White Ngaire J, Perry Caroline M
Adis International Inc., Yardley, Pennsylvania, 19067, USA.
Treat Endocrinol. 2003;2(6):415-20; discussion 421. doi: 10.2165/00024677-200302060-00005.
Risedronate (risedronic acid), an orally administered pyridinyl bisphosphonate, inhibits osteoclast-mediated resorption of bone and modulates bone metabolism in women with postmenopausal osteoporosis. The long terminal exponential half-life of risedronate (480 hours) has led to the development of a 35mg tablet for once-a-week administration. The beneficial effects of risedronate 35mg once a week on total hip, femoral neck and trochanter bone mineral density (BMD) at 12 months were similar to those of risedronate 5mg once daily. Risedronate 35mg once a week was as effective as risedronate 5mg once daily in improving lumbar spine BMD in a randomized, double-blind, multicenter trial of 1456 women with postmenopausal osteoporosis. Mean percentage increases in BMD from baseline at 12 months were 3.94% and 4.25% in the 35mg and 50mg once-a-week dose groups, compared with 4% in the 5mg once-daily dose group. The differences between the once-a-week doses and the once-daily dose met the predetermined criterion for non-inferiority. An historical analysis suggested that risedronate 35mg once a week reduced the incidence of vertebral fracture significantly more than placebo. The tolerability profile (including the incidence of upper gastrointestinal adverse events) of risedronate 35mg once a week in women with postmenopausal osteoporosis, was similar to that of risedronate 5mg once daily.
利塞膦酸盐(利塞膦酸)是一种口服的吡啶基双膦酸盐,可抑制破骨细胞介导的骨吸收,并调节绝经后骨质疏松症女性的骨代谢。利塞膦酸盐的长终末指数半衰期(480小时)促使研发出了一种每周服用一次的35毫克片剂。每周一次服用35毫克利塞膦酸盐对全髋、股骨颈和大转子骨矿物质密度(BMD)在12个月时的有益作用与每日一次服用5毫克利塞膦酸盐相似。在一项针对1456名绝经后骨质疏松症女性的随机、双盲、多中心试验中,每周一次服用35毫克利塞膦酸盐在改善腰椎BMD方面与每日一次服用5毫克利塞膦酸盐效果相当。每周一次服用35毫克和50毫克剂量组在12个月时BMD较基线的平均百分比增加分别为3.94%和4.25%,而每日一次服用5毫克剂量组为4%。每周一次剂量组与每日一次剂量组之间的差异符合预先设定的非劣效性标准。一项历史分析表明,每周一次服用35毫克利塞膦酸盐比安慰剂显著降低了椎体骨折的发生率。绝经后骨质疏松症女性每周一次服用35毫克利塞膦酸盐的耐受性情况(包括上消化道不良事件的发生率)与每日一次服用5毫克利塞膦酸盐相似。