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| 双膦酸盐的作用机制和急性时相反应 |
| Mechanisms of action and acute phase responses of bisphosphonates |
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| DOI： |
| 中文关键词: 双膦酸盐 构效关系 作用机制 急性时相反应 |
| 英文关键词:Bisphosphonates Structure activity relationships Mechanisms of action Acute phase responses |
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| 中文摘要: |
| 双膦酸盐类药物是无机焦磷酸盐人工合成的类似物，对于骨组织具有非凡的选择性。双膦酸盐可分为两种作用模式:不含氮的双膦酸盐通过整合到三膦酸腺苷不可水解的类似物中，引起破骨细胞凋亡;含氮的双膦酸盐通过抑制 FPP 合酶，使APPPI 积累以及抑制蛋白质的异戊稀化，引起破骨细胞凋亡。双膦酸盐能有效抑制骨吸收，减少骨骼相关事件的发生率和恶性肿瘤的骨转移等。同时也发现了一些双膦酸盐的不利影响，其中双膦酸盐引起的急性时相反应，症状普遍见于初始使用的患者中，仅为轻微短暂的流感样症状，包括发热、乏力和肌肉疼痛等，这种非特殊生理性反应与提高了炎症因子的水平有关。本文将详细论述双膦酸盐的作用机制和急性时相反应。 |
| 英文摘要: |
| Bisphosphonates are synthetic analogs of inorganic pyrophosphates with high avidity for bone． Bisphosphonates can be classified into two modes of action: non-nitrogen containing bisphosphonates are incorporated into non-hydrolysable analogues of adenosine triphosphate，which induce osteoclast apoptosis; nitrogen-containing bisphosphonates inhibit FPP synthesis which can
cause osteoclast apoptosis through two routes，inhibition of protein prenylation and accumulation of ApppI． Bisphosphonates are effective in decreasing bone resorption，the incidence of skeletal related events，and bone metastases of malignant tumors et al．However，adverse effects of bisphosphonates have been observed，which can be associated with acute phase responses generally only occur on first exposure to the drug，an nonspecific physiologic reaction associated with increased levels of inflammatory cytokines，involve only slight transient flu like symptoms including fever，fatigue and myalgia et al． This article will discuss the mechanisms of
action and the acute phase responses of bisphosphonates in details． |
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