利培酮的血药浓度与临床效应的关系

目的 观察利培酮治疗精神分裂症时的血药浓度及其与疗效及不良反应之间的关系。方法 共纳入31例精神分裂症患者,其中男性17列,女性14列,平均年龄31.00±8.98岁。在治疗前及治疗后1周,2周、4周.6周及8周评定PANSS、CGI、TESS及ESRS。采用HPLC方法测定治疗后4周及8周时利培酮及其代谢产物9—羟利培酮的血药浓度。结果 利培酮治疗精神分裂症疗效肯定,不良反应较少,部分患者出现轻度的EPS。服用固定剂量利培酮(4mg/d)治疗8周时利培酮的血药浓度为41.46±17.36nmol/L,9-羟利培酮的浓度为60.88±42.73nmol/L。利培酮及代谢产物的总浓度与疗效有关,利培酮浓度与EPS有关。结论 利培酮是一种有效的抗精神病药,服用治疗剂量时,利培酮及其代谢产物的总浓度与疗效有关,而利培酮的血药浓度与EPS有关,故检测利培酮及其代谢产物9-羟利培酮的药物浓度对指导临床用药具有重要意义。

The relationships between plasma concentration of risperidone and clinical effects

Objective: To observe the relationships between drug plasma concentration of risperidone and 9-OH-risperidone and its clinical effects and adverse effects in schizophrenic patients. Methods: 31 schizophrenic patients were enrolled in the study. PANSS, CGI, TESS and ESRS were evaluated before and 1,2,4,6,8 week after the treatment. The drug concentration of risperidone and 9-OH-risperidone were detected by using HPLC at week 4, 8 after the treatment. Results: Risperidone was an effective antipsychotic. Some patients could experience mild EPS. The total concentration of risperidone and 9-OH-risperidone was significantly correlated to the clinical effects while the concentration of risperidone was significantly correlated to EPS. Conclusion: Risperidone is an effective antipsychotic. The drug plasma concentration is related to the clinical effects and EPS. It is useful to monitor regularly the plasma concentration of risperidone and its metabolites in the treatment of schizophrenia.