Fitton A, McTavish D
Adis Drug Information Services, Auckland, New Zealand.
Drugs. 1991 Feb;41(2):289-318. doi: 10.2165/00003495-199141020-00009.
Pamidronate [aminohydroxypropylidene diphosphonate disodium (APD), disodium pamidronate] is an orally and intravenously active amino-substituted bisphosphonate which produces potent and specific inhibition of bone resorption at doses devoid of any significant detrimental effect on bone growth and mineralisation. Clinical trials indicate that pamidronate is effective in a variety of conditions characterised by pathologically enhanced bone turnover, including Paget's disease, hypercalcaemia of malignancy, osteolytic bone metastasis, steroid-induced osteoporosis and idiopathic osteoporosis. Pamidronate is highly effective in restoring normocalcaemia in patients with hypercalcaemia of malignancy associated with bone metastases but, in common with other bisphosphonates, is marginally less effective against humoral hypercalcaemia of malignancy. Comparative studies in this area have suggested that, at therapeutic doses, pamidronate has a more pronounced calcium-lowering action than etidronate (etidronic acid) and clodronate (clodronic acid) and provides a longer period of normocalcaemic remission. In Paget's disease arrest and, in some patients, reversal of the progression of osteolytic lesions by pamidronate is associated with a sustained reduction in bone pain, improved mobility and a possible reduced risk of bone fracture. In patients with osteolytic bone metastasis pamidronate reduces skeletal morbidity and slows the progression of metastatic bone destruction. Long term use of low-dose pamidronate in conjunction with conventional antiosteoporotic therapy may halt bone loss in steroid-induced and idiopathic osteoporosis. Pamidronate appears to represent a valuable addition to the drugs currently available for the treatment of symptomatic Paget's disease and cancer-associated hypercalcaemia, and shows promise in the treatment of osteolytic bone metastasis and osteoporosis.
帕米膦酸盐[氨基羟丙基亚丙基二膦酸二钠(APD),帕米膦酸二钠]是一种口服和静脉注射均有效的氨基取代双膦酸盐,在剂量对骨生长和矿化无任何明显有害影响的情况下,能产生强大而特异的骨吸收抑制作用。临床试验表明,帕米膦酸盐对多种以病理性骨转换增强为特征的病症有效,包括佩吉特病、恶性肿瘤高钙血症、溶骨性骨转移、类固醇诱导的骨质疏松症和特发性骨质疏松症。帕米膦酸盐在恢复与骨转移相关的恶性肿瘤高钙血症患者的血钙正常方面非常有效,但与其他双膦酸盐一样,对恶性肿瘤体液性高钙血症的疗效略差。该领域的比较研究表明,在治疗剂量下,帕米膦酸盐比依替膦酸盐(依替膦酸)和氯膦酸盐(氯膦酸)具有更显著的降钙作用,并能提供更长时间的血钙正常缓解期。在佩吉特病中,帕米膦酸盐使溶骨性病变停止进展,在一些患者中使其逆转,这与骨痛持续减轻、活动能力改善以及骨折风险可能降低有关。在溶骨性骨转移患者中,帕米膦酸盐可降低骨骼发病率并减缓转移性骨破坏的进展。长期低剂量使用帕米膦酸盐联合传统抗骨质疏松治疗可能会阻止类固醇诱导的和特发性骨质疏松症中的骨质流失。帕米膦酸盐似乎是目前可用于治疗有症状的佩吉特病和癌症相关高钙血症的药物的有价值补充,并且在治疗溶骨性骨转移和骨质疏松症方面显示出前景。