Locatelli Francesco, Dimkovic Nada, Spasovski Goce
Alessandro Manzoni Hospital, Department of Nephrology Dialysis and Renal Transplantation , Via Dell'Eremo 9, Lecco, 23900 , Italy +39 0341 489850 ; +39 0341 489860 ;
Expert Opin Pharmacother. 2014 Jul;15(10):1475-88. doi: 10.1517/14656566.2014.928285.
Hyperphosphataemia is common in chronic kidney disease (CKD), particularly in the late stages and is associated with secondary hyperparathyroidism, abnormal bone mineralisation and increased cardiovascular morbidity/mortality. At present, there is a range of phosphate binders designed to keep serum phosphate at normal or near normal levels. Colestilan is a new binder that offers additional actions that may afford further benefits over simply lowering phosphate.
This paper reviews the pharmacology and clinical data currently available in the use of colestilan to treat hyperphosphataemia in CKD stage 5 patients on dialysis.
Available phosphate binders lower serum phosphorus levels to a clinically relevant extent. The balance between the risks and the potential benefits associated with each agent must be considered when choosing a binder. Calcium-based binders can lead to hypercalcaemia and/or positive calcium balance and cardiovascular calcification. Like sevelamer, colestilan is not absorbed and there is no evidence of any risk of hypercalcaemia. In addition, a significant lowering of low-density lipoprotein-cholesterol, similar to simvastatin, a reduction in plasma uric acid and a reduction in high glycosylated haemoglobin values suggest additional beneficial actions that may convert to reductions in mortality.
高磷血症在慢性肾脏病（CKD）中很常见，尤其是在晚期，并且与继发性甲状旁腺功能亢进、骨矿化异常以及心血管发病率/死亡率增加有关。目前，有一系列旨在将血清磷维持在正常或接近正常水平的磷结合剂。考来替兰是一种新型结合剂，它具有一些额外作用，可能比单纯降低磷带来更多益处。
本文综述了目前使用考来替兰治疗5期CKD透析患者高磷血症的药理学和临床数据。
现有的磷结合剂能将血清磷水平降低至临床相关程度。选择结合剂时必须考虑每种药物相关的风险与潜在益处之间的平衡。钙基结合剂可导致高钙血症和/或正钙平衡以及心血管钙化。与司维拉姆一样，考来替兰不被吸收，且没有证据表明存在高钙血症风险。此外，低密度脂蛋白胆固醇显著降低，类似于辛伐他汀，血浆尿酸降低，糖化血红蛋白值降低，提示可能存在其他有益作用，这可能转化为死亡率降低。
