Objective： To investigate the effect of ziprasidone on QTc in Chinese patients with schizophrenia. Methods： The study involved 27 patients with schizophrenia. Ziprasidone was initiated with 40 mg/day. From day 3 to ...Objective： To investigate the effect of ziprasidone on QTc in Chinese patients with schizophrenia. Methods： The study involved 27 patients with schizophrenia. Ziprasidone was initiated with 40 mg/day. From day 3 to day 7, the dose was increased gradually to 120-160 mg/d according to the effectiveness and tolerahility. QTc values were measured at the beginning and month 6. Results： At the beginning of the 6 months treatment, the mean QTc interval of patients was （387.5±19.0） ms. At the end of the study, it was （402.9±23.6） ms. The difference has statistically significance （P〈0.05）. The mean QTc interval changed significantly throughout 6-months period but no one exceed the QTc dangerous limits. Significant correlation was found between QTc interval and the dose. Conclusion： In summary, our results suggest that ziprasidone has good tolerance in patient with schizophrenia despite its dose-related QTc prolongation. Ziprasidone have no pro-arrhythmic profile展开更多
In the present study,we aimed to determine the pharmacokinetics(PK),pharmacodynamics(PD),adverse events(AEs),and their relationships in Chinese patients with schizophrenia after a single dose of long-acting risperidon...In the present study,we aimed to determine the pharmacokinetics(PK),pharmacodynamics(PD),adverse events(AEs),and their relationships in Chinese patients with schizophrenia after a single dose of long-acting risperidone.Schizophrenic patients(six females and seven males)were enrolled in this study.Serial blood samples were collected after drug administration during 63 d,and the drug concentrations were analyzed by LC-MS/MS.Safety and tolerance were evaluated by monitoring the AEs,changes in clinical laboratory results,12-lead ECG,vital signs,physical examination,and injection-site reactions.The extrapyramidal symptoms were evaluated using the ESRS.Efficacy was evaluated by the PANSS and BPRS.Twelve out of the 13 participants completed the trial.There were few clinically meaningful changes in mean clinical laboratory values,vital signs,or ECG parameters,except for the prolactin level and body weight.There were no serious AEs,and those observed were reversible.Significant clinical improvements in PANSS and PANSS-derived BPRS total scores were observed.The mean(standard deviation,coefficient of variation)values for these PK parameters were as follows:C_(max),8.954(8.059,90.0%)ng/mL;area under the curve AUC_(0-t),2453(1156,47.1%)ng·h/mL;AUC_(0-∞),2472(1160,46.9%)ng·h/mL;t_(max),830.0(min:744.0,max:984.0,11.8%)h;and t_(1/2),68.56(10.77,15.7%)h.The PK characteristics of long-acting risperidone showed a high level of inter-individual variation,while there were no clear correlations between PK,efficacy and AEs among the patients in the present study.展开更多
基金Supported by the Natural Science Foundation of Shaanxi Province(2011JM4008)
文摘Objective： To investigate the effect of ziprasidone on QTc in Chinese patients with schizophrenia. Methods： The study involved 27 patients with schizophrenia. Ziprasidone was initiated with 40 mg/day. From day 3 to day 7, the dose was increased gradually to 120-160 mg/d according to the effectiveness and tolerahility. QTc values were measured at the beginning and month 6. Results： At the beginning of the 6 months treatment, the mean QTc interval of patients was （387.5±19.0） ms. At the end of the study, it was （402.9±23.6） ms. The difference has statistically significance （P〈0.05）. The mean QTc interval changed significantly throughout 6-months period but no one exceed the QTc dangerous limits. Significant correlation was found between QTc interval and the dose. Conclusion： In summary, our results suggest that ziprasidone has good tolerance in patient with schizophrenia despite its dose-related QTc prolongation. Ziprasidone have no pro-arrhythmic profile
基金Foundation items:The National Major Scientific and Technological Special Project for"Significant New Drug Development"during the Twelfth Five-year Planning Period of China(Grant No.2014ZX09303303).
文摘In the present study,we aimed to determine the pharmacokinetics(PK),pharmacodynamics(PD),adverse events(AEs),and their relationships in Chinese patients with schizophrenia after a single dose of long-acting risperidone.Schizophrenic patients(six females and seven males)were enrolled in this study.Serial blood samples were collected after drug administration during 63 d,and the drug concentrations were analyzed by LC-MS/MS.Safety and tolerance were evaluated by monitoring the AEs,changes in clinical laboratory results,12-lead ECG,vital signs,physical examination,and injection-site reactions.The extrapyramidal symptoms were evaluated using the ESRS.Efficacy was evaluated by the PANSS and BPRS.Twelve out of the 13 participants completed the trial.There were few clinically meaningful changes in mean clinical laboratory values,vital signs,or ECG parameters,except for the prolactin level and body weight.There were no serious AEs,and those observed were reversible.Significant clinical improvements in PANSS and PANSS-derived BPRS total scores were observed.The mean(standard deviation,coefficient of variation)values for these PK parameters were as follows:C_(max),8.954(8.059,90.0%)ng/mL;area under the curve AUC_(0-t),2453(1156,47.1%)ng·h/mL;AUC_(0-∞),2472(1160,46.9%)ng·h/mL;t_(max),830.0(min:744.0,max:984.0,11.8%)h;and t_(1/2),68.56(10.77,15.7%)h.The PK characteristics of long-acting risperidone showed a high level of inter-individual variation,while there were no clear correlations between PK,efficacy and AEs among the patients in the present study.
