盐酸伊立替康的不良反应及其预防处理

伊立替康(irinotecan,CPT-11)是喜树碱的半合成衍生物,是选择性拓扑异构酶Ⅰ抑制剂,本品及其体内代谢物SN-38可诱导单链DNA损伤,从而阻断DNA复制,产生细胞毒作用。CPT-11于1998年获FDA批准用于标准化疗方案治疗后转移性结肠直肠癌复发和恶化的二线治疗;于2000年3月获FDA批准联合氟尿嘧啶(5-FU)和亚叶酸钙(CF)用于转移性结肠直肠癌的一线治疗。本品单药有效率在18%左右,联合5-FU和CF的有效率约为50%。CPT-11主要不良反应有迟发性腹泻、恶心、呕吐、中性粒细胞减少症、急性胆碱能综合征等,现就其不良反应的表现类型及预防处理方法进行概述。

The adverse reactions and management of irinotecan

Irinotecan(CPT-11)is a semi-synthetic derivative of camptothecin.It is a potent inhibitor of topoisomerase I.Irinotecan and its activated metabolites SN-38 has demonstrated antitumor activity against metastatic colorectal cancer.The inhibition of DNA topoisomerase I by irinotecan or SN-38 induces single-strand DNA lesions which blocks the DNA replication fork and is responsible for the cytotoxicity.Approved by FDA in 1998 as second-line treatment after the failure of standard therapy for metastatic colorectal cancer;in March 2000 as first-line therapy for metastatic colorectal cancer in combination with 5-FU/CF.The total response rate was 18% in irinotecan alone group and 50% in irinotecan plus 5-FU/CF group.The main adverse effects of irinotecan are delayed diarrhea,nausea,vomiting,neutropenia and cholinergic syndrome.The side effects and management of irinotecan were reviewed in this paper.