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依地骨化醇用于治疗骨质疏松症。

Eldecalcitol for the treatment of osteoporosis.

作者信息

Matsumoto T, Endo I

机构信息

University of Tokushima Graduate School of Medical Sciences, Kuramoto-cho, Tokushima, Japan.

出版信息

Drugs Today (Barc). 2012 Mar;48(3):189-96. doi: 10.1358/dot.2012.48.3.1745223.

Abstract

Eldecalcitol [1α,25-dihydroxy-2β-(3-hydroxypropyloxy)-vitamin D₃] is an analogue of 1α,25-dihydroxyvitamin D₃ [1,25(OH)₂D₃], bearing a hydroxypropyloxy residue at the 2β position. Eldecalcitol shows stronger effects than alfacalcidol to increase bone mineral density and reduce bone resorption markers in osteoporotic patients, and oral once-daily 0.75 μg eldecalcitol reduced vertebral fracture incidence by 26% compared to 1.0 μg alfacalcidol in a 3-year randomized, double-blind, active-comparator clinical trial. The effect of eldecalcitol on vertebral fracture incidence was sustained throughout the 3-year study period, and the annual incidence of vertebral fracture during the third year was significantly lower with eldecalcitol rather than with alfacalcidol treatment (3.9% vs 7.0%, respectively). Eldecalcitol also reduced the incidence of wrist fractures by 71% compared to alfacalcidol. Eldecalcitol is well tolerated and is not associated with serious side effects including sustained hypercalcemia. Eldecalcitol was approved for the treatment of osteoporosis in Japan in 2011.

摘要

eldecalcitol[1α,25 - 二羟基 - 2β - (3 - 羟丙氧基) - 维生素D₃]是1α,25 - 二羟基维生素D₃[1,25(OH)₂D₃]的类似物,在2β位带有一个羟丙氧基残基。在骨质疏松症患者中, eldecalcitol在增加骨矿物质密度和降低骨吸收标志物方面比阿法骨化醇表现出更强的效果。在一项为期3年的随机、双盲、活性对照临床试验中,每天口服0.75μg eldecalcitol与1.0μg阿法骨化醇相比,椎体骨折发生率降低了26%。在整个3年的研究期间, eldecalcitol对椎体骨折发生率的影响持续存在,并且在第三年, eldecalcitol治疗组的椎体骨折年发生率显著低于阿法骨化醇治疗组(分别为3.9%和7.0%)。与阿法骨化醇相比, eldecalcitol还使腕部骨折的发生率降低了71%。 eldecalcitol耐受性良好,且不伴有包括持续性高钙血症在内的严重副作用。2011年, eldecalcitol在日本被批准用于治疗骨质疏松症。

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