Risperidone long-acting injectable (RLAI) is approved for the treatment of schizophrenia in many countries. The suggested site is the gluteal muscle with a needle length of two inches (50 mm) in Japan, which is longer...Risperidone long-acting injectable (RLAI) is approved for the treatment of schizophrenia in many countries. The suggested site is the gluteal muscle with a needle length of two inches (50 mm) in Japan, which is longer than the ordinarily used needle for intramuscular injections. The aim of this study was to determine the optimal needle insertion length for accurate delivery of RLAI procedure among subjects who have normal body mass index (BMI: 18 to 25) and high BMI (>25). Thirty-seven patients with schizophrenia were administered RLAI intramuscularly into the dorsogluteal muscle. The standard procedure required inserting 80% of the two inch needle. By using data collected by ultrasonography, the findings confirmed that the median needle insertion lengths for subjects with normal and high BMI were 39.0 and 45.5 mm, respectively. To deliver RLAI effectively and safely, the authors strongly recommend that a specialized needle be used that is “marked” at the 40 mm point from the tip of the needle to the base. In this way regardless of subcutaneous fat content, the RLAI can be safely delivered into the muscle without causing untoward or side effects.展开更多
The objectives of e-STAR Romania (NCT00283517) were to collect clinical outcome data of Romania schizophrenia or schizo-affective disorder patients;prospectively to assess the reasons of treatment initiation, medicati...The objectives of e-STAR Romania (NCT00283517) were to collect clinical outcome data of Romania schizophrenia or schizo-affective disorder patients;prospectively to assess the reasons of treatment initiation, medication usage patterns;to document (long-term) clinical efficacy;and to collect safety data, as well as recording 2-year corresponding retrospective data. In total, 378 eligible subjects were enrolled who were initiated either on risperidone long-acting injectable (RLAI) (290) or on an oral antipsychotic (OA) (88) at baseline as required by the local Summary of the Product Characteristics. Data were collected from per patient both retrospectively and prospectively over a 24-month period at 3-month intervals after starting treatment. The results indicated that subjects suffering from schizophrenia or schizo-affective disorder initiated on RLAI were less likely to be hospitalized within the first 24 months after the initiation of treatment. Moreover, subjects treated with RLAI experienced significant improvements in their illness severity and functioning. Discontinuation rates for RLAI were low and doses were stable throughout the 24 months following the initiation of treatment. In addition, the necessity for supplementary concomitant medication was reduced. Adverse events were reported in 20.3% (RLAI) and 11.4% (OA) of the subjects. In general, patients initiated on RLAI and OA at baseline both clinically improved on all assessed parameters but a larger improvement was observed for patients on RLAI. Incidences of reported AEs during the use of RLAI in a naturalistic setting are comparable with those described in clinical studies;however, the incidence of extrapyramidal signs and weight gain was lower than expected.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
目的比较两种不同剂型的利培酮(注射用长效利培酮微球与口服利培酮)对精神分裂症患者血浆催乳素及社会功能的影响。方法 74例口服利培酮≤4mg/d达6周且病情稳定的门诊精神分裂症患者,被随机分为注射长效利培酮微球组(注射组,利培酮剂量...目的比较两种不同剂型的利培酮(注射用长效利培酮微球与口服利培酮)对精神分裂症患者血浆催乳素及社会功能的影响。方法 74例口服利培酮≤4mg/d达6周且病情稳定的门诊精神分裂症患者,被随机分为注射长效利培酮微球组(注射组,利培酮剂量每2周为25～50mg)和口服利培酮组(口服组,利培酮剂量≤4mg/d)。于分组前及分组后4周、8周、16周检测患者的血浆催乳素水平,于分组前和分组后8周、16周以个人和社会功能量表(Personal and Social Performance,PSP)评定患者的社会功能,以阳性和阴性症状量表(PANSS)、临床疗效总评量表中的病情严重程度(GGI-SI)及Simpson锥体外系副反应评定量表(SEPS)评定疗效和不良反应。结果注射组37例患者中,有30例(82.1%)完成研究,口服组37例患者中,有32例(85.7%)完成研究,将完成全部研究的患者的资料纳入统计分析。分组前两组的PNASS、CGI-SI及SEPS评分比较均无统计学差异。分组治疗16周后,两组的PANSS评分及CGI-SI评分均下降,但两组间比较无统计学差异;注射组、口服组的SEPS评分的均数(标准差)为3.7(2.5)和5.1(2.8),(t=2.12,P=0.037)。分组治疗8周后,注射组与口服组的血浆催乳素均数(标准差)分别为48.2(15.7)μg/L及54.2(18.8)μg/L,(t=2.59,P=0.012),两组的PSP评分的均数(标准差)分别为70.9(9.7)及65.3(11.1),(t=2.01,P=0.049);分组16周后,注射组与口服组的血浆催乳素浓度的均数(标准差)分别为31.5(17.1)μg/L及58.5(16.8)μg/L,(t=6.24,P<0.001),两组的PSP评分的均数(标准差)分别为79.3(6.0)及66.1(9.6),(t=6.44,P<0.001)。两组血浆催乳素水平的差异有统计学意义(F=4.79,P=0.033),两组PSP分值的差异有统计学意义(F=8.70,P=0.005)。结论与口服利培酮相比,注射长效利培酮微球后患者出现的锥体外系不良反应较轻,高催乳素血症的程度较低,社会功能恢复较好。展开更多
文摘Risperidone long-acting injectable (RLAI) is approved for the treatment of schizophrenia in many countries. The suggested site is the gluteal muscle with a needle length of two inches (50 mm) in Japan, which is longer than the ordinarily used needle for intramuscular injections. The aim of this study was to determine the optimal needle insertion length for accurate delivery of RLAI procedure among subjects who have normal body mass index (BMI: 18 to 25) and high BMI (>25). Thirty-seven patients with schizophrenia were administered RLAI intramuscularly into the dorsogluteal muscle. The standard procedure required inserting 80% of the two inch needle. By using data collected by ultrasonography, the findings confirmed that the median needle insertion lengths for subjects with normal and high BMI were 39.0 and 45.5 mm, respectively. To deliver RLAI effectively and safely, the authors strongly recommend that a specialized needle be used that is “marked” at the 40 mm point from the tip of the needle to the base. In this way regardless of subcutaneous fat content, the RLAI can be safely delivered into the muscle without causing untoward or side effects.
