Dooley M, Balfour J A
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 1999 Jan;57(1):101-8; discussion 109-10. doi: 10.2165/00003495-199957010-00011.
Ibandronate (ibandronic acid) is a third generation bisphosphonate which inhibits hone resorption in human and animal studies. It also inhibits bone formation only at high doses (10 microg/kg/day) in animal studies. In animal models, ibandronate was more potent than etidronate, clodronate, pamidronate and alendronate and equivalent in potency or more potent than risedronate in inhibiting induced hypercalcaemia and bone resorption. In clinical studies, single-dose ibandronate (0.2 to 6 mg intravenously) significantly reduced albumin-corrected serum calcium levels and urinary markers of bone resorption in patients with hypercalcaemia of malignancy, and in those with bone metastases. Serum calcium levels were normalised in 50 and 67% of ibandronate 2 mg recipients and in about 76% of 4 mg recipients. In postmenopausal women with osteoporosis or osteopenia. ibandronate (0.5 to 5 mg/day orally or 0.5 to 2 mg every 3 months intravenously) dose-dependently increased bone mineral density, with parallel reductions in the biochemical markers of bone turnover. In preliminary studies in patients with Paget's disease a single intravenous ibandronate dose (2mg) decreased serum alkaline phosphatase levels and urinary markers of bone turnover. Adverse events associated with the use of ibandronate in the management of hypercalcaemia of malignancy include increased body temperature, hypocalcaemia and hypophosphataemia. Less commonly, flu-like symptoms and gastrointestinal intolerance may occur.
伊班膦酸盐(伊班膦酸)是第三代双膦酸盐,在人体和动物研究中可抑制骨吸收。在动物研究中,仅在高剂量(10微克/千克/天)时它才抑制骨形成。在动物模型中,伊班膦酸盐在抑制诱导的高钙血症和骨吸收方面比依替膦酸盐、氯膦酸盐、帕米膦酸盐和阿仑膦酸盐更有效,并且在效力上与利塞膦酸盐相当或更有效。在临床研究中,单剂量伊班膦酸盐(静脉注射0.2至6毫克)可显著降低恶性肿瘤高钙血症患者以及骨转移患者经白蛋白校正的血清钙水平和骨吸收的尿标志物。接受2毫克伊班膦酸盐治疗的患者中,50%和67%的患者血清钙水平恢复正常,接受4毫克治疗的患者中约76%恢复正常。在患有骨质疏松症或骨质减少的绝经后女性中,伊班膦酸盐(口服0.5至5毫克/天或每3个月静脉注射0.5至2毫克)剂量依赖性地增加骨矿物质密度,同时骨转换的生化标志物平行降低。在佩吉特病患者的初步研究中,单次静脉注射伊班膦酸盐剂量(2毫克)可降低血清碱性磷酸酶水平和骨转换的尿标志物。在治疗恶性肿瘤高钙血症中使用伊班膦酸盐相关的不良事件包括体温升高、低钙血症和低磷血症。较少见的情况是,可能会出现流感样症状和胃肠道不耐受。