利培酮血药浓度测定及其临床应用

Plasma drug level of risperidone and its clinical significance

目的 :观察利培酮治疗精神分裂症时的口服剂量、血药浓度及其疗效和不良反应之间的关系。方法 :对 38例精神分裂症患者 ,应用利培酮 2及 4mg ,疗程 8周。第 2 ,4,8周末采用HPLC测定利培酮及其有效代谢产物 9 羟利培酮的血药浓度。治疗前及治疗后第 1,2 ,4,6 ,8周进行阴阳性症状量表 (PANSS)、临床综合印象量表(CCI)、不良反应症状量表 (TESS)及锥体外系症状量表 (ESRS)评定。结果 :利培酮对精神分裂症阴阳性症状均有效 ,对阴性症状起效时间较阳性症状晚。 2及 4mg组利培酮及其代谢产物 9 羟利培酮血药浓度存在显著差异 ,但疗效无显著性差异。利培酮及其代谢产物治疗窗可能在 30～ 45ng·mL-1。结论 :采取逐渐加量的小剂量治疗 (2～4mg)方法既安全又有效 ,临床上开展利培酮及 9 羟利培酮浓度检测对预测疗效、防止不良反应发生是有意义的。

Objective:To observe the relationship among oral dose,plasma drug level,and the efficacy and side effects of risperidone.Methods:The controlled study was conducted in 38 patients with schizophrenia.They were randomly and equally divided to receive 2 or 4 mg risperidone for 8 weeks.The plasma drug level of risperidone and its active metabolite,9-hydroxyrisperidone,were measured by HPLC method at the end of week 2,4 and 8.The PANSS,CGI,TESS,and ESRS were evaluated at week 1,2,4,6 and 8.Results:Risperidone was effective in both positive and negative symptoms of schizophrenia,but the onset of action for positive symptom was quicker than that of the negative.There was a significant difference in plasma drug level of risperidone and its metabolite between 2 mg and 4 mg groups but no significant difference in efficacy.The effective dose range for risperidone and its active metabolite may be 30～45 ng·mL -1.Conclusion:The effective and safe method for medication of risperidone starts with small dose(2～4mg) and then increases in dose gradually.The efficacy and side effect of risperidone can be predicated and prevented by plasma drug concentration of risperidone and its active metabolite.