尿激酶联用硫酸镁治疗急性心肌梗塞的研究

目的 评价尿激酶（UK）联用硫酸镁（MS）治疗急性心肌梗塞（AMI）的临床疗效及安全性。方法 151例AMI住院患随机分为UK＋MS组（UM组，76例）和UK组（75例），除UM组在静滴UK前15min开始加用MS外，余相同。结果 UM组的再通率有高于UK组趋势，而5周病死率、心力衰竭、梗塞后心绞痛、再梗塞及梗塞延展的发生率均明显低于UK组（P均＜0.01）。结论 UK联用MS治疗AMI优于UK疗法，MS可作为一种安全有效的溶栓治疗辅助剂。     

急性心肌梗塞溶栓后肝素应用的临床观察(附225例报告)

应用溶栓剂尿激酶（UK）治疗急性心肌梗塞（AMI），国内外已有诸多报道，溶栓成功后的心梗延展和再梗受到人们关注。本文就溶栓后预防性应用肝素的临床研究报告如下。资料与方法对象：225例1992年1月～1996年12月本院收治的AMI患者，AMI诊断依据：持续心前区痛＞30分钟，ECG至少相邻导联ST段水平抬高＞lmm。按入院单、双日随机编为A、B两组。A组135例，男106例、女29例，年龄28～70岁。平均58．5岁。B组90例，男65例，女25例，年龄36～70岁，平均59．8岁。两组之间性别、年龄、梗塞部位、溶栓时间及入院时并发症无明显差别。方法：…     

尿激酶联用硫酸镁治疗急性心肌梗塞的研究

目的评价尿激酶(UK)联用硫酸镁(MS)治疗急性心肌梗塞(AMI)的临床疗效及安全性。方法151例AMI住院患者随机分为UK MS组(UM组 ,76例)和UK组(75例) ,除UM组在静滴UK前15min开始加用MS外 ,余相同。结果UM组的再通率有高于UK组趋势 ,而5周病死率、心力衰竭、梗塞后心绞痛、再梗塞及梗塞延展的发生率均明显低于UK组(P均<0.01)。结论UK联用MS治疗AMI优于UK疗法 ,MS可作为一种安全有效的溶栓治疗辅助剂。     

急性心肌梗死溶栓后ST段变化对预后的影响

目的探讨急性心肌梗死(AMI)静脉溶栓后ST段升高对预后的临床意义。方法回顾本院收治2009-2011年收治、经尿激酶(UK)溶栓治疗ST段再抬高的AMI患者43例(观察组),及同期收治、经UK溶栓治疗ST段无再抬高的AMI患者47例(对照组),对其预后做分析对比。结果观察组CPK、CK-MB峰值、心绞痛发生率、心率失常发生率和1年内死亡率明显都显著高于对照组(P<0.05),心功能状态显著低于对照组(P<0.05)。结论 AMI患者溶栓治疗后ST段升高对预后质量有重要影响,用心电图监测ST段动态变化的方法来评判早期AMI临床预后及中远期治疗,简便、无创、可靠性高。     

国产注射用比伐卢定对大鼠血栓模型血小板活化功能的影响

目的探讨国产注射用比伐卢定（domesticbivalimdin）对大鼠颈总动脉血栓模型血小板活化功能的影响。方法建立大鼠左颈总动脉血栓模型,分为对照组（n=6）、模型组（n=10）、国产注射用比伐卢定联合尿激酶（urokinase,UK）组（B＆UK组,n=10）、肝素（heparin）联合尿激酶组（H＆UK组,n=10）,检测各组治疗前后GMP-140含量及血栓重量。结果与模型组比较,B＆UK组及H＆UK组血栓重量均明显减轻,而B＆UK组与H＆UK组之间血栓重量比较差异无统计学意义。模型组、B＆UK组及H＆UK组GMP-140含量均显著高于对照组;而治疗后GMP-140含量在B＆UK组显著低于模型组,相反治疗后GMP-140含量在H＆UK组则显著高于模型组。结论国产注射用比伐卢定能在模型中有效抑制血栓形成,但相比肝素,国产注射用比伐卢定能显著抑制血小板活化功能,抑制血小板聚集。在抑制血栓形成过程中国产注射用比伐卢定对血小板活化的影响具有更多优势。     

