Syversen Unni, Halse Johan I
Avdeling for endokrinologi, St. Olavs hospital, Trondheim.
Tidsskr Nor Laegeforen. 2011 Feb 4;131(3):244-7. doi: 10.4045/tidsskr.09.0470.
Bisphosphonates are antiresorptive drugs widely used to treat osteoporosis. They are also used to treat hereditary skeletal diseases with systemic or local defects, and as a supplement in treatment of cancer. This paper provides an overview of pharmacokinetics, mode of action, and clinical effects.
Literature was retrieved through a non-systematic search in Pubmed/Medline.
Bisphosphonates are derivates of pyrophosphate which bind to hydroxyapatite with high affinity. Aminobisphosphonates inhibit an enzyme in the mevalonate pathway, thereby inducing apoptosis and inhibiting osteoclast activity. A reduced incidence of vertebral and hip fractures has been shown for alendronate, risedronate and zoledronate, while ibandronate has been shown to only reduce vertebral fracture. Reduced mortality was observed in a study where patients with recent hip fracture were treated with zoledronic acid. Intravenous bisphosphonates improve compliance and are relatively simple to use. Bisphosphonates reduce the risk for skeletal complications and bone pain in breast cancer, myelomatosis and prostate cancer. They are also effective in the treatment of Paget's disease and bone marrow edema. Gastrointestinal adverse effects are relatively frequent with peroral bisphosphonates, while acute phase reactions with influenza-like symptoms are common with intravenous bisphosphonates.
Aminobisphoshonates are effective in the treatment of osteoporosis and in other bone diseases, and as an adjuvance in the treatment of cancer.
双膦酸盐是广泛用于治疗骨质疏松症的抗吸收药物。它们还用于治疗具有全身或局部缺陷的遗传性骨骼疾病，并作为癌症治疗的补充药物。本文概述了其药代动力学、作用方式和临床效果。
通过在Pubmed/Medline中进行非系统检索获取文献。
双膦酸盐是焦磷酸盐的衍生物，能与羟基磷灰石高亲和力结合。氨基双膦酸盐抑制甲羟戊酸途径中的一种酶，从而诱导细胞凋亡并抑制破骨细胞活性。阿仑膦酸盐、利塞膦酸盐和唑来膦酸盐已显示可降低椎体和髋部骨折的发生率，而伊班膦酸盐仅显示可降低椎体骨折发生率。在一项对近期髋部骨折患者用唑来膦酸治疗的研究中观察到死亡率降低。静脉注射双膦酸盐可提高依从性且使用相对简便。双膦酸盐可降低乳腺癌、骨髓瘤和前列腺癌患者发生骨骼并发症和骨痛的风险。它们在治疗佩吉特病和骨髓水肿方面也有效。口服双膦酸盐相对频繁地出现胃肠道不良反应，而静脉注射双膦酸盐常见类似流感症状的急性期反应。
氨基双膦酸盐在治疗骨质疏松症和其他骨骼疾病以及作为癌症治疗的辅助药物方面有效。
