小剂量阿立哌唑联合氨磺必利对女性精神分裂症患者血清泌乳素水平及认知功能的影响

目的 研究小剂量阿立哌唑联合氨磺必利对女性精神分裂症患者血清泌乳素(PRL)水平及认知功能的影响.方法 将在无锡市精神卫生中心2018年12月～2019年12月住院治疗的女性精神分裂症患者60例,按照随机数字表法分为对照组和研究组各30例.两组均行氨磺必利治疗,研究组在氨磺必利治疗基础上再给予小剂量阿立哌唑治疗,在治疗...     

利培酮和氨磺必利治疗女性精神分裂症患者的疗效比较

目的 研究利培酮和氨磺必利治疗精神分裂症(SP)女性患者的疗效及对其外周血催乳素、骨钙素水平的影响.方法 以2018年1月～2020年7月收治的75例女性SP患者为研究对象,按照随机数字表法分为对照组(37例)和观察组(38例),对照组服用利培酮,观察组服用氨磺必利,均治疗8周.比较治疗前和治疗8周后,两组患者病情严重...     

精神分裂症患者氨磺必利血药浓度与不良反应、泌乳素水平及认知功能相关性

目的 观察氨磺必利用于精神分裂症患者疗效以及其血药浓度与患者不良反应、泌乳素水平及认知功能相关性。方法 选择2019年7月—2020年6月80例经氨磺必利单药治疗精神分裂症患者,连续治疗8周,分别于治疗后1,2,4,8周末监测患者服药剂量、血药浓度、疗效[阳性和阴性症状量表（positive and negative symptom scale,PANSS）]及不良反应[治疗不良反应量表（treatment emergent symptom scale,TESS）];于治疗第8周末,检测患者血清泌乳素水平,测量认知功能水平变化[用韦氏成人记忆量表（wechsler memory scale-revised in China,WMS-RC）、威斯康星卡片分类测验（wisconsin card sorting test,WCST）],并分析血药浓度与服药剂量、疗效、不良反应、血清泌乳素、认知功能相关性。结果 Pearson相关分析法显示,治疗第1周末、第2周末、第4周末、第8周末的血药浓度与PANSS减分率、阳性症状减分率、阴性症状减分率、精神病理减分率、TESS评分均呈正相关（P<0.05）。治疗第8周末,男性、女性患者血清泌乳素均明显高于基线日（P<0.05）,且女性患者氨磺必利血药浓度与血清泌乳素呈正相关（P<0.05）。治疗第8周末,患者WMS-RC测试中记忆商（memory quotient,MQ）明显较基线日升高（P<0.05）,WCST测验中第一个分类所需应答数（number of responses required for the first classification,R1st）较基线日明显下降、完成分类数（completed classification,Cc）较基线日明显升高（P<0.05）,但氨磺必利血药浓度与MQ、R1st、Cc均未发现明显相关性。结论 精神分裂症患者氨磺必利血药浓度与疗效、不良反应及女性患者泌乳素水平均表现出相关性,应对患者血药浓度进行监测,以进一步指导个体化用药。     

氨磺必利对精神分裂症患者血清泌乳素水平及阳性与阴性症状量表分值的影响

目的 探讨氨磺必利对精神分裂症患者血清泌乳素(prolactin,PRL)水平及阳性与阴性症状量表(positive and negative syndrome scale,PANSS)分值的影响.方法 选取2018年3月至2020年3月期间我院收治的精神分裂症患者156例,随机分为研究组和对照组,每组78例.对照组给...     

氨磺必利与奥氮平治疗女性精神分裂症的疗效及安全性

目的：比较氨磺必利和奥氮平对女性精神分裂症患者的疗效与安全性。方法：将60例女性精神分裂症患者随机分组,治疗组30例选用氨磺必利进行治疗,对照组选用奥氮平治疗。观察12周,两组于治疗前及治疗后第2、4、8、12周末,评定阳性与阴性综合量表（PANSS）及治疗时出现的症状量表（TESS）,评价临床疗效与不良反应。结果：两组治疗后2周的阳性与阴性综合量表（PANSS）评分减分率无显著差异（P＞0.05）。经治疗后两组的血清泌乳素值均增加,两组比较无统计学差异（P〉0.05）,但治疗组出现月经改变的几率较对照组高（P〈0.05）;治疗组患者的体重升高发生率比对照组低（P〈0.05）。结论：氨磺必利和奥氮平的疗效相当,氨磺必利引起月经改变现象较奥氮平多见,氨磺必利引起体重增加现象较奥氮平少见。     

