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利塞膦酸盐(risedronate商品名Actonel)属于吡啶二磷酸盐,已获美国FDA批准用于口服治疗paget骨病。该骨病的特征包括过度的骨吸收、骨畸形、骨重建被破坏、结构脆弱。在欧洲和北美,55岁以上的人,3％患paget骨病。 作用机理 利塞膦酸盐能抑制破骨活性,降低骨倒转和吸收。在推荐剂量内,利塞膦酸盐不干扰骨矿化。 药动学 利塞膦酸盐和其它二磷酸盐一样,很难在胃肠道内吸收,禁食状态下吸收很差;不禁食时,吸收更差。禁食时的吸收率低于10％。被吸收的药物主要分布在骨组
Risedronate (trade name Actonel) is pyridinium diphosphate and has been approved by the US FDA for the oral treatment of Paget’s bone disease. The features of this bone disease include excessive bone resorption, bone deformities, destruction of bone remodeling, and structural fragility. In Europe and North America, 3% of people over 55 suffer from Paget’s bone disease. Mechanism of action Risedronate can inhibit osteoclast activity and reduce bone turnover and absorption. Risedronate does not interfere with bone mineralization within the recommended dose. Pharmacokinetics Risedronate, like other bisphosphonates, is difficult to absorb in the gastrointestinal tract and is poorly absorbed in the fasting state; absorption is even worse when it is not fasted. Absorption rate during fasting is less than 10%. Absorbed drugs are mainly distributed in the bone group