前列地尔脂微球载体制剂治疗肺心病心衰及对肺动脉压力的影响

前列地尔(PGE1)以往在心血管疾病中的使用较多，在肺心病心衰和肺心病肺动脉高压治疗中也有较好疗效。近年来开发出的前列地尔脂微球载体制剂(Lipo-PGE1)，国外Ⅲ期临床试验报告有确切效果。本研究旨在观察Lipo-PGE1对肺心病心衰病人的临床疗效及对肺动脉压力的影响。     

前列地尔辅助治疗慢性肺源性心脏病疗效观察

目的：观察前列地尔脂微球载体制剂（Lipo PGE1）治疗慢性肺源性心脏病的临床疗效及对肺动脉压力的影响。方法：将68例慢性肺源性心脏病患者随机分为两组,治疗组35例,在给予常规吸氧,抗生素、支气管扩张剂等治疗基础上加用Lipo PGE120μg/d,共14 d;对照组33例,为常规治疗。观察治疗前后两组患者临床症状缓解情况,呼吸困难评分及肺动脉压力的变化。结果：治疗组与对照组临床缓解率分别为88.57%和66.67%,差异有显著性（P〈0.05）;治疗组及对照组呼吸困难评分,平均肺动脉压力均较治疗前下降,差异有显著性（P〈0.01）;治疗组下降水平较显著,与对照组比较差异有显著性（P〈0.05）;治疗组仅1例患者有轻微头疼,停药后症状消失。结论：前列地尔脂微球载体制剂可改善慢性肺源性心脏病患者临床症状,同时能显著降低肺动脉压力,使用方便安全。     

前列地尔联合低分子肝素治疗肺心病肺动脉高压的疗效观察

目的观察前列地尔联合低分子肝素治疗肺心病肺动脉高压患者的疗效。方法将128例肺心病患者随机分为3个试验组和对照组：对照组38例,为常规治疗;低分子肝素组30例,给与低分子肝素钠0．4ml皮下注射,每日两次,共14d;前列地尔组30例,给与前列地尔注射液20μg静脉注射,1次/d,共14d;联合治疗组30例,同时给与低分子肝素钠0．4ml皮下注射2次/d及前列地尔20μg静脉注射1次／d,共14d。观察治疗前后各组及组间肺动脉压力的变化。结果各组治疗后较治疗前相比肺动脉压力均显著降低,但联合治疗组更为明显,差异有显著性（P〈0．01）。结论前列地尔联合低分子肝素治疗肺心病肺动脉高压患者能显著降低肺动脉压力,使用方便安全。     

前列地尔佐治慢性肺源性心脏病急性加重期的疗效观察

目的：观察前列地尔脂微球载体制剂（Lipo PGE1）佐治慢性肺源性心脏病急性加重期的疗效。方法选择确诊为慢性肺源性心脏病急性加重期的患者60例,随机分为观察组和对照组各30例,对照组按慢性肺源性心脏病急性加重期常规治疗,对有合并症者作相应的对症支持治疗,观察组在常规吸氧,抗生素、支气管扩张剂等治疗的基础上加用前列地尔注射液治疗,治疗期间分别严密观察2组的患者的临床症状、体征、持续时间、心功能改善情况及不良反应,以确定疗效。结果观察组总有效率为90%明显优于对照组的67%,差异有统计学意义（P ﹤0.05）。结论前列地尔佐治慢性肺源性心脏病急性加重期的疗效满意,可改善慢性肺源性心脏病患者临床症状,同时能显著降低肺动脉压力,使用方便安全,近期不良反应小。     

高原地区前列地尔治疗肺原性心脏病肺动脉高压的疗效观察

目的观察高原地区前列地尔（哈药集团,曼新妥）治疗肺心病肺动脉高压患者的疗效。方法将60例肺心病患者随机分为对照组和治疗组,每组30例。对照组为常规治疗;治疗组给予前列地尔注射液（曼新妥）10μg静脉注射,1次／d,共14d;观察治疗前后2组及组间肺动脉压力的变化。结果治疗组肺动脉压力显著降低,与对照组比较差异有统计学意义（P〈0．05）。结论高原地区应用前列地尔（曼新妥）治疗肺心病肺动脉高压能显著降低肺动脉压力,使用方便安全。     

前列地尔治疗肺心病心力衰竭临床观察

慢性肺源性心脏病（肺心病）是临床上常见疾病，后期常发展为心力衰竭（心衰），严重影响患者的生活质量，需要积极有效治疗。本研究旨在观察常规治疗加用前列地尔（前列腺素E1脂质微球）治疗肺心病心衰的临床疗效与安全性。     

前列腺素E1脂微球制剂治疗肺心病心衰并肺动脉高压的疗效观察

本研究旨在观察前列腺素E1脂微球载体制剂(Lipo PGE1)对肺心病患的临床疗效及对心功能、肺动脉压力的影响。     

前列地尔(PGE_1)与米力农联合治疗慢性肺心病心力衰竭33例临床观察

目的观察前列地尔(凯时)和米力农治疗慢性肺心病心力衰竭的疗效,并与常规的抗心衰治疗进行比较。方法将58例肺心病急性加重期心功能Ⅲ~Ⅳ级患者随机分为治疗组33例,对照组25例,治疗组在常规综合治疗基础上加前列地尔和米力农,对照组仅给予常规抗心衰治疗。结果疗程结束后,治疗组经治疗后EF、CO、PaO2、PaCO2较治疗前明显改善,优于对照组(P<0.05)。临床疗效,治疗组总有效率96.9%,对照组总有效率80%,治疗组优于对照组(P>0.05)。结论前列地尔联合米力农治疗慢性肺心病顽固心力衰竭疗效明显,值得临床研究。     

前列地尔脂微球载体制剂(PGE1)对慢性阻塞性肺疾病急性加重期肺动脉高压和动脉血气的影响

目的观察前列地尔脂微球载体制剂（Lipo PGE1）慢性阻塞性肺疾病急性加重期（AECOPD）肺动脉高压和动脉血气的疗效。方法60例AECOPD合并缺氧性肺动脉高压老年患者随机分为治疗组和对照组,每组30例,治疗组在常规治疗的基础上加用Lipo PGE110μg静脉注射,1次/天,15 d为一疗程。对照组仅常规治疗。在治疗前后测量肺动脉平均压（MPAP）,动脉血氧分压（PaO2）及动脉二氧化碳分压（PaCO2）。结果两组治疗后MPAP和PaCO2较治疗前明显降低（P〈0.05）,PaO2较治疗前明显升高（P〈0.01）,治疗组与对照组相比,治疗组MPAP、PaCO2和PaO2均显著改善（P〈0.05）。结论PGE1治疗AE-COPD有良好疗效,它可以降低肺动脉高压和动脉二氧化碳分压,升高动脉氧分压。     

依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死的疗效观察

目的探讨依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死的临床疗效。方法选择80例急性脑梗死患者随机分为治疗组(40例)和对照组(40例),治疗组在常规治疗的基础上给予依达拉奉和前列地尔脂微球载体靶向制剂。结果观察两组治疗后临床疗效,治疗组总有效率95.0%显著优于对照组(75.0%)。结论依达拉奉与前列地尔脂微球载体靶向制剂联合治疗急性脑梗死安全、有效。     

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.     

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.