文摘The objectives of e-STAR Romania (NCT00283517) were to collect clinical outcome data of Romania schizophrenia or schizo-affective disorder patients;prospectively to assess the reasons of treatment initiation, medication usage patterns;to document (long-term) clinical efficacy;and to collect safety data, as well as recording 2-year corresponding retrospective data. In total, 378 eligible subjects were enrolled who were initiated either on risperidone long-acting injectable (RLAI) (290) or on an oral antipsychotic (OA) (88) at baseline as required by the local Summary of the Product Characteristics. Data were collected from per patient both retrospectively and prospectively over a 24-month period at 3-month intervals after starting treatment. The results indicated that subjects suffering from schizophrenia or schizo-affective disorder initiated on RLAI were less likely to be hospitalized within the first 24 months after the initiation of treatment. Moreover, subjects treated with RLAI experienced significant improvements in their illness severity and functioning. Discontinuation rates for RLAI were low and doses were stable throughout the 24 months following the initiation of treatment. In addition, the necessity for supplementary concomitant medication was reduced. Adverse events were reported in 20.3% (RLAI) and 11.4% (OA) of the subjects. In general, patients initiated on RLAI and OA at baseline both clinically improved on all assessed parameters but a larger improvement was observed for patients on RLAI. Incidences of reported AEs during the use of RLAI in a naturalistic setting are comparable with those described in clinical studies;however, the incidence of extrapyramidal signs and weight gain was lower than expected.
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.
文摘目的比较两种不同剂型的利培酮(注射用长效利培酮微球与口服利培酮)对精神分裂症患者血浆催乳素及社会功能的影响。方法 74例口服利培酮≤4mg/d达6周且病情稳定的门诊精神分裂症患者,被随机分为注射长效利培酮微球组(注射组,利培酮剂量每2周为25～50mg)和口服利培酮组(口服组,利培酮剂量≤4mg/d)。于分组前及分组后4周、8周、16周检测患者的血浆催乳素水平,于分组前和分组后8周、16周以个人和社会功能量表(Personal and Social Performance,PSP)评定患者的社会功能,以阳性和阴性症状量表(PANSS)、临床疗效总评量表中的病情严重程度(GGI-SI)及Simpson锥体外系副反应评定量表(SEPS)评定疗效和不良反应。结果注射组37例患者中,有30例(82.1%)完成研究,口服组37例患者中,有32例(85.7%)完成研究,将完成全部研究的患者的资料纳入统计分析。分组前两组的PNASS、CGI-SI及SEPS评分比较均无统计学差异。分组治疗16周后,两组的PANSS评分及CGI-SI评分均下降,但两组间比较无统计学差异;注射组、口服组的SEPS评分的均数(标准差)为3.7(2.5)和5.1(2.8),(t=2.12,P=0.037)。分组治疗8周后,注射组与口服组的血浆催乳素均数(标准差)分别为48.2(15.7)μg/L及54.2(18.8)μg/L,(t=2.59,P=0.012),两组的PSP评分的均数(标准差)分别为70.9(9.7)及65.3(11.1),(t=2.01,P=0.049);分组16周后,注射组与口服组的血浆催乳素浓度的均数(标准差)分别为31.5(17.1)μg/L及58.5(16.8)μg/L,(t=6.24,P<0.001),两组的PSP评分的均数(标准差)分别为79.3(6.0)及66.1(9.6),(t=6.44,P<0.001)。两组血浆催乳素水平的差异有统计学意义(F=4.79,P=0.033),两组PSP分值的差异有统计学意义(F=8.70,P=0.005)。结论与口服利培酮相比,注射长效利培酮微球后患者出现的锥体外系不良反应较轻,高催乳素血症的程度较低,社会功能恢复较好。
