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双膦酸盐:药理学及其在骨质疏松症治疗中的应用

[Bisphosphonates: pharmacology and use in the treatment of osteoporosis].

作者信息

Kishimoto H

机构信息

Department of Orthopaedic Surgery, Tottori University, Faculty of Medicine.

出版信息

Nihon Rinsho. 1998 Jun;56(6):1531-6.

PMID:9648477
Abstract

Bisphosphonates are attractive antiresorptive drugs for osteoporosis. The only compound available in Japan is the first-generation bisphosphonate, etidronate. Etidronate adsorbes to the surface of hydroxyapatite crystals, and can slow bone mineralization and inhibit bone resorption. It has a narrow therapeutic window between these two actions, so that long-term continuous administration is not feasible. The intermittent use of etidronate produces a positive effect on bone mass. But the response varies directly with the rate of bone turnover at baseline. In high turnover osteoporosis there could be a gain in bone mass, but it reaches a plateau after 2 to 3 years. In normal or low turnover osteoporosis bone mass is stabilized but does not increase. However, the long-term effect of bisphosphonates on bone strength is not known.

摘要

双膦酸盐是治疗骨质疏松症颇具吸引力的抗骨吸收药物。日本唯一可用的化合物是第一代双膦酸盐依替膦酸二钠。依替膦酸二钠吸附于羟基磷灰石晶体表面,可减缓骨矿化并抑制骨吸收。在这两种作用之间它具有较窄的治疗窗,因此长期连续给药不可行。间歇性使用依替膦酸二钠对骨量有积极影响。但反应与基线时的骨转换率直接相关。在高转换型骨质疏松症中,骨量可能会增加,但在2至3年后会达到平台期。在正常或低转换型骨质疏松症中,骨量会稳定但不会增加。然而,双膦酸盐对骨强度的长期影响尚不清楚。

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