目的探讨大剂量甲氨碟呤的药代动力对白血病患儿的影响。方法 2008年1月至2011年1月收治的急性淋巴细胞白血病164例分为标准危险组65例,高度危险组99例,观察血药浓度及不良反应。结果两组病例均于用药开始后24 h、44 h和68 h监测血清甲氨碟呤浓度及甲酰四氢叶酸钙解救单位累积剂量比较P<0.05,标准危险组不良反应发生45例,发生率69.23%;高度危险组不良反应99例,发生率100%;经统计学分析,P<0.05,差异有显著性。结论通过对甲氨碟呤药代动力(血药浓度)监测,可以掌握甲氨碟呤在白血病患儿治疗中血药浓度进行调控剂量,使临床治疗效果达到最大化;并且能够及时调整甲酰四氢叶酸钙解救剂量及次数,使得不良反应发生率降至最低,确保临床用药有效性及安全性。 Objective To investigate the effect of high dose methotrexate pharmacokinetics on children with leukemia. Methods 164 patients with acute lymphoblastic leukemia from January 2008 to January 2011 were divided into standard risk group (n = 65) and high risk group (n = 99). The blood concentration and adverse reactions were observed. Results The serum concentrations of methotrexate and the cumulative doses of leucovorin rescue units at 24 h, 44 h and 68 h after the start of treatment were compared in both groups (P <0.05). Adverse reactions occurred in 45 patients in the standard risk group Rate of 69.23%; 99 cases of high risk group of adverse reactions, the incidence of 100%; by statistical analysis, P <0.05, the difference was significant. Conclusion By monitoring the pharmacokinetics of methotrexate (plasma concentration), we can control the dose of methotrexate in the treatment of children with leukemia, so as to maximize the effect of clinical treatment; and the ability to timely adjust formyl Calcium leucovorin rescue dose and frequency, making the incidence of adverse reactions to a minimum, to ensure the effectiveness and safety of clinical medication.