氯诺昔康与曲马多在骨科术后患者自控静脉镇痛中的应用

目的:探讨氯诺昔康、曲马多与芬太尼配伍用于患者自控静脉镇痛(PCIA)的镇痛效果比较.方法:60例各类骨科术后中等以上疼痛患者随机分为两组(每组30例),试验组(L组)用芬太尼 氯诺昔康,对照组(T组)用芬太尼 曲马多.芬太尼用量0.02mg·kg-1,根据患者体重计算芬太尼总用量后,分别用8mg氯诺昔康或100mg曲马多替代0.1mg芬太尼.在L组中芬太尼与氯诺昔康各占一半,T组中芬太尼与曲马多各占一半.镇痛泵背景剂量2mL·h-1,PCIA剂量2mL·次-1,锁定时间15min.依据VAS评分标准分别测定术后4,16,24,36,50h的疼痛值,并观察两组在恶心、呕吐等方面不良反应,最后记录镇痛结束时患者对镇痛效果的总体评价.结果:两组镇痛效果VAS评分无显著差异(P>0.05),L组恶心呕吐等不良反应少于T组.结论:氯诺昔康和曲马多分别与芬太尼配伍用于PCIA镇痛效果无显著差异.氯诺昔康在恶心呕吐等不良反应方面优于曲马多.     

氯诺昔康和曲马多术后静脉自控镇痛的临床观察

目的:比较等效剂量的氯诺昔康及曲马多在术后患者自控镇痛(PCIA)时的镇痛效果及不良反应的发生情况.方法:术后中至重度疼痛成年患者100例,随机分为L组及T组,每组50例.应用静注负荷剂量加上维持剂量和患者自控镇痛量(LCP)方式作镇痛治疗.L组应用氯诺昔康0.15mg·kg-1负荷量后,以0.02mg·kg-1·h-1静注维持,T组应用曲马多2.25mg·kg-1负荷量后,维持量是0.3mg·kg-1·h-1,两组自控量均为2mL.结果:镇痛效果VAS评分、48h累积用药量(DT)两组间无显著差异(P>0.05),L组的不良反应明显少于T组,但胃肠道刺激反应的发生率T组较多(P<0.05).结论:使用氯诺昔康治疗外科手术后中至重度疼痛,能取得与曲马多相当的镇痛效果,不良反应发生率较低,但需注意其胃肠道刺激症状.     

氯诺昔康用于食管癌术后镇痛的临床研究

目的:评价氯诺昔康用于食管癌术后镇痛的效果及安全性.方法:选择行食管癌根治术患者60例,接受术后镇痛治疗(PCIA),随机分为L组和T组.L组使用氯诺昔康64mg·48h-1,T组使用曲马多800mg·48h-1.结果:两组于使用PCIA后4,12,24,36,48h的VAS疼痛评分、PHS术后疼痛评分无显著性差异(P＞0.05).镇静度评分:12h以后T组高于L组(P<0.05).术后镇痛不良反应的发生率L组低于T组,两组相比有显著性差异(P<0.05).总体评价L组优于T组.结论:氯诺昔康用于食管癌术后镇痛安全有效,满意度优于曲马多.     

氯诺昔康与曲马多患者自控静脉镇痛的比较

目的:评价氯诺昔康与曲马多自控静脉镇痛的镇痛效果及不良反应.方法:40例ASA Ⅰ～Ⅱ级喉癌根治术患者,随机分为L(氯诺昔康)组和T(曲马多)组,手术缝合时,L组静注氯诺昔康8mg,T组静注曲马多100mg,手术结束前经外周静脉连接自控式镇痛泵.输注模式:背景量2mL·h-1,追加量0.5mL,锁定时间15min.药液配制:L组:氯诺昔康48mg加生理氯化钠溶液至120mL;T组:曲马多1000mg加生理氯化钠溶液至120mL.镇痛期间观察视觉模拟评分(VAS)、舒适评分(BCS)及不良反应.结果:两组比较VAS与BCS均无统计学差异.曲马多组恶心、呕吐、出汗等反应高于氯诺昔康组.结论:氯诺昔康与曲马多都能提供良好的术后镇痛.氯诺昔康伴有较少的不良反应,在临床上更值得应用和推广.     

氯诺昔康与曲马多合用对开胸术术后止痛的疗效

目的:选用氯诺昔康配合曲马多连续静脉输注用于开胸手术患者的术后止痛,观察其止痛效果及不良反应,评估其在胸科术后止痛的价值.方法:90例开胸手术患者,随机分为三组,氯诺昔康 曲马多组(L组),曲马多组(T组)和硬膜外吗啡组(M).每组30例,L组与T组药物均采用曲马多20mg·kg-1 氟哌利多0.1mg·kg-1 生理氯化钠溶液配成100mL,以2mL·h-1速度输注.L组在切皮前和关胸时各用氯诺昔康8mg静注,而T组不用氯诺昔康.M组药物采用吗啡0.12mg·kg-1 0.15%罗哌卡因100mL,行硬脊膜外腔输注.镇痛效果用4点疼痛分级以及VAS进行评估.结果:在8和28h时段,L组VAS评分低于T组(P<0.05).在28和48h时段,L组的4点疼痛分级低于M组(P<0.01).皮肤瘙痒在L组和T组无一例发生,M组有3例(3/30).恶心呕吐发生率三组比较无统计学意义.结论:开胸术后,采用氯诺昔康联合曲马多静脉输注止痛,可等效于硬脊膜外腔吗啡的止痛效果,同时不增加不良反应.     

