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Drugs. 2018 Oct;78(15):1605-1613. doi: 10.1007/s40265-018-0991-6.
Sodium zirconium cyclosilicate (Lokelma™) [hereafter referred to as SZC] is a non-absorbed, non-polymer zirconium silicate compound that preferentially exchanges hydrogen and sodium for potassium and ammonium ions in the gastrointestinal tract (GIT), thereby increasing faecal potassium excretion and lowering serum potassium levels. It is available as a powder for oral suspension (in water) and is approved in the EU and the USA for the treatment of hyperkalaemia in adults. In two multinational, phase III studies in adults with hyperkalaemia, SZC 10 g three times daily lowered serum potassium levels to within the normal range (3.5-5.0 mmol/L) during the first 48 h of treatment, and SZC 5 and 10 g once daily maintained normokalaemia over ≤ 28 days' therapy. These beneficial effects were consistent across all patient subgroups (e.g. chronic kidney disease, diabetes, heart failure, concomitant use of RAAS inhibitor therapy), and appeared to be maintained over the longer term (≤ 12 months). SZC was generally well tolerated in adults with hyperkalaemia. Its tolerability profile was generally similar to that seen with placebo over ≤ 28 day, and its safety profile appeared to remain consistent over the longer term (≤ 12 months). Moreover, the incidence of hypokalemia was low. Current evidence indicates that SZC is a promising therapy for the management of hyperkalaemia in adults.
硅酸锆酸钠(Lokelma™)[以下简称 SZC]是一种不被吸收的非聚合硅酸锆化合物,它在胃肠道(GI)中优先将氢和钠与钾和铵离子交换,从而增加粪便中钾的排泄并降低血清钾水平。它以粉末形式用于口服混悬液(在水中),在欧盟和美国被批准用于治疗成人高钾血症。在两项针对成人高钾血症的多中心 III 期研究中,SZC 每日三次 10g 可在治疗的前 48 小时内将血清钾水平降低至正常范围(3.5-5.0mmol/L),而每日一次 5g 和 10g 可维持≤28 天的正常血钾水平。这些有益的效果在所有患者亚组中都是一致的(例如,慢性肾脏病、糖尿病、心力衰竭、同时使用 RAAS 抑制剂治疗),并且似乎在较长时间内(≤12 个月)保持稳定。SZC 在成人高钾血症中通常具有良好的耐受性。其耐受性与安慰剂在≤28 天内的情况相似,其安全性在较长时间内(≤12 个月)似乎保持一致。此外,低钾血症的发生率较低。目前的证据表明,SZC 是治疗成人高钾血症的一种很有前途的治疗方法。