齐拉西酮与喹硫平治疗早期精神分裂症的对照研究

目的：比较齐拉西酮与喹硫平治疗早期精神分裂症的疗效及不良反应。方法100例精神分裂症患者随机分为齐拉西酮组与喹硫平组,各50例,分别给予齐拉西酮和喹硫平治疗8周,采用阳性症状与阴性症状量表(PANSS)和不良反应症状量表(TESS)评定疗效及不良反应。结果治疗8周后,齐拉西酮组与喹硫平组显效率为84.00%、80.00%,总有效率96.00%、94.00%,疗效差异无统计学意义(P>0.05)。齐拉西酮组与喹硫平组的不良反应发生率为18.00%、20.00%,差异无统计学意义(P>0.05)。结论齐拉西酮与喹硫平对早期精神分裂症的疗效相当,不良反应相当。     

齐拉西酮与奎硫平治疗精神分裂症的疗效与安全性比较

目的 比较齐拉西酮与奎硫平治疗精神分裂症的临床疗效与安全性.方法 选择符合入组条件的精神分裂症或分裂样精神病住院患者60例,随机均分为口服齐拉西酮片的治疗组和口服奎硫平片的对照组,疗程均为6周.主要疗效用精神分裂症阳性与阴性症状评定量表(PANSS)评定,安全性用不良反应量表(TESS)评定.结果 治疗结束时PANSS减分率治疗组为(60.98±24.04)%,对照组为(61.99±28.25)%;临床总有效率治疗组为80.00%,对照组为76.67%,两组间疗效比较差异无显著性(P>0.05);不良反应的发生率两组间亦无显著性差异(P>0.05).结论 齐拉西酮与奎硫平治疗精神分裂疗效相当且均能有效治疗精神分裂症的各种症状,不良反应二者相当,且均为轻度,是一种有效、安全的抗精神病药物.     

阿立哌唑与奎硫平治疗首发性精神分裂症的对照研究

目的比较阿立哌唑与奎硫平对首发性精神分裂症的疗效及安全性。方法 80例首发性精神分裂症患者,随机分为阿立哌唑组(40例)和奎硫平组(40例),疗程8周。采用阳性和阴性症状量表(PANSS)、临床总体印象量表(CGI)及副反应症状量表(TESS),在治疗基线时及治疗第2、4、6、8周末分别评定疗效和副反应。结果(1)治疗第8周末,阿立哌唑组、奎硫平组临床总有效率分别为87.5%、85.0%,差异无统计学意义(P0.05)。(2)治疗第2周末起,两组CGI-SI分较基线时下降(P0.05);两组间各时点CGI-SI分比较差异无统计学意义(P0.05);(3)阿立哌唑组、奎硫平组不良反应发生率分别为20.0%、22.5%,差异无统计学意义(P0.05)。奎硫平组嗜睡、心率影响发生率高于阿立哌唑组。结论阿立哌唑及喹硫平治疗首发性精神分裂症疗效较好,不良反应轻,患者耐受性好,值得临床推荐使用。     

奎硫平与利培酮治疗精神分裂症的对照研究

目的探讨奎硫平治疗精神分裂症的效果与不良反应。方法将90例精神分裂症患者随机分为奎硫平治疗组和利培酮治疗组,各45例。于治疗前及治疗第1、2、4、8周末采用阳性与阴性症状量表（PANSS）评价临床疗效,副反应量表（TESS）评价不良反应。结果奎硫平组治疗有效率为75.6%高于利培酮组的73.3%,差异无统计学意义（P〉0.05）。奎硫平组锥体外系不良反应明显少于利培酮组（P〈0.05）,其他不良反应2组比较差异均无统计学意义（P〉0.05）。结论奎硫平治疗精神分裂症疗效肯定,不良反应少,依从性好。     

齐拉西酮与喹硫平治疗老年精神分裂症的对照分析

目的探讨齐拉西酮治疗老年精神分裂症的疗效和安全性。方法将60例符合中国精神障碍分类与诊断标准第三版(CCMD-3)的老年精神分裂症的患者,随机分成齐拉西酮组和喹硫平组治疗。每组30例,疗程8周。采用阳性和阴性症状量表(PANSS)不良反应量表(TESS)评定疗效和不良反应。结果齐拉西酮组有效率为90%,喹硫平为86.7%,两组疗效相当,两组治疗后各时点PANSS总分,阳性症、阴性症状及一般病理现状,各项分值均低于治疗前,而治疗后各时点组间差异无统计学意义(P>0.05)。齐拉西酮组很少引起锥体外系反应和体质量增加的发生。结论齐拉西酮治疗老年精神分裂症疗确切不良反应少,有利于老年患者对治疗的依从性,对老年精神分裂症患者较为适用。     

喹硫联合舍曲林治疗以阴性症状为主的精神分裂症效果观察

目的 观察喹硫平联合舍曲林治疗阴性症状为主的精神分裂症的疗效与不良反应.方法 本组患者80例,随机分为研究组和对照组各40例,2组均给予喹硫平治疗,研究组在此基础上给予舍曲林,采用阳性与阴性症状量表(PANSS)和临床疗效总评量表(CGI-GI)评定疗效,不良反应量表(TESS)评定不良反应.结果 研究组总有效率为87.5%,对照组为80.0%,差异无统计学意义(P>0.05).2组治疗后PANSS评分均低于治疗前,且研究组治疗4、8周后阴性症状PANSS评分低于对照组,差异均有统计学意义(P<0.05和P<0.01),2组间不良反应的发生率比较差异无统计学意义(P>0.05).结论 喹硫平联合舍曲林治疗以阴性症状为主的精神分裂症起效快,疗效好.     