急性心肌梗死早期溶栓治疗的疗效

目的 探讨早期应用尿激酶（UK）对急性心肌梗死（AMI）溶栓效果及安全性。方法121例AMI随机分为治疗组和对照组治疗组：治疗组A发病3h内（含3h）予UK100万U＋N．S100ml,20min内静滴完毕;治疗组B发病3～6h内（含6h）予UK150万U＋N．S100ml,30min内静滴完毕;治疗组C发病6～12h内,予UK150万U＋N,S100ml,30min内静滴完毕。对照组：未应用UK溶栓治疗。二组其他常规治疗相同。结果 治疗组冠脉再通率、心功能改善率及死亡率分别为52．44％、91．4％及4．88％,较对照组的7．69％、66．67％及20．51％,差异有显著性（P〈0．01）,且治疗组不同溶栓时间上述指标差异也有显著性（P〈0．05）。结论 早期静脉溶栓治疗AMI可提高冠脉再通率,降低病死率,改善心功能,方便安全,且愈早愈好,在基层医院不失为一种最佳再灌注治疗策略。     

急性心肌梗塞尿激酶治疗临床观察（附10例报告）

急性心肌梗塞（AMI）随着冠脉再灌注治疗，冠状动脉球囊成形术，冠脉搭桥术及药物溶栓等，病死率逐步下降。本文就我院近两年来AMI静脉溶栓治疗的效果报告如下。临床资料对象：AMI患者共20例，回顾性分（l）治疗组10例，男9例，女1例，年龄59～73（平均68．3）岁；梗塞部位：前壁（包括广泛前壁、侧壁、前间壁，下同）4例，下壁6例。其中3例合并心源性休克。（2）对照组10例，男9例，女1例，年龄40～78（平均62．9）岁；梗塞部位：前壁4例，下壁6例。l例合并心源性休克。方法：治疗组采用南京大学制药厂生产的注射用尿激酶（UK），分子…     

急性心肌梗死溶栓治疗与介入治疗的效果对比分析

目的比较直接经皮冠状动脉介入（PCI）治疗与尿激酶（UK）静脉溶栓治疗急性心肌梗死（AMI）患者的近期临床效果。方法选取本院2009年12月～2012年12月收治的AMI患者174例,分为溶栓组68例和PCI组106例,对比两组患者梗死相关动脉血管（IRA）再通率、病死率、严重并发症发生率、平均住院时间。结果PCI组IRA再通率明显高于溶栓组,差异有统计学意义（P〈0．05）;PCI组病死率明显低于溶栓组,差异有统计学意义（P〈0．05）;PCI组严重并发症发生率明显低于溶栓组,差异有统计学意义（P〈0．05）;PCI组平均住院时间明显短于溶栓组,差异有统计学意义（P〈0．05）。结论AMI直接PCI治疗优于溶栓治疗。     

不同溶栓方法治疗AMI对再通和PLT的影响

目的研究不同静脉溶栓方法在AMI（急性心肌梗死）溶栓再通及PLT（血小板）变化。方法将95例AMI随机分为两组,观察组48例,UK（尿激酶）30万U静推,120万U静滴溶栓治疗AMI;对照组47例,UK静滴溶栓治疗AMI,研究两组治疗后再通率和PLT变化。结果观察组溶栓再通率和PLT聚集率明显优于对照组,观察组溶栓再通率为64．58％,对照组为51．06％,差异有显著性（P〈0．05）。结论观察组比对照组溶栓再通率高且PLT聚集显著。     

尿激酶溶栓治疗老年人急性心肌梗死临床观察

目的：探讨尿激酶（UK）溶栓治疗老年急性心肌梗死（AMI）的溶栓效果和不良反应。方法：对22例老年人AMI患给予UK溶栓治疗，观察溶栓再通率和不良反应发生率，并与常规治疗组比较。结果：溶栓再通率为72．7％，较再通率较非溶栓组高（P＜0．05），不良反应没有增加。结论：UK溶栓治疗AMI疗效较，副反应轻。     

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.     

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.