纤溶酶序贯蚓激酶联合阿司匹林预防脑梗死复发的临床疗效观察

目的观察纤溶酶序贯蚓激酶联合阿司匹林预防脑梗死复发的临床疗效。方法 73例符合入组要求的脑梗死患者随机分成对照组和治疗组,对照组在急性期静脉纤溶酶治疗7天后单独服用小剂量肠溶阿司匹林,治疗组在纤溶酶治疗结束后联合服用阿司匹林及蚓激酶,随访12个月,观察患者纤维蛋白原水平及神经功能恢复情况,同时记录复发率及出血事件发生率。结果在常规治疗基础上加用小剂量降纤治疗(纤溶酶序贯蚓激酶),改善神经功能缺损方面疗效优于对照组,且能减少梗死复发率。联合使用不增加出血危险及肝肾毒性。结论常规治疗基础上加用小剂量降纤治疗(纤溶酶序贯蚓激酶)能明显提高临床疗效,有效预防缺血性卒中复发,且副作用较小、耐受性好。     

降纤和抗凝治疗进展性脑梗死的疗效研究

目的观察单纯巴曲酶、低分子肝素以及二者联合治疗进展性脑梗死的临床疗效。方法选择入院1周内进展性脑梗死患者88例随机分为降纤组、抗凝组、联合组和对照组,各22例;降纤组于入院第1、3、5天内分别予巴曲酶10单位、5单位、5单位;抗凝组予低分子肝素5000U,皮下注射,2次/d,一共10d;联合治疗组于入院第1、3、5天内分别予巴曲酶10单位、5单位、5单位,第6天予低分子肝素5000U皮下注射,2次/d,一共5d;各组均口服肠溶阿司匹林100mg,1次/d、同时静脉滴注奥扎格雷钠40mg和吡拉西坦8g,均1次/d,治疗10d;对照组仅采用口服肠溶阿司匹林100mg,1次/d、静脉滴注奥扎格雷钠40mg和吡拉西坦8g,均1次/d,治疗10d;治疗前和治疗10d后患者临床神经功能缺损评分进行评定,比较疗效。结果 10d后联合治疗组较降纤组、抗凝组和对照组患者的美国国立卫生院神经功能缺损评分(NIHSS)明显降低(P<0.05),联合治疗组的临床疗效明显优于其他各组(P<0.05)。结论巴曲酶和低分子肝素联合治疗进展性脑梗死效果明显。     

OCSP亚型脑梗死对巴曲酶疗效的差异

目的观察巴曲酶对不同OCSP亚型脑梗死降纤治疗的疗效差异。方法 102例行巴曲酶治疗的脑梗死患者,按照OCSP标准分为部分前循环梗死（PACI）组,完全前循环梗死（TACI）组,后循环梗死（POCI）组和腔隙性梗死（LACI）组,观察神经功能的改善情况。结果在脑梗死治疗后7和14 d,神经功能缺损评分和日常生活活动能力评定改善的有效率在组间均存在显著差异,以部分前循环梗死（PACI）恢复最为明显,后循环梗死（POCI）、腔隙性梗死（LACI）疗效次之,完全前循环梗死（TACI）最差。结论巴曲酶对不同OCSP亚型脑梗死具有不同的疗效,此对于降纤治疗具有一定的指导意义。     

巴曲酶联合低分子肝素治疗急性进展性脑梗死40例疗效观察

目的：观察巴曲酶与低分子肝素联合治疗急性进展性脑梗死的临床疗效及安全性。方法：120例急性进展性脑梗死病例随机分为巴曲酶组、低分子肝素组、巴曲酶联合低分子肝素治疗组（联合治疗组）。巴曲酶组患者给予巴曲酶10BU静脉滴注每日1次，连用3d；低分子肝素组给予低分子肝素5000U皮下注射，每日2次，连用10d；联合治疗组给予巴曲酶10BU静脉滴注每日1次，连用3d，及低分子肝素5000U皮下注射，每日2次，连用10d。于治疗前、治疗后7d，14d时进行神经功能缺损程度评分（NDS），在治疗前、治疗后10d进行凝血指标检测。结果：联合治疗组总有效率（97．5％）明显高于巴曲酶组（77．5％）与低分子肝素组（70％）（均P〈0．05）。各组治疗前后凝血酶原时间、活化部分凝血酶时间、凝血酶时间差异均无统计学意义。联合治疗组和巴曲酶组经治疗，血浆蛋白原含量比治疗前显著降低（均P〈0．01）。联合治疗组5例，巴曲酶组1例，低分子肝素组2例出现轻微皮下、牙龈出血，无其他不良反应。结论：巴曲酶与低分子肝素联合治疗急性进展性脑梗死的疗效较好，优于单独使用巴曲酶或低分子肝素，且无明显不良反应。     

