Amisulpride in the short-term treatment of depressive and physical symptoms in cancer patients during chemotherapies

Introduction Amisulpride is a substituted benzamide that, at low doses, selectively blocks D2 and D3 presynaptic dopamine receptors, enhancing dopaminergic transmission in frontal cortex and limbic areas. Many clinical studies versus placebo, tricyclic antidepressants and selective serotonin reuptake inhibitors showed amisulpride antidepressant effect, supporting its safety and rapid onset of action. In oncological population, depression is quite frequent and difficult to treat because of the particular sensitivity of cancer patients to the antidepressants’ side effects. Goals of work The aims of this study were to evaluate efficacy, safety and tolerability of low doses of amisulpride (50 mg) in oncological, depressed patients during chemotheraphy. Materials and methods One hundred six consecutive cancer outpatients with depressive symptoms were treated in a prospective, intention to treat, 4-week study, and were evaluated in single-blind with Montgomery Asberg rating scale for depression (MADRS), clinical global impression (CGI) and dosage record treatment emergent symptom scale (DOTES) to assess side effects of treatment. Main results After 4 weeks of treatment, scores of MADRS and CGI significantly improved (p < 0.002; p < 0.001, respectively), with a reduction of depressive symptoms concerning both emotional (such as apparent sadness, reported sadness, inner tension, etc.) and physical cluster (such as lack of appetite, reduction in weight, tiredness and insomnia) with good tolerability (only two patients dropped out). Conclusions This study is the first trial on the use of amisulpride in a cohort of oncological, depressed patients during chemotherapy. Amisulpride demonstrated high efficacy and safety. Controlled studies are needed to confirm these preliminary data.     

氨磺必利联合丙戊酸钠治疗酒精所致精神障碍的临床效果及预后影响分析

目的 评价氨磺必利联合丙戊酸钠治疗酒精所致精神障碍（mental disorder induced by alcohol，MDIA）的临床疗效与安全性。方法 选择2015 年6 月~2017 年5 月66 例男性MDIA 患者，根据随机数字表法分为研究组和对照组，研究组予氨磺必利联合丙戊酸钠治疗，对照组予氨磺必利治疗，应用阳性与阴性症状量表（Positive and Negative Syndrome Scale，PANSS）、不良反应症状量表（Treatment Emergent Symptom Scale，TESS）评价临床治疗效果和用药安全性。结果 研究组总有效率96.97%，高于对照组的81.82%，差异有统计学意义（P<0.05）；研究组患者治疗后PANSS 评分逐渐降低，两组比较，差异有统计学意义（F=6.937，P<0.05）；研究组不良反应率9.09%，对照组6.06%，两组比较，差异无统计学意义（χ2=0.926，P>0.05）；两组TESS 评分比较，差异无统计学意义（F=0.234，P>0.05）。结论 氨磺必利联合丙戊酸钠可提高治疗MDIA 效果，安全性高。     

氨磺必利与奥氮平治疗女性精神分裂症患者的对照研究

目的 比较氨磺必利与奥氮平治疗女性精神分裂症患者的疗效及安全性.方法 采用随机、单盲对照的方法,将100例女性精神分裂症患者随机均分为2组(n=50),分别使用氨磺必利(氨磺必利组)和奥氮平(奥氮平组)治疗8周,采用阳性症状与阴性症状(PANSS)量表评定疗效,采用副反应(TESS)量表评定不良反应.结果 经过8周治疗,氨磺必利组和奥氮平组显效率分别为76.6%和72.9%,2组疗效差异无统计学意义(U=0.167,P>0.05);但治疗4周末氨磺必利组阴性症状分较奥氮平组减少更显著(P<0.05).而氨磺必利和奥氮平组的不良反应发生率分别为38.3%和45.8%,差异无统计学意义,但奥氮平组嗜睡和体质量增加指标显著高于氨磺必利组,差异具有统计学意义(P<0.05),其他不良反应发生率差异无统计学意义.结论 氨磺必利是一种安全有效的抗精神病药,较适合女性精神分裂症患者的临床治疗.     