氨磺必利和舒必利治疗女性精神分裂症的临床效果比较

目的总结分析氨磺必利和舒必利治疗女性精神分裂症的临床效果。方法选择2013年1月～2013年12月本院收治的80例女性精神分裂症患者为研究对象,随机分为观察组和对照组,各40例,观察组给予氨磺必利治疗,对照组给予舒必利治疗,治疗2个月后,比较两组的治疗效果和不良反应。结果观察组的有效率87.50%,对照组为85.00%,两组比较差异无统计学意义（P〈0.05）;两组治疗后的PANSS评分均明显低于治疗前（P〈0.05）,但两组治疗后的PANSS评分比较差异无统计学意义（P〈0.05）;观察组的不良反应发生率为10.00%,明显低于对照组的37.50%（P〈0.05）。结论氨磺必利与舒必利对女性精神分裂症的治疗效果相当,但舒必利的不良反应发生率较高,临床要慎重选择用药。     

氨磺必利联合奥氮平对精神分裂症患者认知功能的影响

目的:研究氨磺必利联合奥氮平对精神分裂症患者认知功能的影响。方法:选择2014年3月—2015年12月精神分裂症患者94例,根据随机数字表法均分为两组。单一药物组采用奥氮平治疗,药物联合组采用氨磺必利联合奥氮平治疗。比较两组患者疾病治疗总有效率、治疗前后阳性和阴性症状量表(PANSS)总分、治疗前后患者认知功能和生存质量情况的差异。结果:药物联合组疾病治疗总有效率比单一药物组高,差异有统计学意义(P<0.05);治疗前两组PANSS总分相似,差异无统计学意义(P>0.05);治疗后药物联合组相较于单一药物组PANSS总分改善更显著,差异有统计学意义(P<0.05)。治疗前两组认知功能和生存质量情况相似,差异无统计学意义(P>0.05);治疗后药物联合组相较于单一药物组认知功能和生存质量情况改善更显著,差异有统计学意义(P<0.05)。结论:氨磺必利联合奥氮平治疗精神分裂症,可有效改善患者认知功能和临床症状,促进患者治疗后生存质量的改善,可减轻患者痛苦,对减轻其家庭和社会负担均有重大意义。     

氨磺必利治疗首发精神分裂症50例临床疗效探讨

目的探讨氨磺必制治疗首发精神分裂症患者的临束疗效。方法选择符合条件的首发精神分裂症患者50例,阳性亚型组以≥400mg/d为起始剂量,阴性亚型组以100～300mg/d为起始剂量的氨磺必利治疗10周,疗效评定采用阳性与阴性量表(PANSS)。结果治疗结束时,痊愈3.7%,显效66.1%,有效22.2%,PANSS量表总分及分量表分与治疗前比较均有显著性差异。结论氨磺必利对精神分裂症的阳性及阴性症状均有疗效,且以较低剂量即能明显改善阴性症状为突出特点。     

Effect of the amisulpride isomers on rat prolactinemia

The effects on rat serum prolactin level of the two isomers constituting the racemic form of amisulpride were compared. (S-)-amisulpride induced hyperprolactinemia at lower doses (ED(50) = 0.09 +/- 0.01 mg/kg) than racemic- (ED(50) = 0.24 +/- 0.03 mg/kg) and (R+)-amisulpride (ED(50) = 4.13 +/- 0.05 mg/kg), in accord with their affinities for pituitary dopamine D(2) receptor (K(i) = 3.8 +/- 0.2, 6.4 +/- 0.2 and 143.3 +/- 2.3 nM, respectively). At doses twice the ED(50), (S-)-amisulpride produced a maximal increase in prolactin level similar to that of the racemic form (403 +/- 21% and 425 +/- 15%, respectively), but higher than that of (R+)-amisulpride (198 +/- 8%). These results suggest that the hyperprolactinemia induced by the racemic-amisulpride is mostly due to its (S-)-isomer.     