不同剂量巴曲酶治疗动脉粥样硬化性脑梗死的临床观察

目的研究不同剂量巴曲酶治疗动脉粥样硬化性脑梗死的临床疗效。方法将132例发病72 h内的动脉粥样硬化性脑梗死患者随机分为巴曲酶常规治疗组（A组）50例,大剂量延长疗程组（B组）44例和灯盏花对照组（C组）38例,观察3组治疗前7、14、30 d的神经功能缺损评分（NIHSS）及纤维蛋白原含量的变化。结果B组患者治疗后7、14、30 d的NIHSS与A组和C组相比,有明显改变（P〈0.05）,B组血浆纤维蛋白原水平与A组相比差异无统计学意义（P〉0.05）,但2组血浆纤维酶原水平明显低于C组（P〈0.05）。结论巴曲酶能改善动脉粥样硬化性脑梗死的预后,尤以B组效果最理想,是治疗动脉粥样硬化性脑梗死的有效药物之一。     

蚓激酶胶囊治疗急性脑梗死的临床研究

目的观察蚓激酶胶囊治疗急性脑梗死的疗效。方法选择入院的急性脑梗死患者83例,随机分为常规治疗组（对照组）和在常规治疗基础上加用蚓激酶胶囊（治疗组）。分别在治疗前、治疗3周测定凝血功能、血流变学及神经功能评分,并进行比较。结果治疗3周后,两组均有改善,但是治疗组恢复明显,治疗组有效率为88.89%,对照组71.05%（P〈0.05）。结论蚓激酶胶囊能有效降低纤维蛋白原及血浆黏度,改善神经功能缺损。     

巴曲酶联合低分子肝素治疗急性脑梗死疗效观察

目的　比较研究单纯纤溶、抗凝及联合应用治疗急性脑梗死的疗效。方法　将 134例急性脑梗死患者随机分为纤溶组 (A组 )、抗凝组 (B组 )、纤溶 +抗凝组 (C组 ) ,A组于入院第 1、 3、 5天分别加用巴曲酶 10Bu、 5Bu、 5Bu静滴 ;B组于低分子肝素 0 4ml腹壁皮下注射每天 2次 ,连用 10天 ;C组用药的前 5天同A组 ,第6天起同B组。结果　A组的临床总有效率优于B组及C组 ,且不良反应无明显差异 ((P >0 0 5 )。结论　联合应用巴曲酶和低分子肝素能有效提高神经功能评分。     

巴曲酶治疗老年人进展性脑梗死的疗效观察

目的 观察巴曲酶对老年人急性脑梗死的治疗效果。方法 将老年进展性脑梗死患者随机分为巴曲酶治疗组和常规治疗组各26例。巴曲酶治疗组在常规治疗基础上加用巴曲酶，隔日1次，共用3次，每次10BU加入生理盐水250ml静脉滴注，于入院时及治疗14d后进行神经功能缺损评分。结果 巴曲酶治疗组基本痊愈5例，显著进步12例，进步6例，无变化2例，恶化1例；对照组基本痊愈2例，显著进步4例，进步10例，无变化7例，恶化3例，两组疗效比较，差异有统计学意义（P〈0.05）。结论 巴曲酶能明显改善老年进展性脑梗死患者的临床症状。     

蚓激酶联合血塞通治疗急性脑梗死临床观察

目的评价蚓激酶胶囊联合血塞通粉针治疗急性脑梗死的疗效和安全性。方法将120例急性脑梗死患者随机分为治疗组和对照组各60例,治疗组口服蚓激酶胶囊并静滴血塞通粉针,对照组静滴复方丹参粉针,均以14d为1疗程;观察两组患者治疗前后的凝血、纤溶、血液流变学指标,并评价患者的神经功能缺损程度和临床疗效。结果治疗组各项实验室指标均有明显改善,对照组则部分改善;神经功能缺损两组均有改善,但治疗组改善更为明显;两组患者均未出现明显不良反应。结论蚓激酶胶囊联合血塞通粉针治疗急性脑梗死有较好的疗效,且安全性好。     

蚓激酶胶囊治疗脑梗死患者的疗效和安全性

目的:评价蚓激酶胶囊治疗脑梗死的疗效和安全性.方法:采用多中心、随机双盲、安慰剂对照(2∶1)临床试验设计,73例发病3周后用药的脑梗死患者,分治疗组(n=50)和对照组(n=23),分别口服蚓激酶肠溶胶囊60万U和安慰剂2粒,tid,给药28d.统一实验室检测病例的凝血、纤溶、血液流变学指标,并评价患者的神经功能缺损和生活能力缺损程度.结果:治疗28d后,治疗组凝血酶原时间(PT)和部分凝血活酶时间(APTT)延长;纤维蛋白原(Fg)降低,D-二聚体含量增加;组织型纤溶酶原激活物(t-PA)含量提高,纤溶酶原激活物抑制物(PAI)含量降低;血浆黏度和全血黏度改善,且均具有显著性.安慰剂对照组则改变不明显.临床神经功能缺损评价,2组均有改善,但是治疗组恢复明显,治疗组有效率为88%,对照组47.8%.73例患者中,治疗组出现1例轻度上消化道出血(2%),无肝肾功能影响.结论:百奥蚓激酶胶囊治疗脑梗死安全有效,可作为治疗和预防缺血性脑血管病的有效药物.     

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.     

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.