牛黄宁宫片联合氨磺必利治疗精神分裂症的临床研究

目的探讨牛黄宁宫片联合氨磺必利治疗精神分裂症的临床疗效。方法选取2017年2月—2017年11月在武威市红十字精神病院进行诊治的94例精神分裂症患者,根据用药差别分为对照组和治疗组,每组各47例。对照组口服氨磺必利片,0.4 g/次,1次/d;治疗组在对照组基础上口服牛黄宁宫片,6片/次,3次/d。两组均连续治疗2个月。观察两组的临床疗效,比较两组治疗前后PANSS评分、HAMD评分、GQOLI-74评分、血清学指标的变化情况。结果治疗后,对照组和治疗组的总有效率分别是80.85%、95.74%,两组比较差异具有统计学意义(P0.05)。治疗后,治疗后,两组PANSS评分、HAMD评分较治疗前均显著降低,GQOLI-74评分显著升高,同组治疗前后比较差异有统计学意义(P0.05);治疗后,治疗组PANSS评分、HAMD评分低于对照组,GQOLI-74评分高于对照组,两组比较差异有统计学意义(P0.05)。治疗后,两组血清神经元特异性烯醇化酶(NSE)、S100β蛋白、白细胞介素-1β(IL-1β)、高迁移率族蛋白B1(HMGBl)水平均较治疗前显著降低,但胶质源性神经营养因子(GDNF)水平均显著增高,同组治疗前后比较差异有统计学意义(P0.05);治疗后,治疗组NSE、S100β蛋白、IL-1β、HMGBl低于对照组,GDNF水平高于对照组,两组比较差异有统计学意义(P0.05)。结论牛黄宁宫片联合氨磺必利治疗精神分裂症具有较好的临床疗效,可有效改善患者症状体征,提高患者生活质量,调节血清学指标,具有一定的临床推广应用价值。     

比较氨磺必利与利培酮治疗精神分裂症的效果评价

目的：分析氨磺必利与利培酮治疗精神分裂症的临床效果和不良反应。方法精神分裂症患者130例,分为研究组和对照组,研究组65例予以氨磺必利治疗,对照组65例采用利培酮治疗,疗程共计8周,采用阳性与阴性症状量表（ PANSS）和副反应量表（TESS）评定其疗效和不良反应。结果研究组总有效率为83%,对照组总有效率为77%,两组间差异无统计学意义（P〉0.05）。8周末研究组和对照组PANSS总分值均显著下降（P〈0.05）;两组不良反应差异无统计学意义（ P〉0.05）。结论氨磺必利治疗精神分裂症疗效优于利培酮,且不良反应与利培酮相似。     

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。     

氨磺必利与氯丙嗪对以阴性症状为主的精神分裂症认知功能影响的对照研究

目的比较氨磺必利和氯丙嗪对以阴性症状为主的精神分裂症患者认知功能的影响。方法应用随机对照的方法,将76例符合条件的以阴性症状为主的精神分裂症患者随机分为氨磺必利组和利培酮组各38例,进行为期12周的治疗。于治疗前及治疗后12周末采用威斯康星卡片(WCST)和连续作业测验(CPT)评定患者的认知功能。结果治疗12周末氨磺必利组的各项认知功能指标均有不同程度的改善(χ2=4.12,P0.05;t=3.41,P0.05),且氨磺必利组的总体疗效优于氯丙嗪组。结论氨磺必利较氯丙嗪能显著改善以阴性症状为主的精神分裂症患者的认知功能,其具体作用机制尚需进一步探讨。     

Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers

Objective: Amisulpride is a substituted benzamide neuroleptic, which binds selectively to dopamine D₂ and D₃ receptors, mainly in the limbic structures. States of delusion and agitation occur frequently in the population aged more than 65 years, especially in demented patients and this sometimes requires the use of neuroleptics. The objectives of this study were to determine the safety and the pharmacokinetic profile of 50 mg of amisulpride administered orally as a single dose to elderly volunteers. Methods: Twenty healthy volunteers (10 men and 10 women) aged 65–79 years were included in this open trial. Frequent measurements of blood pressure and heart rate were made and ECG and blood samples were performed up to 72 h after drug intake. Results: The overall clinical and cardiovascular safety was satisfactory. The mean C_max of the racemate amisulpride in elderly people was 64.1 ± 6.7 ng · ml⁻¹, and was not different from the value of 56 ± 4.1 ng · ml⁻¹ in young subjects. As with the C_max, the mean values of t_1/2 and AUC in elderly people (15.6 ± 1.3 h and 667 ± 51 ng · ml⁻¹· h, respectively) were not different to values observed in young subject (respectively 11.7 ± 0.5 h and 603 ± 25 ng · ml⁻¹· h). Conclusions: A single oral dose of amisulpride was well tolerated and showed a similar pharmacokinetic profile in healthy elderly and young subjects. However, these findings should be confirmed after multiple dosing in a larger population in order to establish the lack of need of dosage adjustment in this elderly population. Received: 13 October 1997 / Accepted in revised form: 11 March 1998     

Single oral doses of amisulpride do not enhance the effects of alcohol on the performance and memory of healthy subjects

Objectives: Amisulpride is a benzamide antipsychotic that binds selectively to dopamine D₂- and D₃-receptors, preferentially in limbic and hippocampal structures. Since other substituted benzamides have a limited or negligible interaction with alcohol on human performance, amisulpride was studied for this potential. Methods: In a randomised double-blind crossover study, 18 young, non-smoking men took single oral doses of placebo and amisulpride 50 mg and 200 mg, without and with ethanol (0.8 g ⋅kg⁻¹) taken 30 min later. Objective performance tests and self-ratings were done at baseline and 1.5, 3.5 and 6.5 h after drug intake. Memory (immediate and delayed recall) was tested 2 h after dosing. Breath ethanol and the plasma concentrations of amisulpride and prolactin were measured. Three-way ANOVA + Newman-Keul tests were used for statistical analyses; interactions were confirmed by factorial contrast ANOVA. Results: Mean blood ethanol was 0.94, 0.62 and 0.26 g ⋅l⁻¹ at the three test times. It produced significant impairment in all performance tests (symbol digit substitution, simulated driving, body sway, flicker fusion, tapping, nystagmus), reduced both immediate and delayed recall in memory tests, and caused subjective clumsiness, muzziness and mental slowness, mainly between 1.5 to 4.5 h after dosing. Amisulpride, 50 and 200 mg elevated plasma prolactin but had minimal or no effect on performance, attention and memory. The decreases in immediate free recall after the 50 mg dose and in delayed free recall after the 200 mg dose were slight. Amisulpride neither modified blood ethanol concentrations nor enhanced the detrimental effect of ethanol on skilled and cognitive performance; it slightly antagonised ethanol in the digit copying test. Ethanol did not modify the effect of amisulpride on plasma prolactin, and the plasma concentrations of amisulpride were little changed by ethanol. Conclusions: Amisulpride in single oral doses of 50 and 200 mg did not interact significantly with the effects of high, moderate or low concentrations of ethanol on human skilled and cognitive performance. The drugs did interact pharmacokinetically. Received: 22 December 1995/Accepted in revised form: 1 April 1996     

Amisulpride: efficacy in the management of chronic patients with predominant negative symptoms of schizophrenia

Amisulpride is a dopamine D2/D3-selective antipsychotic drug with potent antipsychotic efficacy in acute exacerbations of schizophrenia. It also possesses substantial efficacy in chronic schizophrenic patients with enduring predominant negative symptoms. This unique property has been demonstrated in a series of short (6 weeks) and medium-/long-term (6–12 months) double-blind placebo-controlled studies. The patients in these studies were carefully selected and assessed to avoid confounding results with non-specific changes in other symptom domains. The results not only show effects on negative symptoms at the optimal dose of 100 mg/day, but also significant improvement in global functioning. The effect observed in short-term studies was maintained over longer treatment periods (6–12 months). Amisulpride was well tolerated with a safety profile similar to placebo. These results open a new therapeutic approach for negative symptoms, one of the most disabling aspects of schizophrenia. Received: 25 July 2000 / Accepted: 26 July 2001