手术后氯诺昔康静脉自控镇痛的临床研究

目的评价氯诺昔康在手术后患者静脉自控镇痛(PCIA)的临床效果和不良反应。方法96例ASAⅠ～Ⅱ择期手术患者随机分两组:氯诺昔康组(L组,n=48)于手术结束前约30min静注氯诺昔康8mg和丹恩西酮4mg后连接镇痛泵(48mg氯诺昔康+生理盐水至100ml);曲马朵组(T组,n=48)于手术结束前约30min时静注曲马朵100mg和丹恩西酮4mg后连接镇痛泵(800mg曲马朵+生理盐水至100ml),连续量为2ml/h,自控量为0.5ml/15min。术后连续监测BP、RR、ECG、SpO2,定时观察记录视觉模拟评分法(VAS)的评分及恶心、呕吐、嗜睡多汗等不良反应的发生情况。结果两组术后4h、8h、16h、20h、24h、32h和48h的VAS评分接近(P>0.05)。恶心、呕吐、多汗发生率T组明显多于L组(P<0.05)。其他不良反应T组高于L组,但差异无显著意义(P>0.05)。结论氯诺昔康手术后PCIA效果良好,镇痛效果与曲马朵接近,但不良反应较少。     

氯诺昔康与吗啡用于开胸手术后患者自控镇痛的比较

目的:在肋间神经阻滞的基础上,比较氯诺昔康与吗啡用于开胸手术后患者自控镇痛的疗效及不良反应.方法:择期行开胸手术的患者35例,术前均行肋间神经阻滞,术后随机双盲分为两组,给予患者自控镇痛:M组给予吗啡0.5 mg·mL-1 氟哌利多0.02 mg·mL-1,L组给予氯诺昔康0.32 mg·mL-1 氟哌利多0.02 mg·mL-1.镇痛效果评价采用VAS评分.结果:两组患者术后各时段的VAS评分无显著性差异,而不良反应的发生率L组明显少于M组.结论:在术前肋间神经阻滞的基础上,通过PCA系统静脉输注氯诺昔康,也能提供开胸手术后满意的镇痛治疗,疗效与吗啡相似.     

氯诺昔康和高乌甲素用于老年人中上腹部手术后自控镇痛的效果比较

目的比较氯诺昔康和高乌甲素用于老年人中上腹部手术术后自控镇痛的效果和安全性。方法择期行中上腹部手术的老年患者60例，随机分为A、B两组，每组 30例。两组均采用患者静脉自控镇痛(PCIA)，A组给予氯诺昔康32～40 mg，B组给予高乌甲素48～56 mg，用0.9%氯化钠注射液配成100 mL，首次剂量均为8 mg，维持量为2 mL·h^-1，采用视觉疼痛模拟评分(VAS)评估两者镇痛效果并观察镇痛期间可能出现的不良反应。结果A组VAS评分明显低于B组(P＜0.05)；两组术后不良反应的发生率差异无显著性(P＞0.05)。结论氯诺昔康和高乌甲素用于老人中上腹部手术PCIA安全有效，氯诺昔康的镇痛效果优于高乌甲素。     

氯诺昔康复合芬太尼在上腹部手术自控镇痛中的平衡应用

目的:观察氯诺昔康复合芬太尼用于上腹部手术患者自控静脉镇痛(PCIA)的有效性和不良反应.方法:选择择期上腹部手术患者120例,随机分成三组:F组用芬太尼0.6mg 氟哌利多5mg,100mL·48h-1,L组用氯诺昔康48mg 氟哌利多5mg,100mL·48h-1,M组用氯诺昔康32mg 芬太尼0.2mg 氟哌利多5mg,100mL·48h-1.手术结束后,给予负荷剂量8mL,接镇痛泵由患者行PCIA.记录三组患者在1,4,8,16,24及48h等时间点的镇痛(VAS)、镇静(OAA/S)评分及不良反应.结果:F组的基本无痛率(65%)优于L组(55%)与M组(60%),但总的优良率三组间无统计学差异(P>0.05).F组尿潴留、呼吸抑制、恶心呕吐、嗜睡、和皮肤瘙痒等不良反应明显高于L组与M组(P<0.05).结论:氯诺昔康镇痛效果明显,与芬太尼合用于上腹部手术的PCIA镇痛,可减少芬太尼的不良反应,提高镇痛质量.     

氯诺昔康及曲马多用于老年人胆囊切除术后自控镇痛的比较

目的对氯诺昔康在胆囊切除术后自控镇痛的有效性和安全性进行评价.方法将60例行胆囊切除术后的老年患者随机分为两组,L组(氯诺昔康40～48mg+氟哌利多5mg)和T组(曲马多组500～600mg+氟哌利多5mg),观察术后4,8,12,24,32,48h的疼痛程度,镇静评分,恶心、呕吐、尿潴留等不良反应发生情况.结果L组和T组在镇痛效果上无显著差别,但L组中恶心、呕吐等不良反应发生率明显低于T组.结论氯诺昔康用于老年人胆囊切除术后自控镇痛效果确切,不需特别减量,不良反应少,在老年人胆囊切除术后自控镇痛中使用较为理想.     

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.