Effect of the amisulpride isomers on rat catalepsy

The substituted benzamide amisulpride is currently administered in its racemic form. In the present study, the biochemical and cataleptogenic profiles of the two enantiomers (R+ and S-) were compared with those of the racemic mixture. Displacement binding studies showed that the (S-)-isomer possesses an higher affinity for dopamine D2-like receptor (K(i) 5.2+/-0.4 nM) compared to (R+)-amisulpride (K(i) 244+/-12 nM) and to (RS)-amisulpride (K(i) 9.8+/-0.8 nM). In contrast, (S-)-amisulpride binds the alpha(2)-receptor with an affinity (K(i) 1528+/-45 nM) lower than that of the (R+)-isomer (K(i) 375+/-34 nM) and of (RS)-amisulpride (K(i) 783+/-27 nM). The bar test was used to evaluate the catalepsy induced by each drug. (RS)-amisulpride induced catalepsy only at very high doses (>100 mg/kg, s.c.) whereas, (S-)-amisulpride produced a catalepsy at a lower dose (30 mg/kg, s.c.) and (R+)-amisulpride did not produce any catalepsy up to the dose of 75 mg/kg. Interestingly, (R+)-amisulpride reduced the catalepsy induced by (S-)-amisulpride (50 mg/kg, s.c.) or haloperidol (0.3 mg/kg, s.c.), at the doses of 50 or 30 mg/kg, respectively. These results indicate that the weak cataleptic properties of (RS)-amisulpride might partially rely on its (R+)-isomer and provide a further explanation for the atypical properties of amisulpride as an antipsychotic.     

Focus on amisulpride

Amisulpride is a second-generation antipsychotic, a substituted benzamide. It appears to be an effective agent in treating schizophrenia for what are characterised as positive and negative symptoms. The recommended doses are between 400 mg/day and 800 mg/day. Amisulpride demonstrates a good global safety profile, particularly when compared with first-generation antipsychotics, such as haloperidol. There are interesting studies that point towards amisulpride's antidepressant effect in dysthymia speculative on possible roles in affective psychoses and chronic fatigue syndrome.     

阿立哌唑对利培酮所致催乳素升高的作用研究

目的探讨阿立哌唑对男性抗精神病药所致的高催乳素（PRL）副作用的治疗作用。方法对74例利培酮治疗的男性精神分裂症患者随机分组,均采用利培酮治疗,起始1 mg/d,并根据精神症状调整药量至治疗量4-6 mg/d。研究组于第3周开始加用阿立哌唑5 mg/晚,直至研究结束不再增加阿立哌唑剂量,分别于0、2、4、8、12周末进行催乳素检测,对治疗中出现的其他不良反应进行TESS评定。结果加用阿立哌唑后,研究组PRL在12周末时（164.54±69.26）μIU/mL与基线期（151.97±64.66）μIU/mL比较差异无统计学意义（P=0.435,t=0.785）,而对照组第2周后PRL持续增高（177.28±45.18）μIU/mL,第4周末时明显异常（351.41±61.56）μIU/mL。但第8周（379.59±73.62）μIU/mL和12周（382.50±76.89）μIU/mL相比较变化不大。两组不良反应发生率差异无统计学意义（χ2=3.12,P=0.077）。但不良反应的构成存在一定差异,研究组静坐不能7例（20%）,震颤6例（17.14%）,头痛11例（31.43%）,肌强直3例（8.57%）,对照组静坐不能10例（31.25%）,震颤9例（28.12%）,肝功能异常3例（9.38%）,肌强直9例（28.13%）,便秘6例（18.75%）,体重增加11例（34.38%）。结论阿立哌唑对于利培酮导致的男性催乳素升高有一定的控制及治疗作用。且两药联用并未增加副反应的风险。     