喹硫平与利培酮治疗精神分裂症的临床疗效对照观察

目的 探讨喹硫平治疗精神分裂症的疗效及安全性.方法 选取2011年2月-2012年7月在我院治疗的精神分裂症患者98例为研究对象,平均分为治疗组和对照组各49例,治疗组采用喹硫平治疗,对照组采用利培酮治疗,两组的疗程相同.采用潘氏量表及不良反应量表评定疗效和不良效应.结果 治疗组总有效率85.7%,对照组总有效率63.2%,治疗组有效率高于对照组,差异有统计学意义（P＜0.05）.对照组患者在治疗4周末疗效明显,潘氏量表（PANSS）评定总分与治疗前比较差异有统计学意义（P＜0.05）,治疗组患者在治疗2周末疗效明显,PANSS评定总分与治疗前比较差异有统计学意义（P＜0.05）;两组患者的PANSS评定总分在治疗前、1周末、2周末比较差异均无统计学意义（P＞0.05）,在4周末、6周末、8周末差异有统计学意义（P＜0.05）.两组不良反应发生率比较差异无统计学意义（P＞0.05）.结论 喹硫平治疗精神分裂症疗效显著、安全,可在临床进一步推广应用.     

奎硫平与利培酮对精神分裂症伴抑郁症状疗效的对照研究

目的:比较奎硫平与利培酮对精神分裂症伴抑郁症状的疗效.方法:将符合条件的60例首发精神分裂症患者随机分成两组,分别给予奎硫平(奎硫平组)和利培酮(利培酮组)治疗8周,以阳性与阴性症状量表(PANSS)及汉密尔顿抑郁量表(HAMD)评定临床疗效;以副反应量表(TESS)和相关检查评定不良反应.结果:治疗后两组患者PANSS评分均明显下降,两组之间差异无显著性(P均＞0.05),但奎硫平起效较快,且在治疗后阴性症状评分比较,奎硫平改善显著(P＜0.05);治疗后两组患者HAMD评分均明显下降,两组间比较,奎硫平组改善抑郁疗效优于利培酮组(P＜0.05),奎硫平组的副反应发生率低于利培酮组,但差异无显著性.结论:奎硫平和利培酮治疗精神分裂症的精神病性症状疗效相当,奎硫平对精神分裂症的抑郁症状及阴性症状的改善好于利培酮,两者副反应较轻.     

齐拉西酮与利培酮治疗精神分裂症的对照研究

目的 观察齐拉西酮与利培酮治疗精神分裂症的疗效及不良反应,并进行比较分析.方法 将100例精神分裂症患者随机分为两组,齐拉西酮组与利培酮组,分别给予齐拉西酮与利培酮治疗,每组各50例,进行为期8周治疗观察.采用阳性与阴性症状量表(PANSS)评定临床疗效,采用副反应量表(TESS)、体质量指数、空腹血糖、心电图QT 间期评定不良反应.结果 治疗8周两组PANSS评分较治疗前均显著降低(均P<0.05),各时点PANSS评分两组间减分差异无统计学意义(P>0.05).治疗8周末,两组间比较差异无统计学意义(P>0.05).齐拉西酮组锥体外系反应(静坐不能)、体重增加、失眠等副反应与利培酮相比差异有统计学意义(P< 0.05).结论 齐拉西酮与利培酮对精神分裂症患者的疗效相仿,但齐拉西酮比利培酮较少引起静坐不能、体质量改变,具有安全性方面的优势,是较为理想的抗精神分裂症药物.     

奎硫平与利培酮治疗精神分裂症的对照研究

目的:比较奎硫平与利培酮治疗精神分裂症的疗效和安全性。方法:选取60例精神分裂症患者,随机平分为奎硫平组与利培酮组,治疗8周,在治疗前及治疗后2、4、8周末分别采用阳性与阴性症状量表(PANSS)和副反应量表(TESS)进行评定。结果:两组治疗后较治疗前PANSS评分均有显著下降,两组间比较无显著差异。两组TESS评定,锥体外系反应,月经紊乱,失眠、体重增加,嗜睡、口干、便秘、视物模糊等不良反应的差异有显著性。结论:两药对精神分裂症均有较好疗效,但利培酮组出现锥体外系反应,月经紊乱、失眠、多于奎硫平组。而奎硫平组出现嗜睡、体重增加、口干、便秘、视物模糊多于利培酮组。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.