Sparidans R W, Twiss I M, Talbot S
Department of Clinical Pharmacy and Toxicology, Leiden University Medical Centre, The Netherlands.
Pharm World Sci. 1998 Oct;20(5):206-13. doi: 10.1023/a:1008626026484.
Bisphosphonates are a class of drugs which are strongly attracted to the bone where they influence the calcium metabolism, mainly by inhibition of the osteoclast-mediated bone resorption. This property makes these compounds suited for the treatment of several diseases of the bone. In Paget's disease, several bisphosphonates can reduce bone pain and decrease the bone turnover 60-70%. Cyclical oral etidronate and daily oral alendronate both proved to reduce the vertebral fracture rate for postmenopausal osteoporotic woman, while most investigated bisphosphonates can increase spinal bone mass in osteoporosis. Bisphosphonates can help lowering serum calcium and reverse skeletal complications in malignancy mediated bone diseases. Oral and intravenous administration of therapeutic doses is relatively safe. In general, gastrointestinal disturbances are described most often and the oldest, least potent, bisphosphonate etidronate can induce osteomalacia. The various characteristics of bisphosphonates: physicochemical, biological, therapeutic and toxicological, vary greatly depending on the structure of the individual bisphosphonate. Even small changes in the structure can lead to enormous differences in potency. Overall, this class of drugs offers several prospects for the future.
双膦酸盐是一类药物，它们对骨骼具有强烈的亲和力，在骨骼中主要通过抑制破骨细胞介导的骨吸收来影响钙代谢。这一特性使这些化合物适用于多种骨骼疾病的治疗。在佩吉特病中，几种双膦酸盐可减轻骨痛并使骨转换降低60% - 70%。周期性口服依替膦酸和每日口服阿仑膦酸钠均已证明可降低绝经后骨质疏松女性的椎体骨折率，而大多数研究的双膦酸盐可增加骨质疏松症患者的脊柱骨量。双膦酸盐有助于降低血清钙水平，并逆转恶性肿瘤介导的骨病中的骨骼并发症。口服和静脉给予治疗剂量相对安全。一般来说，胃肠道不适最为常见，而最古老、效力最低的双膦酸盐依替膦酸可诱发骨软化症。双膦酸盐的各种特性，如物理化学、生物学、治疗和毒理学特性，因个体双膦酸盐的结构不同而有很大差异。即使结构上的微小变化也可能导致效力上的巨大差异。总体而言，这类药物为未来提供了多种前景。
