齐拉西酮与奥氮平治疗早期精神分裂症的临床效果比较

目的 探讨齐拉西酮和奥氮平对于治疗早期精神分裂症的临床疗效及比较两者的安全性。方法 选取我院2017年9月～2019年2月收治的60例早期精神分裂症患者作为研究对象,采用数字随机法将所有患者分成对照组30例和观察组30例,对照组给予奥氮平治疗,观察组给予齐拉西酮治疗。2周为1个疗程,两组均进行8周4个疗程治疗。比较两组患者于治疗前和治疗后2、4、8周进行阳性和阴性症状量表(PANNS)评分,病情严重程度(SI)、疗效总评(GI)评分和不良反应。结果 治疗2周、4周后,两组患者的PANSS评分和SI、GI评分均较低于治疗前,但两组的PANSS评分和SI、GI评分比较,差异无统计学意义(P0.05);疗程结束后,观察组的患者PANSS评分和SI、GI评分均低于对照组,差异有统计学意义(P0.05);治疗期间,对照组的不良反应发生率高于观察组,差异有统计学意义(P0.05)。结论 对于治疗早期分裂症患者,齐拉西酮的长期治疗效果明显优于奥氮平,且安全可靠,值得临床上进一步推广。     

利培酮和齐拉西酮对精神分裂症患者血浆细胞因子的影响

目的:研究抗精神病药对精神分裂症患者细胞因子的影响。方法:符合ICD-10精神分裂症诊断的60名患者,随机分为利培酮组(给予利培酮治疗)和齐拉西酮组(给于齐拉西酮治疗),并以健康对照组比较,对患者在治疗前及治疗8周后测量血浆IL-2、IL-6及TNF-α水平,并对患者进行PANSS量表评定。结果:两组患者治疗前后血浆IL-2、IL-6及TNF-α水平与对照组比较,差异有统计学意义(P0.05)。两组患者治疗后血浆IL-2、IL-6及TNF-α水平较治疗前降低,差异有统计学意义(P0.05)。治疗前IL-2水平与PANSS量表阳性症状评分呈正相关(r=0.54,P0.05)治疗后TNF-α与阴性症状分呈显著正相关(r=0.41,P0.05)。结论:精神分裂症患者存在免疫功能异常,利培酮和齐拉西酮可以降低精神分裂症患者细胞因子水平。细胞因子水平与精神病理存在一定相关性。     

盐酸齐拉西酮在中国健康志愿者中的药代动力学研究

目的评价国产盐酸齐拉西酮胶囊的人体药代动力学特点;初步评价国产盐酸齐拉西酮胶囊的安全性。方法采用HPLC法测定血浆中齐拉西酮浓度。10位男性健康受试者进食时单剂量口服40mg盐酸齐拉西酮胶囊。于服药前及服药后0.5、1、2、3、4、5、6、8、10、12、24、36、48小时采集5m l血样。抗凝处理取血浆,-20℃保存,用于血药浓度的测定。安全性评价包括体检、实验室检查(心电图、血常规、生化常规及尿常规等)及不良事件的记录。结果主要药动学参数:Cm ax为(175.0±63.73)ng/m l;Tm ax为(3.80±1.32)h;MRT为(9.37±1.53)h;t1/2为(6.10±1.65)h;Ka为0.1831±0.0708/h;Kel为0.1219±0.0349/h;Vd为(685.3±325.4)L;C l为(83.30±34.50)L/h;AUC0→t为(1312±261.3)ng/m l/h,AUC0→∝为(1339±261.1)ng/m l/h。药物不良事件主要为嗜睡、口干、头昏、静坐不能、体位性低血压等,程度多为轻至中度,均能在短时间内缓解。结论研究结果显示了国产盐酸齐拉西酮在中国人中药代动力学特点,单剂量口服胶囊40mg是安全的。     

The in vivo effects of olanzapine and other antipsychotic agents on receptor occupancy and antagonism of dopamine D1, D2, D3, 5HT2A and muscarinic receptors

