Giljević Zlatko, Vlak Tonko
Zavod za endokrinologiju i bolesti metabolizma, Klinika za unutarnje bolesti Klinicki bolnicki centar Zagreb, Kispatićeva 12, 10000 Zagreb.
Reumatizam. 2006;53(2):66-71.
Risedronate (Actonel 35 mg), which was promoted in Croatia a few months ago, is the latest (III) generation of bisphosphonates, the most efficient anti-resorption drugs that inhibit osteoclast-mediated bone resorption and change the bone metabolism. The effect of risedronate is 10 times stronger than that of alendronate, and 10.000 times stronger than that of etidronate. The bone turnover is reduced while the osteoblast activity and bone mineralisation are preserved. Decreases in biochemical markers of bone turnover were observed as soon as within 1 month and reached a maximum in 3-6 months of Actonel 35 mg application once a week or 5 mg a day. Several major international, randomised and placebo controlled clinical studies (VERT-NA, VERT-MN, HIP...) on more than 15,000 patients over 3-5 years of therapy have confirmed the speed, efficacy and excellent tolerability of risedronate in treating postmenopausal and corticosteroid-induced osteoporosis. After only 6 months of treatment VERT-NA and VERT-MN have shown a significant reduction in vertebral fracture risk versus control group, radiographically by 62% and clinically by 69% in the first year, which remains significant even after 5 years of treatment (50%) of postmenopausal osteoporosis. All the best properties of bisphosphonates have also been confirmed through a significant reduction in the relative risk of femoral neck fracture over 3 years of treatment by 40%, or by as much as 60% in female patients with osteoporosis and prevalent vertebral fracture, compared with controls. With risedronate we can achieve a quick and significant reduction in vertebral fracture risk in postmenopausal women (65%), especially among a high-risk population such as patients on long-term glucocorticoid therapy (70%) in the very first year of treatment. Prevention and treatment of glucocorticoid-induced osteoporosis is recommended in the administration of 27,5 mg of prednisone or prednisone equivalent in a duration longer than 3 months, irrespective of age or gender. Tolerability and safety of risedronate administration in osteoporosis is very good, almost the same as in the control group, although patients with earlier described or ongoing gastrointestinal troubles were also included. The incidence of endoscopically confirmed gastric ulcer in treatment with alendronate is significantly higher (13,2%) versus controls than in treatment with risedronate (4,1%). Risedronate is hence the first line of bisphosphonates for the reduction of vertebral and non-vertebral fracture risks in postmenopausal women with osteoporosis or those with a high risk of osteoporosis. It also efficiently prevents bone loss or improves bone density in men and women on a long-term corticosteroid therapy.
利塞膦酸盐（阿屈膦酸35毫克）几个月前在克罗地亚上市，是最新一代（第三代）双膦酸盐药物，是抑制破骨细胞介导的骨吸收并改变骨代谢的最有效的抗吸收药物。利塞膦酸盐的效果比阿仑膦酸钠强10倍，比依替膦酸强10000倍。骨转换减少，而成骨细胞活性和骨矿化得以保留。在每周一次应用阿屈膦酸35毫克或每日应用5毫克的情况下，在应用后1个月内即可观察到骨转换生化标志物下降，并在3至6个月时达到最大降幅。多项针对超过15000名患者进行的为期3至5年的大型国际随机安慰剂对照临床研究（VERT-NA、VERT-MN、HIP等）证实了利塞膦酸盐在治疗绝经后和糖皮质激素诱导的骨质疏松症方面的速度、疗效和极佳的耐受性。仅治疗6个月后，VERT-NA和VERT-MN就显示出与对照组相比，椎体骨折风险显著降低，在第一年，影像学上降低了62%，临床上降低了69%；即使在治疗绝经后骨质疏松症5年后（50%），这一效果仍然显著。双膦酸盐的所有最佳特性也通过治疗3年后股骨颈骨折相对风险显著降低40%得到证实，在患有骨质疏松症和椎体骨折的女性患者中，与对照组相比降低幅度高达60%。使用利塞膦酸盐，我们可以在绝经后女性中迅速且显著地降低椎体骨折风险（65%），尤其是在高危人群中，如长期接受糖皮质激素治疗的患者（在治疗的第一年为70%）。在给予27.5毫克泼尼松或等效泼尼松且疗程超过3个月时，无论年龄或性别，均建议预防和治疗糖皮质激素诱导的骨质疏松症。在骨质疏松症治疗中，利塞膦酸盐的耐受性和安全性非常好，几乎与对照组相同，尽管纳入了先前描述有胃肠道问题或正在出现胃肠道问题的患者。与利塞膦酸盐治疗（4.1%）相比，阿仑膦酸钠治疗中经内镜确诊的胃溃疡发生率显著更高（13.2%）。因此，利塞膦酸盐是用于降低患有骨质疏松症或有骨质疏松症高风险的绝经后女性椎体和非椎体骨折风险的一线双膦酸盐药物。它还能有效预防长期接受糖皮质激素治疗的男性和女性的骨质流失或提高骨密度。
