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[氯膦酸在矿物质代谢疾病中的应用:2000年的现状]

[Use of clodronic acid in mineral metabolism conditions: state of the art in 2000].

作者信息

Brandi M L

机构信息

Dipartimento di Medicina Interna, Università degli Studi, Firenze, Italy.

出版信息

Minerva Med. 2001 Aug;92(4):251-68.

Abstract

Clodronic acid is a non-aminate bisphosphonate capable of inhibiting bone resorption. Pharmacological and clinical trials have shown the efficacy of clodronic acid in the treatment of post-menopausal osteoporosis and in all conditions of excess bone resorption, such as Paget's disease, malignant tumoral hypercalcemia and osteolytic metastases. Clodronic acid is the only bisphosphonate currently on the market available for both oral and parenteral administration. Intramuscular therapy with clodronic acid at a dose of 100 mg/week has shown significant effects on bone mineral density after 6 months treatment in patients with postmenopausal osteoporosis and these effects were maintained 3 years after the start of treatment. Increased bone mass is associated with a reduced risk of the onset of vertebral fractures. In a recent three-year study a significant increase was observed in bone mineral density associated with a 46% reduction in the incidence of vertebral fractures. The reduction in bone pain after parenteral treatment with clodronic acid is an important added value in the use of this molecule in osteopenic pathologies. Moreover the costs of parenteral clodronic acid treatment is certainly competitive compared to other drugs. Oral and parenteral clodronic acid was well tolerated in clinical trials. Gastrointestinal adverse effects were described only with high oral doses. These effects were transient and generally resolved without interrupting the treatment. Clodronic acid is an effective and well tolerated drug able to inhibit bone resorption. The low incidence of undesired effects at a gastroenteric level, the possibility of formulas for parenteral administration, the antalgic effect and low costs make clodronic acid an extremely interesting molecule for the prevention and treatment of postmenopausal osteoporosis and all conditions of excessive bone resorption, such as Paget's disease, malignant tumoral hypercalcemia, osteolytic metastasis and hyperparathyroidism.

摘要

氯膦酸是一种能够抑制骨吸收的非氨基双膦酸盐。药理学和临床试验已表明氯膦酸在治疗绝经后骨质疏松症以及所有骨吸收过多的病症中具有疗效,如佩吉特病、恶性肿瘤性高钙血症和溶骨性转移。氯膦酸是目前市场上唯一可用于口服和肠胃外给药的双膦酸盐。对于绝经后骨质疏松症患者,每周100mg剂量的氯膦酸肌肉注射治疗6个月后对骨矿物质密度显示出显著效果,且这些效果在治疗开始3年后仍得以维持。骨量增加与椎体骨折发病风险降低相关。在最近一项为期三年的研究中,观察到骨矿物质密度显著增加,同时椎体骨折发生率降低了46%。氯膦酸肠胃外治疗后骨痛减轻是该分子用于骨质减少性疾病治疗的一个重要附加价值。此外,与其他药物相比,氯膦酸肠胃外治疗的成本肯定具有竞争力。在临床试验中,口服和肠胃外使用氯膦酸耐受性良好。仅在高口服剂量时才描述有胃肠道不良反应。这些反应是短暂的,通常在不中断治疗的情况下即可缓解。氯膦酸是一种有效且耐受性良好的药物,能够抑制骨吸收。在胃肠道水平不良反应发生率低、有肠胃外给药剂型、有止痛效果且成本低,这些使得氯膦酸成为预防和治疗绝经后骨质疏松症以及所有骨吸收过多病症(如佩吉特病、恶性肿瘤性高钙血症、溶骨性转移和甲状旁腺功能亢进)的极具吸引力的分子。

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