比较奥氮平与氟哌啶醇对青年精神分裂症患者血清生长激素的影响

目的 比较研究奥氮平和氟哌啶醇对青年精神分裂症患者生长激素(GH)水平的影响.方法 用化学发光法测定51例青年精神分裂症患者奥氮平与氟哌啶醇治疗前后的GH水平,并与20例健康者作对照.奥氮平组29例,剂量(14±7)mg·d~(-1),氟哌啶醇组22例,剂量(26±8)mg·d~(-1),均疗程8周.结果 治疗前,青年精神分裂症患者(含2组)与健康者GH分别为(2.24±1.32),(2.48±1.67)μg·L~(-1)(P＞0.05).治疗8周后,奥氮平组于治疗前后的GH分别为(2.62±1.40),(2.30±1.51)μg·L~(-1),差异无统计学意义(P＞0.05);而氟哌啶醇GH分别为(1.42±0.87),(2.49±1.10)μg·L~(-1),差异有统计学意义(P＜0.01).结论 氟哌啶醇能使青年精神分裂症患者GH水平显著降低;而奥氮平对青年精神分裂症患者GH水平无明显影响,安全性较好.     

喹硫平与氟哌啶醇治疗首发精神分裂症对照研究

目的比较喹硫平与氟哌啶醇治疗首发精神分裂症的疗效及安全性。方法将71）例首发精神分裂症患者随机分为两组,喹硫平组35例,氟哌啶醇组35例。两组分别应用喹硫平或氟哌啶醇治疗,疗程8周。采用PANSS量表评定临床疗效和不良反应。结果治疗第8周末,喹硫平组显效率为75．21％,氟哌啶醇组76．11％,两组总体疗效相当,喹硫平组不良反应明显少于氟哌啶醇组（P〈005）。结论喹硫平与氟哌啶醇治疗首发精神分裂症疗效相当,但喹硫平不良反应少,安全性高。     

喹硫平和氟哌啶醇治疗首发精神分裂症对比研究

目的比较喹硫平和氟哌啶醇治疗首发精神分裂症的疗效和安全性。方法将首发精神分裂症患者60例随机分为2组,各30例,分别单用喹硫平和氟哌啶醇进行8周治疗,采用阳性和阴性症状量表（PANSS）、不良反应量表（TESS）于治疗前、治疗2周、4周和8周末评定疗效和不良反应。结果2组治疗后2周、4周、8周PANSS总分及各因子分与治疗前比较均有显著性差异（P〈0.05或P〈0.01）;第8周末喹硫平组PANSS总分及阴性症状因子分较氟哌啶醇组显著降低（P〈0.05或P〈0.01）。喹硫平组不良反应发生率显著低于氟哌啶醇组（P〈0.01）。结论喹硫平对精神分裂症阴性症状疗效优于氟哌啶醇,且不良反应较轻。     

评价喹硫平治疗中国精神分裂症患者急性期兴奋激越的疗效和安全性

目的探讨喹硫平治疗中国精神分裂症患者急性期兴奋激越的临床疗效及安全性。方法选取100例急性期兴奋激越精神分裂症患者随机分为观察组与对照组,每组50例。对照组给予药物氟哌啶醇治疗,观察组给予药物喹硫平治疗,均连续用药8周。结果观察组患者治疗总有效率(90%)明显高于对照组(68%)(P<0.05);而观察组患者不良反应发生率(4%)明显低对照组(60%)(P<0.05)。结论喹硫平治疗中国精神分裂症患者急性期兴奋激越临床效果显著,优于氟哌啶醇治疗。     

喹硫平与氟哌啶醇治疗老年痴呆患者精神行为症状的对照研究

目的:对比观察喹硫平与氟哌啶醇治疗老年痴呆患者精神行为症状的临床疗效和安全性。方法:选取2012年7月—2013年8月收治的老年痴呆伴精神行为功能障碍患者164例,以随机数字表法分为喹硫平组和氟哌啶醇组各82例,前者给予喹硫平(145±50)mg/d治疗,后者给予氟哌啶醇(4.5±1.5)mg/d治疗。治疗2周后,观察2组患者的痴呆病理性评分、疗效及不良反应发生情况。结果:治疗后,2组患者的痴呆病理性评分均明显降低,2组治疗前后的差异均有统计学意义(P<0.05);治疗后,喹硫平组患者的痴呆病理性评分明显低于氟哌啶醇组,差异有统计学意义(P<0.05)。氟哌啶醇组患者不良反应发生率为46.9%(35/82),喹硫平组为31.3%(26/82),喹硫平组患者的不良反应发生率明显低于氟哌啶醇组,差异有统计学意义(P<0.05)。结论:与氟哌啶醇相比,喹硫平治疗老年痴呆患者精神行为症状的疗效更显著,且不良反应发生率低,能有效促进老年痴呆患者精神行为功能快速恢复。     

奥氮平、氟哌啶醇对精神分裂症病人血清催乳素和生长激素的影响

目的:探讨精神分裂症病人催乳素(PRL)和生长激素(GH)的基础水平与正常人的差异,及奥氮平、氟哌啶醇治疗前后PRL,GH水平的变化。方法:采用放射免疫法测定61例精神分裂症病人治疗前和治疗8wk末的PRL和GH水平,并与30名健康者对照,同时将61例精神分裂症病人分为奥氮平治疗组28例和氟哌啶醇治疗组33例,观察药物对PRL和GH水平的影响。结果:精神分裂症病人的基础PRL,GH水平与对照组差异无显著意义(P>0.05);奥氮平组治疗8wk末PRL,GH均无显著改变(P>0.05);氟哌啶醇组治疗8wk末PRL值为(99±48)μg·L-1,较治疗前(17±10)μg·L-1显著增高(P<0.01),GH值为(1.6±1.4)μg·L-1,较治疗前(2.4±1.6)μg·L-1显著降低(P<0.01)。结论:精神分裂症病人PRL和GH的基础水平与正常群体差异不显著。奥氮平对PRL,GH无明显影响,氟哌啶醇致PRL升高,GH降低。     

