厄贝沙坦与依那普利治疗轻中度老年原发性高血压的疗效比较

目的比较厄贝沙坦与依那普利治疗轻、中度老年原发性高血压的临床疗效。方法选择轻、中度老年原发性高血压患者47例，随机分组，24例应用厄贝沙坦150mg／d，23例应用依那普利10mg／d，每周观察血压下降幅度，并于服药4周后行动态血压监测（ABPM）。结果2组患者治疗后血压均有下降，治疗4周后与给药前相比，各项血压指标的比较值差异均有显著性（均P〈0．01）。试验不同时期的同一时间点，试验组与对照组差异无显著性（P〉0．05）。但2组间ABPM结果显示，厄贝沙坦组血压负荷日间和晚间较依那普利组均有显著降低（均P〈0．01）。2组降压的谷／峰（T／P）比值比较，厄贝沙坦组优于依那普利组（P〈0．05）。且不良反应少。结论厄贝沙坦优于依那普利，是一种安全和有效的治疗轻、中度老年原发性高血压的药物。     

厄贝沙坦与依那普利治疗轻中度高血压疗效观察

目的：观察厄贝沙坦治疗轻、中度原发性高血压（EH）的疗效及安全性。方法：随机将87例轻、中度原发性高血压患者分为厄贝沙坦组48例和依那普利组39例,分别接受厄贝沙坦150mg/d或依那普利40mg／d。治疗前后测量坐位血压,记录疗效和不良反应。结果：厄贝沙坦与依那普利均能有效降低血压,治疗总有效率分别为97．9％和1197．0％,两组疗效比较,差异无显著性（P〉0．05）。依那普利组有6例发生干咳。结论：厄贝沙坦是治疗轻、中度原发性高血压安全有效的药物。     

国产厄贝沙坦治疗轻中度高血压的临床疗效观察

目的观察国产厄贝沙坦（irbesartan,吉加）治疗轻、中度原发性高血压的疗效及安全性。方法将60例轻、中度高血压患者随机分为2组,治疗组30例口服国产厄贝沙坦片150mg,每天1次,观察组30例口服进口厄贝沙坦片150mg,每天1次。治疗时间为8周。治疗4周后对舒张压（DBP）≥90mmHg者,药物剂量增至300mg,每天1次。结果经过8周治疗后,治疗组血压由155/97mmHg降至138/86mmHg,对照组血压由155/98mmHg降至136/85mmHg。两组与服药前比较,血压均有明显降低（t值分别为25.94,29.35,P均〈0.01）,总有效率分别为80.00%和83.33%（χ^2=0.004,P〉0.05）。两组在治疗过程中均未发生明显不良反应,也无明显心率变化。结论国产与进口厄贝沙坦对轻、中度原发性高血压具有相近的降压效果和安全性。     

厄贝沙坦与依那普利治疗轻中度老年原发性高血压的疗效比较

目的比较厄贝沙坦与依那普利治疗轻、中度老年原发性高血压的临床疗效。方法选择轻、中度老年原发性高血压患者47例,随机分为2组,24例应用厄贝沙坦150 mg/d,23例应用依那普利10 mg/d,每周观察血压下降幅度,并于服药4周后行动态血压监测(ABPM)。结果2组患者治疗后血压均有下降,治疗4周后与1周时相比,各项血压指标的差异均有统计学意义(P<0.01),试验不同时期的同一时间点,试验组与对照组差异无统计学意义(P>0.05)。但2组间ABPM结果显示,厄贝沙坦组血压负荷日间和晚间较依那普利组均有显著降低(P<0.01)。2组降压的谷峰(T/P)比值比较,厄贝沙坦组优于依那普利组(P<0.05),且不良反应少。结论厄贝沙坦优于依那普利,是一种安全有效的治疗轻、中度老年原发性高血压的药物。     

厄贝沙坦治疗轻、中度高血压病的疗效观察

目的:观察血管紧张素Ⅱ受体阻滞剂厄贝沙坦治疗轻中度原发性高血压的疗效及安全性。方法:78例轻、中度原发性高血压患者服用厄贝沙坦75mg,每日1次,2周无效加至150mg,每日1次,经6周治疗后观察血压、心率。结果:治疗后收缩压和舒张压较前明显下降(P＜0．05),降压总有效率达81．67％;治疗期间无明显不良反应。结论:厄贝沙坦冶疗原发性高血压安全有效,同时能改善心室舒张功能。     

