氨磺必利与利培酮治疗精神分裂症对照研究

目的：观察氨磺必利治疗精神分裂症的临床疗效与安全性。方法将60例首发精神分裂症患者,随机分为氨磺必利组30例,利培酮组30例,疗程8周。采用阳性与阴性症状量表（ PANSS ）评定疗效,采用副反应量表（ TESS ）评定治疗中出现的不良反应。结果氨磺必利组的治疗总有效率为83.33%,利培酮组为80.00%,两组疗效差异无统计学意义（ P＞0.05）;氨磺必利组的体重增加明显少于利培酮组（ P〈0.05）。结论氨磺必利与利培酮治疗精神分裂症疗效相当,且氨磺必利引起体重增加数例明显较少,值得临床推广。     

进口与国产利培酮薄膜衣片在健康志愿者的生物等效性

目的 研究利培酮薄膜衣片(抗精神分裂症药)在健康志愿者的药代动力学和生物等效性.方法 23名健康男性志愿者随机交叉、单剂量口服受试制剂(进口)和参比制剂(国产)2 mg后,用HPLC-MS/MS测定血浆中利培酮及9-羟基利培酮浓度,计算主要药代动力学参数,评价2种制剂的生物等效性.结果 受试制剂和参比制剂的主要药代动力学参数,利培酮:AUC0～t分别为(94.76±82.93)和(103.05±117.71)ng·h·mL-1;AUC0～1分别为(96.72±84.52)和(105.19±119.36)ng·h·mL0-1;Cmax分别为(15.91±5.63)和(16.21±11.56)ng·mL-1;tmax分别为(1.14±0.73)和(1.15±0.54)h;t1/2分别为(7.32±5.94)和(7.44±6.50)h,受试制剂的相对生物利用度为(106.68±40.21)%.9-羟基利培酮:AUC0-96h分别为(268.56±85.20)和(279.64 ±117.86)ng·h·mL-1;AUC0-∞分别为(282.74±87.46)和(294.28±120.32)ng·h·mL-1;Cmax分别为(10.84±4.69)和(11.11±4.80)ng·mL-1;tmax分别为(3.35±2.32)和(4.48±2.76)h;t1/2分别为(23.18±3.26)和(23.12±4.31)h,受试制剂的相对生物利用度为(101.37±27.23)%.结论 2种制剂具有生物等效性.     

Onset of action of antipsychotics in the treatment of mania

Introduction: An important consideration in treating acute mania is the promptness with which a chosen therapy can bring symptom amelioration. This article reviews the available published data from controlled, blinded studies regarding the latency of responses to antipsychotics in patients with acute mania.

Methods: Articles for this review were obtained from a search of the Medline database (1966–1999), using the following keywords and phrases: antipsychotic, atypical, bipolar disorder, mania, neuroleptic, typical. The bibliographic sections of articles gleaned from this search were used to direct further inquiries.

Results: Although information regarding the onset of action of antipsychotics is limited, we discovered data for four typical and three atypical antipsychotics. Drugs with the fastest onsets include haloperidol, risperidone, and olanzapine, with onsets appearing in 2–6 days. Chlorpromazine and thiothixene were at the slowest end of the continuum, with onsets of 2 weeks or longer. Data regarding pimozide are mixed, with some studies showing an onset equivalent to that of the 'fast' compounds and others showing one similar to that of the 'slow' compounds.

Conclusions: Choice of therapy should consider not only efficacy and safety, but also onset speed. Atypical antipsychotics appear to offer safer, faster, and more effective therapies.     

3种抗精神病药对精神分裂症认知功能的影响

目的:探讨阿立哌唑、利培酮和氯丙嗪对首发精神分裂症患者认知功能的影响。方法:56例首发精神分裂症患者分为阿立哌唑组(n=18)、利培酮组(n=24)和氯丙嗪组(n=14),在治疗前和治疗6周进行阳性与阴性症状量表(PANSS)评分,威斯康星卡片分类测验(WCST)、连线测验(A和B)、韦氏成人智力量表(WAIS)中的数字符号和数字广度(顺、逆)测验等神经心理测验。结果:治疗6周后,3组PANSS评分均明显下降,3组之间差异无显著性。阿立哌唑组和利培酮组各项认知功能指标均有不同程度的改善,而氯丙嗪组只有2项(WCST中持续反应数和数字广度测验)较治疗前显著好转。连线测验B阿立哌唑组显著优于利培酮组,其余各指标两组间差异无显著性。阿立哌唑组除WCST中持续反应数、完成分类数和数字广度测验外,其余各指标均显著优于氯丙嗪组;利培酮组除WCST中持续反应数外,其余各指标均显著优于氯丙嗪组。结论:阿立哌唑和利培酮对首发精神分裂症患者认知功能的改善作用相当,均显著优于氯丙嗪。     

Neuroprotection of posttreatment with risperidone,an atypical antipsychotic drug,in rat and gerbil models of ischemic stroke and the maintenance of antioxidants in a gerbil model of ischemic stroke

