:10.1093/humupd/6.3.255
PMID:10874570
Abstract

Women suffer a higher incidence of osteoporosis than men, in part due to oestrogen deficiency after menopause. In fact, the administration of oestrogen to post-menopausal women is associated with a decrease of bone resorption. Tamoxifen is a widely used selective oestrogen receptor modulator in women with breast cancer, which has been shown an agonistic profile in bone. However, tamoxifen seems less effective than oestradiol as an anti-resorptive agent and has no effect when the endogenous production of oestrogen is normal. Additionally, tamoxifen exhibits agonistic activity on the endometrium and has been suggested an oncogenic potential on that tissue. Raloxifene, a selective oestrogen receptor modulator from the benzothiophene family, behaves also as an agonist on the bone in both laboratory and clinical studies. Ongoing clinical trials confirm a protective effect of raloxifene similar to oestrogens. The Multiple Outcome of Raloxifene Evaluation (MORE) study is a prospective, randomized trial which, in a recent 2 year interim analysis, has shown that women suffering from osteoporosis receiving raloxifene had 42% fewer vertebral fractures than women receiving a placebo.

摘要

女性患骨质疏松症的发病率高于男性,部分原因是绝经后雌激素缺乏。事实上,给绝经后女性服用雌激素与骨吸收减少有关。他莫昔芬是一种广泛用于乳腺癌女性的选择性雌激素受体调节剂,已显示在骨骼方面具有激动剂特性。然而,作为一种抗吸收剂,他莫昔芬似乎不如雌二醇有效,并且当雌激素内源性分泌正常时它没有效果。此外,他莫昔芬对子宫内膜表现出激动活性,并被认为在该组织上具有致癌潜力。雷洛昔芬是一种来自苯并噻吩家族的选择性雌激素受体调节剂,在实验室和临床研究中在骨骼上也表现为激动剂。正在进行的临床试验证实雷洛昔芬具有与雌激素相似的保护作用。雷洛昔芬评估多项结果(MORE)研究是一项前瞻性随机试验,在最近的一项为期2年的中期分析中表明,患有骨质疏松症的女性服用雷洛昔芬比服用安慰剂的女性椎体骨折少42%。

相似文献

1
Skeletal effects of selective oestrogen receptor modulators (SERMs).选择性雌激素受体调节剂(SERMs)对骨骼的影响。
Hum Reprod Update. 2000 May-Jun;6(3):255-8. doi: 10.1093/humupd/6.3.255.
2
[Specific estrogen receptor modulators (SERMs)].[特异性雌激素受体调节剂(SERMs)]
Presse Med. 2002 Sep 7;31(28):1323-8.
3
A pharmacological review of selective oestrogen receptor modulators.选择性雌激素受体调节剂的药理学综述
Hum Reprod Update. 2000 May-Jun;6(3):212-24. doi: 10.1093/humupd/6.3.212.
4
Raloxifene: recent information on skeletal and non-skeletal effects.雷洛昔芬:关于骨骼和非骨骼效应的最新信息。
Curr Opin Rheumatol. 2002 Jul;14(4):429-32. doi: 10.1097/00002281-200207000-00017.
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Novel agents to modulate oestrogen action.调节雌激素作用的新型药物。
Br Med Bull. 2000;56(3):773-86. doi: 10.1258/0007142001903355.
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[Selective estrogen-receptor modulators (SERM's) in postmenopausal women].绝经后女性中的选择性雌激素受体调节剂(SERM)
Ned Tijdschr Geneeskd. 1999 Aug 28;143(35):1771-6.
7
Selective estrogen receptor modulation and reduction in risk of breast cancer, osteoporosis, and coronary heart disease.选择性雌激素受体调节与降低乳腺癌、骨质疏松症和冠心病风险
J Natl Cancer Inst. 2001 Oct 3;93(19):1449-57. doi: 10.1093/jnci/93.19.1449.
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Review of raloxifene and its clinical applications in osteoporosis.雷洛昔芬及其在骨质疏松症中的临床应用综述。
Expert Opin Pharmacother. 2002 Jun;3(6):767-75. doi: 10.1517/14656566.3.6.767.
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Benefit-risk assessment of raloxifene in postmenopausal osteoporosis.雷洛昔芬用于绝经后骨质疏松症的获益-风险评估
Drug Saf. 2005;28(8):721-30. doi: 10.2165/00002018-200528080-00006.
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The search for the ideal SERM.
Expert Opin Pharmacother. 2002 Jun;3(6):681-91. doi: 10.1517/14656566.3.6.681.

引用本文的文献

1
Influence of Supplementary Vitamin D on Bone Mineral Density When Used in Combination with Selective Estrogen Receptor Modulators.补充维生素D与选择性雌激素受体调节剂联合使用时对骨密度的影响。
J Menopausal Med. 2019 Aug;25(2):94-99. doi: 10.6118/jmm.19193. Epub 2019 Jul 23.
2
Raloxifene Administration in Women Treated with Long Term Gonadotropin-releasing Hormone Agonist for Severe Endometriosis: Effects on Bone Mineral Density.长期使用促性腺激素释放激素激动剂治疗严重子宫内膜异位症的女性服用雷洛昔芬:对骨密度的影响
J Menopausal Med. 2016 Dec;22(3):174-179. doi: 10.6118/jmm.2016.22.3.174. Epub 2016 Dec 31.
3
Effects of raloxifene and estradiol on bone turnover parameters in intact and ovariectomized rats.
雷洛昔芬和雌二醇对去势和完整大鼠骨转换参数的影响。
J Physiol Biochem. 2010 Mar;66(1):23-8. doi: 10.1007/s13105-010-0008-8. Epub 2010 Apr 29.