Spotlight on amisulpride in schizophrenia

Amisulpride, a substituted benzamide derivative, is a second-generation (atypical) antipsychotic. At low doses, it enhances dopaminergic neurotransmission by preferentially blocking presynaptic dopamine D(2)/D(3) autoreceptors. At higher doses, amisulpride antagonises postsynaptic D(2) and D(3) receptors, preferentially in the limbic system rather than the striatum, thereby reducing dopaminergic transmission. In patients with acute exacerbations of schizophrenia, the recommended dosage of amisulpride is 400 to 800 mg/day, although dosages < or = 1200 mg/day may be administered. In comparative trials, amisulpride administered within this range (400 to 1200 mg/day) was as effective as haloperidol 5 to 40 mg/day, flupenthixol 25 mg/day and risperidone 8 mg/day in patients with acute exacerbations of schizophrenia with predominantly positive symptoms. Amisulpride was more effective than haloperidol but equally effective as risperidone in controlling negative symptoms. Amisulpride 400 to 800 mg/day was more effective than haloperidol, risperidone and flupenthixol in controlling affective symptoms in these patients. In randomised, double-blind trials involving patients with predominantly negative symptoms of schizophrenia, amisulpride 50 to 300 mg/day was more effective than placebo. Amisulpride is effective as maintenance therapy in patients with chronic schizophrenia. Long-term treatment with amisulpride was associated with improvements in quality of life and social functioning. Amisulpride is generally well tolerated. In well-controlled trials, the neurological tolerability profile (including ratings on extrapyramidal symptom scales) of amisulpride 400 to 1200 mg/day was superior to that of the conventional antipsychotics (haloperidol or flupenthixol), but was similar to that of the atypical antipsychotic risperidone. At low dosages of amisulpride (< or = 300 mg/day), the incidence of adverse events (including extrapyramidal symptoms) reported with amisulpride was similar to that with placebo. Conclusion: In comparative trials, amisulpride 400 to 1200 mg/day showed efficacy in reducing overall symptomatology and positive symptoms similar to that of conventional antipsychotics and newer atypical antipsychotics in patients with acute exacerbations of schizophrenia. Moreover, its effective alleviation of negative and affective symptoms, its lower association with extrapyramidal symptoms and loss of cognitive function than conventional antipsychotics and its long-term efficacy justifies consideration of the use of higher dosages of amisulpride in this group of patients. Consequently, the dosage of amisulpride that is recommended in patients with acute exacerbations of schizophrenia is 400 to 800 mg/day, although dosages < or = 1200 mg/day may be administered. Lower dosages of amisulpride (50 to 300 mg/day) should be considered for the management of patients with negative symptoms of schizophrenia. Amisulpride is a first-line treatment option in the management of schizophrenia in the acute phase and for the maintenance of treatment response.     

Effect of methyldopa on prolactin serum concentration

Summary In a group of ten hypertensive patients, the effects of methyldopa administration in two different formulations on serum prolactin (PRL) were studied. A single oral dose of normal release methyldopa significantly increased serum prolactin levels, peak concentrations occurring 3 to 6 h after drug administration. On the contrary, administration of sustained release methyldopa at the same dose was only followed by slight and not significant fluctuations in prolactin plasma levels. Both formulations produced a significant decrease of systolic and diastolic blood pressures, without significant differences between sustained and normal release methyldopa effects.     

Effects of amisulpride on consummatory negative contrast

Two groups of rats, 'shifted' (32-4% sucrose) and 'unshifted' (4-4% sucrose), were given access to sucrose solutions for 5 min/day for 10 days. On day 11, shifted animals had access to a devalued incentive (4% sucrose) and subgroups of each group received doses of amisulpride (10 or 60 mg/kg, i.p.) or its vehicle before a 10-min access period to sucrose solutions. Lick frequency was measured both pre- and post-shift. A high dose of amisulpride reduced successive negative contrast (SNC) after a brief period of exposure to the devalued stimulus, whereas a low dose had no effect. The acute effects of high doses of amisulpride seem to act on contrast effects in a similar way to anxiolytic compounds such as the benzodiazepine, chlordiazepoxide.     

氨磺必利与利培酮治疗精神分裂症的疗效及安全性对比

目的：比较氨磺必利与利培酮治疗精神分裂症的疗效及安全性。方法选取2013年6月—2014年6月收治的精神分裂症患者58例,随机分为氨磺必利组和利培酮组,每组29例。氨磺必利组给予氨磺必利治疗,利培酮组给予利培酮治疗。应用阳性和阴性症状量表（ PANSS）评定疗效,应用副反应量表（ TESS）评定不良反应。结果两组临床疗效、治疗后PANSS评分以及锥体外系反应、头痛、失眠、恶心发生率比较,差异无统计学意义（ P﹥0.05）,利培酮组体质量增加发生率高于氨磺必利组,差异有统计学意义（ P﹤0.05）。结论氨磺必利与利培酮治疗精神分裂症均安全有效。