The atypical antipsychotic olanzapine was compared to other atypical as well as typical antipsychotic agents for in vivo occupancy of D₁, D₂, D₃, 5HT₂, and muscarinic receptors in rat brain. Blockade of D₂ receptors was determined by measuring the levels of the dopamine metabolite 3,4-dihydroxyphenylacetic acid (DOPAC). To assess the interaction with phosphoinositide (PI)-coupled 5HT_2A and muscarinic receptors in vivo, we used a novel radiometric technique to measure in vivo PI hydrolysis. The antagonism of olanzapine and other antipsychotic agents on 5HT_2A and muscarinic receptors was determined by in vivo blockade of PI hydrolysis, stimulated by the 5HT₂ agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) or the muscarinic agonist pilocarpine. Olanzapine inhibited 5HT₂, D₂, and D₃ in vivo binding with high potency (ID₅₀ = 0.15, 0.6 and 1.2 mg/kg, IP, respectively), while inhibiting D₁ and muscarinic in vivo binding with much less potency (ID₅₀ > 10 mg/kg, IP). The binding of olanzapine to D₂ receptors in neostriatum was well correlated with the increase of DOPAC (ED₂₀₀ = 0.8 mg/kg, IP) in vivo, indicating dopamine D₂ antagonism. In vivo PI hydrolysis was increased by DOI in frontal cortex and by pilocarpine in hippocampus up to 2- and 7-fold above the basal level, respectively. The agonist-induced increases in PI hydrolysis were fully blocked by the 5HT_2A antagonist MDL100907 and the muscarinic antagonist scopolamine, indicating the mediation by 5HT_2A receptors in frontal cortex and PI-coupled muscarinic receptors (m1, m3, and m5) in hippocampus, respectively. Olanzapine was about 8-fold more potent in vivo in blocking DOI-induced stimulation of PI hydrolysis (ID₅₀ = 0.1 mg/kg, IP) than pilocarpine-induced stimulation of PI hydrolysis (ID₅₀ = 0.8 mg/kg, IP). In conclusion, olanzapine is more potent in blocking the 5HT_2A receptor than D₁, D₂, D₃ and muscarinic receptors in vivo, consistent with its favorable clinical profiles. In addition, the novel in vivo PI hydrolysis assay proved to be a useful and reliable in vivo method to assess the functional efficacy of compounds that interact with the 5HT₂ and muscarinic receptors. Received: 10 February 1998/Final version: 22 April 1998     

齐拉西酮与利培酮治疗首发精神分裂症的疗效和安全性

目的观察齐拉西酮与利培酮对首发精神分裂症患者的治疗效果和不良反应,以更好地为精神分裂症患者进行治疗。方法选择2010年8月-2012年8月广州市脑科医院收治的首发精神病患者64例为研究对象,随机分为两组。对照组给予利培酮治疗,实验组给予齐拉西酮治疗,对比观察两组疗效和不良反应。结果实验组患者经治疗,其PANSS优于对照组患者,组间比较差异有统计学意义(P<0.05);实验组不良反应发生率明显低于对照组(32例患者共发生14例),组间比较差异有统计学意义(P<0.05)。结论使用齐拉西酮对首发精神病患者进行治疗可取得更好的治疗效果,且患者不良反应少,值得临床推广应用。     

齐拉西酮和奥氮平治疗精神分裂症的疗效及对认知功能的影响

目的探讨齐拉西酮和奥氮平治疗精神分裂症的疗效及对认知功能的影响。方法选取住院治疗的精神分裂症患者76例,随机分为观察组与对照组。观察组患者予齐拉西酮片治疗,先予以20 mg/d,2周内逐渐加至维持量80~160 mg/d;对照组患者予以奥氮平片治疗,先予5 mg/d,2周内逐渐加至维持剂量10~20 mg/d。两组疗效均为8周。观察两组患者治疗前与治疗8周后认知功能指标的变化,并比较其临床疗效和安全性。结果治疗8周后,两组患者MMSE评分和WMS评分较治疗前明显上升(P0.05或P0.01),且观察组患者上升幅度较对照组更明显(P0.05);同时观察组患者临床总有效率明显优于对照组(χ~2=4.15,P0.05);观察组患者TESS评分为(3.47±0.76)分,明显低于对照组的(4.47±0.89)分。两组患者治疗期间血尿常规、肝肾功能及心电图均无明显异常变化。结论齐拉西酮和奥氮平治疗精神分裂症能明显改善其认知功能,具有良好的临床效果及安全性,且前者改善认知功能及临床效果更佳,安全性较高。     

单磷酸阿糖腺苷联合布地奈德治疗小儿毛细支气管炎的临床研究

目的探讨单磷酸阿糖腺苷联合布地奈德治疗小儿毛细支气管炎的临床疗效。方法选取2014年9月—2016年9月沈阳医学院附属中心医院儿科收治的毛细支气管炎患者151例,随机分成对照组(75例)和治疗组(76例)。对照组雾化吸入吸入用布地奈德混悬液,0.5 mg加入生理盐水3 m L,1次/d,10 min/次。治疗组在对照组的基础上静脉滴注注射用单磷酸阿糖腺苷,0.1 g加入5%葡萄糖溶液100 m L中,1次/d。所有患者均治疗1周。观察两组患者临床效果,对比两组治疗前后症状消失时间、住院时间、炎性指标以及不良反应情况。结果治疗后,对照组和治疗组总有效率分别为84.00%和96.05%,两组总有效率比较差异具有统计学意义(P0.05)。治疗后,治疗组患儿的退热时间、湿啰音消失时间、喘息消失时间和咳嗽消失时间以及住院时间均明显短于对照组,两组比较差异具有统计学意义(P0.05)。治疗后,两组患儿肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)以及IL-8指标均明显降低(P0.05);且治疗组的降低程度明显优于对照组,两组比较差异有统计学意义(P0.05)。结论单磷酸阿糖腺苷联合布地奈德治疗小儿毛细支气管炎,在临床症状消失时间、住院时间以及炎症因子水平改善方面上均优于单独使用布地奈德治疗,具有一定的临床推广应用价值。     