厄贝沙坦氢氯噻嗪片治疗原发性高血压的疗效观察

目的比较厄贝沙坦氢氯噻嗪片与厄贝沙坦治疗轻、中度原发性高血压的临床疗效。方法将lOO傩者随机分为2组：观察组50例,厄贝沙坦氢氯噻嗪片（含厄贝沙坦150mg,氢氯噻嗪12．5mg）,1片／d;对照组50例,厄贝沙坦150mg／d。用药4周后进行疗效分析。结果观察组总有效率为98％,对照组总有效率为80％,2组比较差异有统计学意义（P〈0．05）。结论厄贝沙坦氢氯噻嗪片治疗轻、中度原发性高血压疗效优于单独使用厄贝沙坦。     

厄贝沙坦-氢氯噻嗪治疗原发性高血压合并高尿酸血症的疗效观察

目的观察厄贝沙坦-氢氯噻嗪治疗原发性高血压合并高尿酸血症的临床疗效。方法选择120例原发性高血压1～2级患者,血尿酸440～5301amol／L,随机分成两组：厄贝沙坦氢氯噻嗪组（厄贝沙坦150mg／d,氢氯噻嗪12．5mg／d）62例,氯沙坦组（50mg／d）58例,平均8周,进行治疗前后血压、血尿酸的对比研究。结果厄贝沙坦一氢氯噻嗪治疗原发性高血压的临床效果同氯沙坦一样有效,两组总有效率分别为95-2％和93．1％（P〉0．05）;治疗后两组高尿酸水平有明显的下降（P〈0．05）。结论厄贝沙坦-氢氯噻嗪除有良好的降压作用外,尚能安全有效地降低原发性高血压患者合并的高尿酸血症。     

厄贝沙坦治疗老年原发性高血压临床观察

目的观察厄贝沙坦治疗老年原发性高血压的临床疗效。方法采用厄贝沙坦治疗老年原发性高血压患者72例,比较服药前后血压、心功能变化。结果本组患者服药前、后血压变化有显著差异（P〈0.05）,且0周与8周LVEF值、E/A值均有显著差异（P〈0.05）。结论厄贝沙坦治疗老年原发性高血压,能有效降低血压,改善患者的心功能。     

巨贝沙坦氢氯噻嗪片治疗原发性高血压临床效果观察

目的探讨厄贝沙坦氢氯噻嗪片对原发性高血压的临床疗效。方法选择本院收治的原发性高血压128例患者作为研究对象,随机分为观察组和对照组,每组各64例,对照组给予厄贝沙坦片治疗,观察组给予厄贝沙坦氢氯噻嗪片治疗,两组治疗时间均为4周。观察两组治疗前后血压变化及不良反应的发生率。结果治疗4周后,观察组收缩压和舒张压均显著低于对照组,差异有统计学意义（P〈0．05）;观察组总有效率分别为89．1％,对照组总有效率为79．7％,两组比较差异有统计学意义（P〈0．05）。两组均未见严重不良反应发生。结论厄贝沙坦氢氯噻嗪片治疗原发性高血压疗效显著,且不良反应少,安全性较好,值得临床推广使用。     

厄贝沙坦治疗轻中度原发性高血压32例

目的:通过偶测血压和动态血压监测评价新型降压药物厄贝沙坦的降压效果及安全性.方法:轻、中度原发性高血压患者32例,经2周安慰剂治疗后口服厄贝沙坦(150 mg,1次/d)4周,其中20例作动态血压监测.结果:治疗4周后偶测血压和动态血压监测的总有效率分别为93.7%和95%;动态血压监测还表明,不仅24 h平均血压和血压负荷值显著降低(P＜0.01),而且白昼和夜间的平均血压值亦呈一致性显著降低(P＜0.01或0.05),其收缩压和舒张压的降压谷峰比值分别达到71.3%和66.7%;未见不良反应发生.结论:厄贝沙坦每日一次口服对轻、中度原发性高血压患者具有较好的降压效果和安全性.     

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.