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不同类型骨质疏松治疗方案 骨质疏松 原发性OP 继发性OP 特发性OP 绝经后OP 老年性OP 不同类型骨质疏松治疗方案 不同类型OP 治疗方案 首选治疗药物 基础用药 绝经后OP HRT/SERM ②双膦酸盐 钙剂 活性维生素D 老年性OP ①1,25(OH)2D3 ②双膦酸盐 继发性OP 继发于 疾病 ①治疗原发病 ②双膦酸盐 ③活性维生素D 继发于 药物 尽可能停用或使用最低剂量 维生素D 双膦酸盐 降钙素 特发性OP 双膦酸盐 身高缩短和驼背并非必然 奥德丽 赫本年逾60依然骨骼挺拔 ! Functional Domains of Bisphosphonates Bisphosphonates have several functional domains and different molecular structures. As a class, all bisphosphonates work by binding their phosphonate groups to hydroxyapatite. All approved bisphosphonates have and OH group in R1; this creates a triple hook and enhances binding to bone. Varying the R2 substituents can result in differences in antiresorptive potency of several orders of magnitude. Pamidronate and alendronate have an R2 side chain that contains a basic primary nitrogen atom in an alkyl chain and have greater antiresorptive potency than either etidronate or clodronate. Ibandronate has a more highly substituted nitrogen moiety in R2 and shows greater antiresorptive potency than pamidronate or alendronate. The most potent antiresorptive bisphosphonates are risedronate and zoledronic acid, which both contain a nitrogen atom within a heterocyclic ring in the R2 position. Enhancements in antiresorptive potency resulting from differences in the R2 groups appear to be particularly linked to inhibition of the farnesyl pyrophosphate synthase enzyme within the mevalonate pathway in osteoclasts. Reference Nancollas GH, Tang R, Phipps RJ, et al. Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite. Bone. 2006;38:617-627. 唑来膦酸在骨组织的微循环使其具有更长久的疗效 与骨组织的结合力对于不同的双膦酸盐的不同临床疗效,包括作用强度,药代特点以及持久疗效。 唑来膦酸进入体内后被骨组织迅速吸收,由于强大的吸附力,药物的脱落率很低,并且少量脱落出来的药物可以通过强大的再吸附作用而重被骨组织吸收。因此,唑来膦酸具有更长的作用周期。 Reference Nancollas GH, Tang R, Phipps RJ, et al. Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite. Bone. 2006;38:617-627. Concept of a SERM Selective estrogen receptor modulators (SERMs) are non-horm
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