二膦酸盐防治骨质疏松症的进展

骨质疏松症是一种骨量减少和骨微结构破坏为特征，骨脆性增加，易导致骨折的全身性疾病。其主要病理生理机制是破骨细胞所介导的骨吸收增加。二膦酸盐在体内能抑制破骨细胞的骨吸收，因此被用于骨质疏松的治疗。二膦酸盐是焦磷酸盐的类似物，是碳（Ｃ）原子替代了焦磷酸盐...

Proogress of Bisphosphonate Research in Prevention and Treatment of Osteroporosis

Bisphosphonates are analogs of inorganic pyrophosphate and potent inhibitors of bone resorption. The effects of bisphosphonates on bone resorption are determined by the structure of R 2. At present, more than ten kinds of bisphosphonates have been developed. Of them, etidronate and alendronate have been approved to treat osteoporotic patients in many countries. Etidronate belongs to the first generation of bisphosphonate. It can effect mineralization at the therapy dose, so the intermitent and cyclical regimen is recommended. Bone mass can increase by 5% and the fracture rate decreases by 50%. No increase of osteoid and mineralization lag time were observed. The alendronate is 1000 times more potent inhibitor of bone resorption than etidronate. It can influence mineralization at 6000 times of therapy dose. A multicenter, double blind, placebo controlled study showed that alendronate treatment for 3 years improved lumbar bone mineral density by 8.8% and decreased fracture rate by 47%. A few side effects were observed in mild gastrointestinal intolerance.