6种抗癌药对奥丹西酮在原发性肺癌患者体内药物动力学的影响

目的 研究 6种抗癌剂对奥丹西酮药动学的影响。方法 奥丹西酮的药动学在 21例分别应用 甲氨蝶呤、5-氟尿嘧啶 、环已亚硝脲、环磷酰胺和长春新碱 、顺氯氨铂的原发性肺癌患者中进行 观察, 化疗前和化疗同时服用奥丹西酮, 其血浆浓度采用反相高效液相色谱法测定。数据处理采 用 PKBP-N 1 程序。结果 奥丹西酮吸收快, 并符合二房室模型, 除单/大剂量冲击疗法, 持续应 用抗癌药物均使其药动学参数发生明显变化, T_1/2β 延长约 1h, T_1/2α 发生不规则变化, C_max 和 AUC 也明显升高, 但 T_max 和 T_1/2ka 长期用药将发生体内蓄积。结论 临床应用奥丹西酮防治化 疗所致胃肠道反应时, 应据患者条件和化疗方案调整给药。

Effects of anticarcinogents on ondansetron pharmacokinetics in primary lung carcinoma patients

Aim To research the effects of anticarcinogens on the pharmacokinetics of on-dansetron. Methods The pharmacokinetics of ondansetron was studied in 21 cases of primary lung carcinoma treated with methotrexate, 5-fluorouracil, lomustine, cyclophosphamide plus vincristine, and cis-platin. Before and within chemotherapy, ondansetron concentrations in plasma were determined by a reversed-phase high performance liquid chromatography. The data obtained were fitted with PKBP-N1 pharmacokinetic program. Results The plasma drug concentration-time course conformed to a two-compartment open model with a rapid absorption both before and after chemotherapy. Because methotrexate and lomustine were taken in single/large dose schedule, they did not cause the pharmacokinetic parameters of ondansetron to change markedly, but T_1/2β was prolonged for about 0.5h. Other three chemother apiescaused the parametersof ondansetron to changemarkedly, except T_1/2ka and T_max, T_1/2β was prolonged for 1h T_1/2α hada irregular change, and C_max and AUC were remarkably increased.But ondansetronwas stored up in patient's body after taken with multi-dose.Conclusion The test points out that regulating rationaly medicine plan is necessary when ondansetron is used within sustained chemotherapy.