Catalina Pointe Clinical Research, Inc., University of Arizona School of Medicine, 5501 N. Oracle Road, Suite 161, Tucson, AZ 85704, USA.
Clin Rheumatol. 2010 Oct;29(10):1079-84. doi: 10.1007/s10067-010-1486-3. Epub 2010 Jun 11.
Bisphosphonates are the current standard of care for treatment of osteoporosis. However, oral bisphosphonates are associated with complicated dosing regimens because of poor absorption and have the potential for upper gastrointestinal (GI) tract irritation, resulting in poor adherence and persistence. Zoledronic acid (ZOL) 5 mg, a once-yearly intravenous bisphosphonate, is approved for treatment and prevention of postmenopausal osteoporosis, increasing bone mass in men with osteoporosis, and treatment and prevention of glucocorticoid-induced osteoporosis. Because it is administered as an infusion, ZOL ensures adherence and persistence over the entire 12-month dosing interval and bypasses the GI absorption/irritation problems associated with oral bisphosphonates. The objective of this study was to review the safety and efficacy of 5 mg ZOL and its potential for improving patient compliance. Published reports dating back to 2001 were reviewed, with emphasis on osteoporosis treatment. In the HORIZON-Pivotal Fracture Trial, annual infusions of 5 mg ZOL produced significant reductions in risk of morphometric vertebral fractures (70%) and hip fractures (41%) vs placebo over 3 years in postmenopausal women with osteoporosis. In the HORIZON-Recurrent Fracture Trial, an annual infusion of 5 mg ZOL after repair of a recent low-trauma hip fracture was associated with significant reductions in risk for new clinical fractures (35%) vs placebo. In men with osteoporosis, an annual treatment of ZOL over 2 years increased lumbar spine bone mineral density (BMD) by 6% compared with baseline. In patients starting or continuing treatment with chronic glucocorticoids, ZOL resulted in significantly greater increases in lumbar spine BMD over 1 year than an oral bisphosphonate. In postmenopausal women with osteopenia, a single infusion of ZOL over a 2-year period produced significantly greater gains in lumbar spine and hip BMD than placebo. ZOL is generally safe and well tolerated. Five milligrams of ZOL has the potential to improve compliance with osteoporosis therapy and, consequently, to reduce fracture risk in clinical practice.
双膦酸盐类药物是目前治疗骨质疏松症的标准药物。然而，由于口服双膦酸盐类药物吸收不良，且有可能对上消化道（GI）造成刺激，导致患者顺应性和持续性较差，因此其用药方案较为复杂。唑来膦酸（ZOL）5mg 是一种每年一次的静脉用双膦酸盐类药物，用于治疗和预防绝经后骨质疏松症、增加男性骨质疏松症患者的骨量、治疗和预防糖皮质激素诱导的骨质疏松症。由于其为输注用药，因此在整个 12 个月的用药间隔内可确保患者的顺应性和持续性，并避免了与口服双膦酸盐类药物相关的 GI 吸收/刺激问题。本研究旨在综述 5mg ZOL 的安全性和有效性及其改善患者顺应性的潜力。检索了 2001 年以来发表的相关报告，重点关注骨质疏松症的治疗。在 HORIZON-Pivotal Fracture 试验中，与安慰剂相比，接受骨质疏松症治疗的绝经后妇女在 3 年内，每年接受 5mg ZOL 静脉输注可显著降低椎体骨折（70%）和髋部骨折（41%）的风险。在 HORIZON-Recurrent Fracture 试验中，在近期低创伤性髋部骨折修复后，每年接受 5mg ZOL 输注治疗与安慰剂相比，新发临床骨折风险显著降低（35%）。在骨质疏松症男性患者中，2 年期间每年接受 ZOL 治疗可使腰椎骨密度（BMD）增加 6%，与基线相比。在开始或继续接受慢性糖皮质激素治疗的患者中，与口服双膦酸盐类药物相比，ZOL 可使腰椎 BMD 在 1 年内显著增加。在患有骨量减少的绝经后妇女中，2 年期间单次输注 ZOL 可使腰椎和髋部 BMD 显著增加，与安慰剂相比。ZOL 一般安全且耐受性良好。5mg ZOL 具有提高骨质疏松症治疗顺应性的潜力，因此可降低临床实践中的骨折风险。
