Moro-Alvarez María J, Díaz-Curiel Manuel
Servicio de Medicina Interna, Hospital Central Cruz Roja, Madrid, España.
Clin Interv Aging. 2008;3(2):227-32. doi: 10.2147/cia.s2502.
Postmenopausal osteoporosis increases susceptibility to low-trauma fractures due to reduced bone volume and microarchitectural deterioration. Daily nitrogen-containing bisphosphonates have shown antifracture efficacy in many studies and are the most commonly prescribed treatment for women with postmenopausal osteoporosis. However, optimal efficacy is often not achieved due to poor patient adherence to medication. Current dosing schedules are often inconvenient or impractical for patients. Poor adherence increases risk of fracture, which itself increases morbidity, healthcare costs and, potentially, mortality. Although weekly rather than daily dosing of bisphosphonates has improved adherence, significant problems remain. Efforts to reduce dosing frequency as a possible means for further improving adherence (compliance and persistence), and therefore treatment outcomes, are ongoing. Risedronate, a third-generation bisphosphonate, has been shown in multiple clinical trials to reduce fracture risk and improve bone mineral density in postmenopausal women with osteoporosis. Risedronate has a specific structure and set of characteristics that enable less frequent dosing. This paper reviews the structure of risedronate, and how this translates into high antiresorptive potency, favorable bone binding, persistence in bone, and good tolerability that permits less frequent dosing. The paper also reviews the clinical evidence for risedronate, demonstrating the viability of less frequent dosing, with its potential benefits for patient convenience and adherence to therapy. Two equivalence or non-inferiority bridging studies have demonstrated the option of novel risedronate dosing regimens. These studies are reviewed to demonstrate the efficacy and safety of two different monthly regimens of risedronate in the treatment of postmenopausal osteoporosis: 75 mg on 2 consecutive days a month and 150 mg once a month. Data for oral risedronate 150 mg once a month are limited to 1 year's treatment duration. In previous clinical trials, patients receiving risedronate 5 mg daily have been followed for up to 7 years, with no evidence of loss of effectiveness. Risedronate 150 mg once a month has a comparable efficacy and safety to daily doses in the treatment of postmenopausal osteoporosis. These additional treatment options with risedronate provide easier dosing alternatives for patients.
绝经后骨质疏松症会因骨量减少和微结构恶化而增加低创伤骨折的易感性。在许多研究中，每日服用含氮双膦酸盐已显示出抗骨折疗效，并且是绝经后骨质疏松症女性最常用的处方治疗方法。然而，由于患者对药物的依从性差，往往无法达到最佳疗效。目前的给药方案对患者来说通常不方便或不实用。依从性差会增加骨折风险，而骨折本身又会增加发病率、医疗成本，并可能增加死亡率。尽管双膦酸盐每周给药而非每日给药提高了依从性，但仍存在重大问题。作为进一步提高依从性（依从性和持续性）从而改善治疗效果的一种可能手段，减少给药频率的努力正在进行中。利塞膦酸钠是一种第三代双膦酸盐，在多项临床试验中已显示可降低绝经后骨质疏松症女性的骨折风险并提高骨密度。利塞膦酸钠具有特定的结构和一系列特性，使得给药频率可以更低。本文综述了利塞膦酸钠的结构，以及这如何转化为高抗吸收效力、良好的骨结合能力、在骨中的持久性以及允许更低给药频率的良好耐受性。本文还综述了利塞膦酸钠的临床证据，证明了更低给药频率的可行性及其对患者便利性和治疗依从性的潜在益处。两项等效性或非劣效性桥接研究证明了新型利塞膦酸钠给药方案的选择。对这些研究进行了综述，以证明利塞膦酸钠两种不同的每月给药方案在治疗绝经后骨质疏松症方面的疗效和安全性：每月连续2天服用75毫克和每月服用1次150毫克。口服利塞膦酸钠每月150毫克的数据仅限于1年的治疗持续时间。在先前的临床试验中，接受每日5毫克利塞膦酸钠治疗的患者已随访长达7年，没有疗效丧失的证据。利塞膦酸钠每月150毫克在治疗绝经后骨质疏松症方面的疗效和安全性与每日剂量相当。利塞膦酸钠的这些额外治疗选择为患者提供了更简便的给药替代方案。
