Hamdy Ronald C
Quillen Chair of Geriatrics and Gerontology, Quillen College of Medicine, East Tennessee State University, Box 70429, Johnson City, TN 37614, USA.
Drug Des Devel Ther. 2010 Nov 18;4:321-35. doi: 10.2147/DDDT.S6287.
The availability of a once-a-year zoledronic acid infusion heralds a new era in the management of osteoporosis. It virtually eliminates the problem of poor compliance with orally administered bisphosphonates and, because it bypasses the gastrointestinal tract, it is not associated with gastrointestinal side effects. Zoledronic acid is effective for the treatment and prevention of postmenopausal osteoporosis, and for the treatment of osteoporosis in men, and glucocorticoid-induced osteoporosis. When administered within three months of a hip fracture, it reduces mortality and the risk of subsequent fractures. It is remarkably free of serious adverse effects. After administration of the intravenous infusion, about 18% of bisphosphonate-naïve patients experience an acute-phase reaction, including low-grade temperature, aches, and pains. This is reduced to about 9% in those who have been treated with oral bisphosphonates, and is further reduced by the concomitant and subsequent administration of acetaminophen. The likelihood and magnitude of the acute-phase reaction is less after the second infusion. Other adverse effects are similar to those encountered with other bisphosphonates. Because it is mostly excreted by the kidneys, zoledronic acid should not be administered to patients with a creatinine clearance less than 35 mL/min. It should not be administered to patients with hypocalcemia.
每年一次的唑来膦酸静脉输注为骨质疏松症的治疗开创了一个新时代。它几乎消除了口服双膦酸盐类药物时依从性差的问题，而且由于它绕过胃肠道，所以不会产生胃肠道副作用。唑来膦酸对绝经后骨质疏松症的治疗和预防、男性骨质疏松症以及糖皮质激素诱导的骨质疏松症均有效。在髋部骨折后三个月内使用，可降低死亡率和后续骨折风险。它几乎没有严重的不良反应。静脉输注后，约18%未使用过双膦酸盐类药物的患者会出现急性期反应，包括低热、疼痛。在曾接受口服双膦酸盐类药物治疗的患者中，这一比例降至约9%，而对乙酰氨基酚的同时使用及后续使用可进一步降低该比例。第二次输注后急性期反应的可能性和严重程度会降低。其他不良反应与其他双膦酸盐类药物相似。由于唑来膦酸主要经肾脏排泄，肌酐清除率低于35 mL/min的患者不应使用。低钙血症患者也不应使用。
