AbstractA simple flow-injection chemiluminescence method with synergistic enhancement has been investigated for the rapid and sensitive determination of antipsychotic risperidone. The synergistic action was significant in the chemiluminescence system of luminol—hydrogen peroxide with risperidone as an enhancer. The increased chemiluminescence intensity was correlated with risperidone concentration within the range from 10 pg mL−1 to 1.0 ng mL−1 with relative standard deviations lower than 5.0 % and the detection limit of 4 pg mL−1. At a flow rate of 2.0 mL min−1, the flow-injection chemiluminescence method exhibited both a high sensitivity and excellent selectivity giving a throughput of 120 times per hour. The proposed method was successfully applied to determine the risperidone content in human urine without any pretreatment. It was found that the excretive amounts of risperidone reached their maximum after taking 2.0 mg of risperidone for 1 h, with a total excretive ratio of 17.37 % in 8.5 h.