Papapoulos Socrates E
Department of Endocrinology and Metabolic Diseases, Leiden University Medical Center, Leiden, The Netherlands.
Best Pract Res Clin Endocrinol Metab. 2008 Oct;22(5):831-47. doi: 10.1016/j.beem.2008.07.001.
Bisphosphonates (BPs) are taken up preferentially by the skeleton and decrease osteoclast-mediated bone resorption. The capacity of the skeleton to retain BPs is large, and there is no indication for saturation of binding sites with the doses used in osteoporosis. The anti-resorptive action of BPs includes their selective binding to calcium crystals and their subsequent release and uptake by the osteoclasts. There are differences in the affinities of PBs for bone as well as in their anti-resorptive potencies, and the whole molecule is responsible for their inhibitory effect on bone resorption. At the tissue level, they decrease the rate of bone resorption and turnover, increase bone mineral density, and maintain or improve structural and material properties of bone and thereby reduce the risk of fractures. Current studies address questions related primarily to the pharmacological properties of these compounds that are essential for their optimal clinical use, such as for example long-term safety and efficacy.
双膦酸盐（BPs）优先被骨骼摄取，并减少破骨细胞介导的骨吸收。骨骼保留双膦酸盐的能力很强，且没有迹象表明骨质疏松症治疗中所使用剂量会使结合位点饱和。双膦酸盐的抗吸收作用包括它们与钙晶体的选择性结合以及随后被破骨细胞释放和摄取。双膦酸盐对骨骼的亲和力及其抗吸收效力存在差异，且整个分子对其对骨吸收的抑制作用负责。在组织水平上，它们降低骨吸收和骨转换速率，增加骨矿物质密度，并维持或改善骨骼的结构和材料特性，从而降低骨折风险。当前的研究主要探讨与这些化合物的药理学特性相关的问题，这些特性对于其最佳临床应用至关重要，例如长期安全性和疗效。
