Reid Ian R, Billington Emma O
Department of Medicine, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand; Auckland District Health Board, Auckland, New Zealand.
Division of Endocrinology and Metabolism, Cumming School of Medicine, University of Calgary, Calgary, AB, Canada.
Lancet. 2022 Mar 12;399(10329):1080-1092. doi: 10.1016/S0140-6736(21)02646-5.
The goal of osteoporosis management is to prevent fractures. Several pharmacological agents are available to lower fracture risk, either by reducing bone resorption or by stimulating bone formation. Bisphosphonates are the most widely used anti-resorptives, reducing bone turnover markers to low premenopausal concentrations and reducing fracture rates (vertebral by 50-70%, non-vertebral by 20-30%, and hip by ~40%). Bisphosphonates bind avidly to bone mineral and have an offset of effect measured in months to years. Long term, continuous use of oral bisphosphonates is usually interspersed with drug holidays of 1-2 years, to minimise the risk of atypical femoral fractures. Denosumab is a monoclonal antibody against RANKL that potently inhibits osteoclast development and activity. Denosumab is administered by subcutaneous injection every 6 months. Anti-fracture effects of denosumab are similar to those of the bisphosphonates, but there is a pronounced loss of anti-resorptive effect from 7 months after the last injection, which can result in clusters of rebound vertebral fractures. Two classes of anabolic drugs are now available to stimulate bone formation. Teriparatide and abaloparatide both target the parathyroid hormone-1 receptor, and are given by daily subcutaneous injection for up to 2 years. Romosozumab is an anti-sclerostin monoclonal antibody that stimulates bone formation and inhibits resorption. Romosozumab is given as monthly subcutaneous injections for 1 year. Head-to-head studies suggest that anabolic agents have greater anti-fracture efficacy and produce larger increases in bone density than anti-resorptive drugs. The effects of anabolic agents are transient, so transition to anti-resorptive drugs is required. The optimal strategy for cycling anabolics, anti-resorptives, and off-treatment periods remains to be determined.
骨质疏松症管理的目标是预防骨折。有几种药物可用于降低骨折风险,要么通过减少骨吸收,要么通过刺激骨形成。双膦酸盐是使用最广泛的抗骨吸收药物,可将骨转换标志物降低到绝经前的低水平,并降低骨折发生率(椎体骨折降低50 - 70%,非椎体骨折降低20 - 30%,髋部骨折降低约40%)。双膦酸盐与骨矿物质紧密结合,其作用抵消期以月至年计。长期连续使用口服双膦酸盐通常穿插1 - 2年的药物假期,以将非典型股骨骨折的风险降至最低。地诺单抗是一种抗核因子κB受体活化因子配体(RANKL)的单克隆抗体,可有效抑制破骨细胞的发育和活性。地诺单抗每6个月皮下注射一次。地诺单抗的抗骨折作用与双膦酸盐相似,但在最后一次注射后7个月开始,抗骨吸收作用明显丧失,这可能导致椎体骨折反弹聚集。现在有两类促合成代谢药物可用于刺激骨形成。特立帕肽和阿巴洛帕肽均作用于甲状旁腺激素-1受体,每日皮下注射,最长使用2年。罗莫单抗是一种抗硬化蛋白单克隆抗体,可刺激骨形成并抑制骨吸收。罗莫单抗每月皮下注射一次,共注射1年。头对头研究表明,促合成代谢药物比抗骨吸收药物具有更强的抗骨折疗效,并且能使骨密度有更大幅度的增加。促合成代谢药物的作用是短暂的,因此需要过渡到抗骨吸收药物。促合成代谢药物、抗骨吸收药物以及停药期的最佳循环策略仍有待确定。