毒理性
在兰瑞肽的预注册研究中，血清酶水平没有显著变化，并且没有临床明显的急性肝损伤的报告。汇总分析报告称，在治疗期间血清ALT、AST或碱性磷酸酶水平没有整体变化，也没有出现具有临床意义的升高。与其它生长抑素类似物一样，长期使用兰瑞肽与胆泥和胆石症的高发生率相关，这可能是由于胆囊收缩性抑制和胆汁分泌减少所致。在长期研究中，20%到33%的使用兰瑞肽治疗的患者出现了胆石症。在某些情况下，会出现有症状的胆囊炎，这可能会伴有血清酶和胆红素的轻度至中度升高。然而，大多数与兰瑞肽相关的胆结石是无症状的。与奥曲肽不同，兰瑞肽和其他长效生长抑素类似物并没有与临床明显的肝损伤病例相关联，这种损伤独立于胆石症或胆泥，尽管它们的使用范围较窄，并且没有用于许多曾用奥曲肽治疗的情况（如门脉高压、静脉曲张出血和先天性高胰岛素血症的婴儿）。
In preregistration studies of lanreotide, serum enzyme levels did not change appreciably and there were no reports of clinically apparent acute liver injury. Pooled analyses reported that there were no overall changes in serum ALT, AST or alkaline phosphatase levels during therapy or instances of clinically meaningful elevations with treatment. Prolonged therapy with lanreotide, as with other somatostatin analogues, was associated with a high rate of biliary sludge and cholelithiasis, probably due to inhibition of gall bladder contractility and decrease in bile secretion. In long term studies, cholelithiasis developed in 20% to 33% of lanreotide treated patients. In some instances, symptomatic cholecystitis occurred which can be accompanied by mild-to-moderate elevations in serum enzymes and bilirubin. However, most lanreotide associated gallstones were asymptomatic. Unlike octreotide, lanreotide and other long acting somatostatin analogues have not been liked to cases of clinically apparent liver injury, independent of cholelithiasis or biliary sludge, although they have had more limited use and have not been used in many of the clinical situations that were treated with octreotide (portal hypertension, variceal hemorrhage and infants with congenital hyperinsulinemia).
来源:LiverTox