利培酮与齐拉西酮对精神分裂症患者糖脂代谢和细胞因子水平的影响研究

目的:观察利培酮与齐拉西酮对精神分裂症患者糖脂代谢和细胞因子水平的影响。方法:选择76例精神分裂症患者,随机均分为利培酮组和齐拉西酮组。利培酮组患者口服利培酮片,起始剂量为1 mg/d,1周内逐渐加量至4⁶ mg/d;齐拉西酮组患者口服齐拉西酮片,起始剂量为40 mg/d,分2次服用,1周内逐渐加量至1206 mg/d;齐拉西酮组患者口服齐拉西酮片,起始剂量为40 mg/d,分2次服用,1周内逐渐加量至120¹60 mg/d。两组患者均以2周为1个疗程,共治疗4个疗程。比较患者治疗前后血糖、胰岛素、血脂、瘦素(LEP)和细胞因子水平。结果:治疗后两组患者血糖、胰岛素、血脂、LEP水平均较治疗前显著升高,治疗前后比较差异大多有统计学意义(P<0.05),且齐拉西酮组患者空腹胰岛素(FINS)、胰岛素敏感指数(ISI)、LEP升高较利培酮组更显著,利培酮组患者总胆固醇(TC)升高较齐拉西酮组更显著,两组比较差异均有统计学意义(P<0.05);治疗后两组患者细胞因子水平均较治疗前显著降低,治疗前后比较差异均有统计学意义(P<0.05),且利培酮组患者细胞因子水平的改善均优于齐拉西酮组,两组比较差异均有统计学意义(P<0.05)。结论:利培酮与齐拉西酮均可能使精神分裂症患者超重、肥胖和糖尿病的发生率升高,利培酮对患者TC影响较大,齐拉西酮对患者FINS、ISI和LEP影响较大,同时两药可降低精神分裂症患者的细胞因子水平,利培酮对细胞因子水平的改善优于齐拉西酮。     

The Effectiveness of Cross-Tapering Switching to Ziprasidone in Patients with Schizophrenia or Schizoaffective Disorder

Objective

Switching antipsychotics is one useful therapeutic option when the treatment of schizophrenia encounters suboptimal efficacy and intolerability issues. This study aimed to investigate the efficacy and tolerability of cross-tapering switching to ziprasidone from other antipsychotics.

Methods

A total of 67 patients with schizophrenia or schizoaffective disorder were recruited in this 12-week, multicenter, non-comparative, open-label trial. Prior antipsychotics were allowed to be maintained for up to 4 weeks during the titration of ziprasidone. Efficacy was primarily measured using the 18-item Brief Psychotic Rating Scale (BPRS) at baseline, 4 weeks, 8 weeks, and 12 weeks. Efficacy was secondarily measured by the Clinical Global Impression-Severity (CGI-S) scale and the Global Assessment of Functioning (GAF) scale at each visit. Regarding the metabolic effects of switching to ziprasidone, weight, body mass index (BMI), waist-to-hip ratio (WHR), and lipid profile-including triglyceride (TG), high-density lipoprotein (HDL), low-density lipoprotein (LDL), and total cholesterol levels-were measured at each follow-up visit.

Results

The BPRS scores were significantly improved at 12 weeks after switching to ziprasidone (F=5.96, df=2.11, p=0.003), whereas the CGI-S and GAF scores were not significantly changed. BMIs, WHRs, and TG levels were significantly decreased, with no significant changes in other lipid profiles.

Conclusion

Cross-tapering switching to ziprasidone is effective for patients with schizophrenia spectrum disorders. Beyond the efficacy of the procedure, favorable metabolic profiles show that switching to ziprasidone may be helpful for maintenance therapy over an extended period.     

齐拉西酮和奥氮平治疗老年精神分裂症患者的效果及对机体糖脂代谢的影响

目的 分析齐拉西酮、奥氮平对老年精神分裂症患者治疗效果及机体糖脂代谢的影响.方法 选取本中心2018年9月至2019年9月收治的86例老年精神分裂症患者,根据抽签法分为观察组和对照组,各43例.对照组采用奥氮平片口服治疗,观察组采用齐拉西酮口服治疗.比较两组临床疗效及糖脂代谢情况[空腹血糖(FBG)、甘油三酯(TG)及...