Risperidone, an atypical antipsychotic drug, has been discovered to have some beneficial effects beyond its original effectiveness. The present study examines the neuroprotective effects of risperidone against ischemic damage in the rat and gerbil induced by transient focal and global cerebral ischemia, respectively. The results showed that pre‐ and posttreatment with 4 mg/kg risperidone significantly protected against neuronal death from ischemic injury. Many NeuN‐immunoreactive neurons and a few F‐J B‐positive cells were found in the rat cerebral cortex and gerbil hippocampal CA1 region (CA1) in the risperidone‐treated ischemia groups compared with those in the vehicle‐treated ischemia group. In addition, treatment with risperidone markedly attenuated the activation of microglia in the gerbil CA1. On the other hand, we found that treatment with risperidone significantly maintained the antioxidants levels in the ischemic gerbil CA1. Immunoreactivities of superoxide dismutases 1 and 2, catalase, and glutathione peroxidase were maintained in the stratum pyramidale of the CA1; the antioxidants were very different from those in the vehicle‐treated ischemia groups. In brief, our present findings indicate that posttreatment as well as pretreatment with risperidone can protect neurons in the rat cerebral cortex and gerbils CA1 from transient cerebral ischemic injury and that the neuroprotective effect of risperidone may be related to attenuation of microglial activation as well as maintenance of antioxidants. © 2014 Wiley Periodicals, Inc.     

Atypical antipsychotics to treat the neuropsychiatric symptoms of dementia

Neuropsychiatric symptoms are common in older adults with dementia and can be associated with a rapid decline in cognitive and functional status. This article reviews the current literature supporting the use of atypical antipsychotic medications in this population. Among the currently available atypical antipsychotics, risperidone and olanzapine have been the most widely studied in double-blind, randomized, placebo-controlled clinical trials. Despite the common use of other atypical antipsychotic medications, their efficacy and safety in older adults with dementia has not been as extensively studied. Some controversy surrounds the use of atypical antipsychotic agents in older adults with the suggestion that they may increase the incidence of stroke or even death. Despite the potential for increased risk of harm from the use of these medications, atypical antipsychotics are often effective in treating troublesome neuropsychiatric symptoms refractory to other treatments. Whenever possible, these atypical antipsychotic drug treatments should be combined with non-pharmacological treatments to limit the need and dose of antipsychotic drugs and constant monitoring for potential harms should be maintained. The choice of which atypical antipsychotic agent can be guided by the nature and severity of the target symptom and the medication least likely to cause harm to the patient.     

利培酮和氯丙嗪治疗时血糖代谢变化

目的:研究使用抗精神病药影响血糖代谢的特点。方法:198例未曾治疗或停药3个月以上的精神分裂症住院患者给予氯丙嗪或利培酮治疗。于入院时及治疗1、2、3和6个月时检测血糖浓度。结果:氯丙嗪组治疗2个月餐后2 h糖耐量试验(2hPG)、6个月后糖化血红蛋白(HbA1C)浓度均明显高于治疗前。治疗6个月血葡萄糖调节受损(IGR),氯丙嗪组有15.54%,利培酮组有7.37%;≥40岁者2hPG和HbA1C明显高于<40岁者。结论:2hPG和HbA1C浓度增高是糖代谢异常的早期表现,早期干预有利于防止IGR。     

注射用利培酮微球与口服利培酮对精神分裂症血浆催乳素及社会功能的影响

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。     

Risperidone versus haloperidol in children and adolescents with AD

Objective The aim of the study was to compare safety, efficacy and tolerability of risperidone with haloperidol in the treatment of Autistic Disorder (AD). Method This study was designed as a double-blind, prospective, for a 12-week period. A total of 30 subjects, between the ages of 8 and 18 with AD based on DSM IV criteria, were included in the study. Behavioral Rating Scales were performed by the investigators and the parents. Safety assessment included vital signs, electrocardiogram, electroencephalogram, adverse events, laboratory tests, extrapyramidal symptoms and the side effects. Both treatments were applied in a once daily dosage regimen of 0.01–0.08 mg/kg/day. Results The reduction from baseline in Ritvo–Freeman Real Life Rating Scale (RF-RLRS), sensory motor (subscale I) and language (subscale V) scores were significant in risperidone group (P < 0.05). Compared to haloperidol, risperidone led to a significantly greater reduction in the Aberrant Behavior Checklist (ABC) and Turgay DSM-IV Pervasive Developmental Disorder (PDD) scale scores (P < 0.05 and P < 0.01). There was a greater increase of prolactin in the risperidone group, while alanine amino transferase (ALT) had further increased in the haloperidol group. Sensory motor behaviors (subscale I) and language at the end of the 12th week, RF-RLRS sensory motor and language subscale scores decreased in the risperidone group further than the other group (P < 0.05). Conclusions Risperidone was found to be more effective than haloperidol in the treatment of behavioral symptoms, impulsivity, language skills, and impaired social relations in children with AD. These results demonstrated that both drugs were safe and well tolerated in the treatment of AD.