Saito Mitsuru
Department of Orthopaedic Surgery, Jikei University School of Medicine.
Clin Calcium. 2010 Mar;20(3):345-54.
Selective Estrogen Receptor Modulators (SERMs) such as raloxifene are characterized as anti-bone resorptive agent as well as bisphosphonate. Recently, bone mass and quality affect bone strength independently. Oxidative stress induced by hyperhomocysteinemia deteriorates bone quality in terms of collagen enzymatic and non-enzymatic cross-links such as pentosidine (Saito M, Osteoporos Int [REVIEW], 2010). Such deterioration of bone quality also exist in osteoporotic patient with mildly elevated plasma homocysteine (Saito M, Calcif Tissue Int, 2006). Such detrimental cross-link formation in bone was ameliorated by raloxifene treatment (Saito M, Osteoporos Int, 2009, May 30, in press). In contrast. bisphosphonate treatment increases degree of mineralization, collagen maturity, and pentosidine. The treatment had no effect on the total amount of enzymatic cross-link formation (Saito M, Osteoporos Int, 2008). Based on these results, osteoporotic patients with hyperhomocysteinemia had better take raloxifene, while patients with severe low bone mineral density should take bisphosphonate.
选择性雌激素受体调节剂（SERM），如雷洛昔芬，其特性与双膦酸盐一样，是抗骨吸收剂。近来发现，骨量和骨质量对骨强度有独立影响。高同型半胱氨酸血症诱导的氧化应激会使骨质量在胶原酶促和非酶促交联方面恶化，如戊糖苷（斋藤M，《骨质疏松国际》[综述]，2010年）。在血浆同型半胱氨酸轻度升高的骨质疏松患者中也存在这种骨质量恶化情况（斋藤M，《钙化组织国际》，2006年）。雷洛昔芬治疗可改善骨中这种有害交联的形成（斋藤M，《骨质疏松国际》，2009年，5月30日，即将发表）。相比之下，双膦酸盐治疗会增加矿化程度、胶原成熟度和戊糖苷。该治疗对酶促交联形成的总量没有影响（斋藤M，《骨质疏松国际》，2008年）。基于这些结果，患有高同型半胱氨酸血症的骨质疏松患者最好服用雷洛昔芬，而骨矿物质密度严重偏低的患者应服用双膦酸盐。