阿立哌唑与喹硫平治疗精神分裂症的疗效和安全性

目的 评价阿立哌唑与喹硫平治疗精神分裂症的疗效及安全性.方法 169例符合DSM-Ⅳ(第4版)精神分裂症患者,阿立哌唑组79例,剂量10～30mg·d-1;喹硫平组90例,剂量400～ 750 mg·d-1,疗程均8周.治疗前,治疗第4,8周用阳性和阴性症状量表(PANSS)评价主要疗效.用实验室检查、生命体征、心电图等评价安全性.结果 2组治疗4,8周PANSS总分均较治疗前有显著下降(P均＜0.01),治疗8周末,PANSS总分减分差值及疗效2组间差异无统计学意义.2组药物不良反应发生率分别为25.3％(20/79)和17.7％ (16/90).阿立哌唑组对心率的影响较喹硫平组小;阿立哌唑组甘油三酯水平和心电图QRS间期较治疗前变化明显(P＜0.05).喹硫平组心率、体重、体重指数、血红蛋白、总胆固醇和低密度脂蛋白较治疗前变化明显(P＜0.01).结论 阿立哌唑与喹硫平对精神分裂症疗效相当,两者所致不良反应发生率相近.     

喹硫平治疗精神分裂症患者急性期兴奋激越的疗效和安全性分析

目的探讨喹硫平治疗精神分裂症患者急性期兴奋激越的疗效和安全性。方法将100例精神分裂症患者机均分为对照组与观察组,分别采用氟哌啶醇与喹硫平进行治疗。比较两组临床疗效及治疗前后血清PBL、PANSS量表评分变化情况及不良反应发生率。结果对照组临床总有效率为66.00%,显著低于观察组(90.00%),差异具有统计学意义(P<0.05);对照组患者治疗前后PBL值分别为(42.02±11.27)与(24.96±5.86),观察组患者治疗前后分别为(41.79±11.04)与(13.58±4.24),两组治疗前后PBL水平差异均具有统计学意义(P<0.05),且两组治疗后PBL水平差异也具有统计学意义(P<0.05);对照组患者治疗前后PANSS量表评分分别为(57.02±18.97)分与(49.93±8.96)分,观察组患者治疗前后分别为(57.83±19.01)分与(43.09±10.24)分,两组患者治疗前后PANSS量表评分差异均具有统计学意义(P<0.05),且两组治疗后PANSS评分差异也具有统计学意义(P<0.05);对照组不良反应发生率为22.00%,显著高于观察组(10.00%),差异具有统计学意义(P<0.05)。结论与氟哌啶醇相比,喹硫平治疗精神分裂症患者急性期兴奋激越的疗效更为显著,安全性相对较高,应加以推广应用。     

卡马西平联合喹硫平对痴呆患者精神行为症状的疗效

目的观察卡马西平联合喹硫平治疗痴呆患者精神行为症状的临床疗效。方法痴呆患者96例,分为治疗组46例,对照组50例。治疗组给予喹硫平25～300 mg.d-1,平均(160.4±135.2)mg.d-1;卡马西平0.3～0.6 g.d-1,平均(0.49±0.25)g.d-1,在1周内联合用药;对照组给予喹硫平25～400 mg.d-1,平均(260.5±235.4)mg.d-1,均口服,共观察8周。治疗期间禁用其他抗精神病药,锥体外系反应明显时可使用苯海索1～2 mg.d-1;严重失眠者晚间可短期使用苯二氮类药物辅助睡眠。用简易智能状态检查量表(MMSE)、痴呆病理行为评定量表(BEHAVE-AD)和不良反应量表(TESS)于治疗前,治疗第1,2,4,6,8周末评价临床疗效及不良反应。结果治疗组和对照组总有效率分别为84.8%,87.5%。两组疗效在第4周差异有统计学意义,在第8周差异无统计学意义(P>0.05),且两组间治疗4,6周末BEHAVE-AD总分和攻击行为因子分差异有统计学意义(P<0.05),两组间不良反应发生率差异有统计学意义(P<0.01)。结论卡马西平联合喹硫平对痴呆患者精神行为症状疗效确切,可减少喹硫平用量及不良反应,对精神行为控制较快,疗效相对明显。     

国产与进口喹硫平治疗精神分裂症的疗效比较

目的:评价国产与进口喹硫平治疗精神分裂症的临床疗效及安全性.方法:随机选择本院门诊及住院精神分裂症患者76例,分为试验组38例和对照组38例,分别口服国产及进口喹硫平150～600 mg·d-1,疗程8周.结果:试验组痊愈率为65.8%,有效率为89.5%;对照组痊愈率为68.4%,有效率86.8%,两组疗效差异无显著性(P>0.05).两组的不良反应均轻微,安全性好,常见的不良反应有失眠、激越、嗜睡、头疼、心动过速、体位性低血压和体重增加.结论:国产喹硫平对精神分裂症的疗效肯定,使用安全性和耐受性好,与进口喹硫平疗效相当.     

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.     

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.     

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.     

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.