Adis, Auckland, New Zealand.
Drugs. 2010 Apr 16;70(6):733-59. doi: 10.2165/10481900-000000000-00000.
This is a review of the pharmacology of strontium ranelate (Protelos, Protos, Protaxos, Bivalos, Osseor), and its efficacy and tolerability in the treatment of patients with postmenopausal osteoporosis. Strontium ranelate is a divalent strontium salt of ranelic acid that is capable of increasing bone formation and reducing bone resorption, thereby uncoupling and rebalancing bone turnover in favour of bone formation. The drug is effective in reducing the risk of fractures, including both vertebral and nonvertebral fractures, in patients with postmenopausal osteoporosis, according to data from two large, double-blind, placebo-controlled, multicentre trials of 5 years' duration, and reduced the risk of hip fracture in high-risk patients in a post hoc analysis of one trial. Moreover, data from patients who continued to receive the drug during the 3-year extension phases of these trials indicate that strontium ranelate continues to provide protection against new vertebral fractures and nonvertebral fractures for up to 8 years of therapy. It also improves bone mineral density at numerous sites and both increases markers of bone formation and decreases markers of bone resorption. Strontium ranelate is administered orally as a suspension and is generally well tolerated. The nature of adverse events was generally similar regardless of treatment duration in clinical trials, with the most commonly reported being nausea and diarrhoea over 5 years of treatment, and memory loss and diarrhoea during longer-term treatment. Although an increased risk of venous thromboembolism was associated with strontium ranelate relative to placebo over 5 years of treatment in a pooled analysis of clinical trials, postmarketing data have not confirmed this finding. Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis.
这是一篇关于雷奈酸锶（普罗泰索、普罗特斯、普罗塔克索、比伐洛斯、奥索拉）药理学的综述，以及其在治疗绝经后骨质疏松症患者中的疗效和耐受性。雷奈酸锶是雷奈酸的二价锶盐，能够增加骨形成并减少骨吸收，从而使骨转换脱耦联并重新达到骨形成的平衡。根据两项为期 5 年的大型、双盲、安慰剂对照、多中心试验的数据，该药能够降低绝经后骨质疏松症患者骨折的风险，包括椎体和非椎体骨折，并且在一项试验的事后分析中降低了高危患者髋部骨折的风险。此外，这些试验的 3 年扩展阶段继续接受该药治疗的患者数据表明，雷奈酸锶在长达 8 年的治疗中持续提供对新椎体骨折和非椎体骨折的保护。它还能改善多个部位的骨密度，增加骨形成标志物，减少骨吸收标志物。雷奈酸锶作为混悬剂口服给药，一般耐受性良好。临床试验中无论治疗持续时间如何，不良事件的性质通常相似，最常见的是 5 年治疗期间的恶心和腹泻，以及长期治疗期间的记忆力减退和腹泻。尽管在临床试验的汇总分析中，与安慰剂相比，雷奈酸锶在 5 年的治疗中与静脉血栓栓塞风险增加相关，但上市后数据并未证实这一发现。总的来说，现有临床数据表明，雷奈酸锶是绝经后骨质疏松症一线治疗的一种有效且通常耐受性良好的选择。
