拉西地平与赖诺普利治疗高血压的疗效比较

目的：比较拉西地平和赖诺普利对高血压患者的疗效。方法：６０例高血压病Ⅰ期或Ⅱ期患者分拉西地平组（Ａ）、赖诺普利组（Ｂ）,实行２４ｈ动态血压监测。结果：二药均能显著降压,且降低偶测血压的幅度无显著差异。拉西地平降低２４ｈ平均压和白天平均压的幅度大于赖诺普利。结论：对轻、中度高血压拉西地平与赖诺普利均为安全且易耐受的药物,每日１次能维持２４ｈ降压效应。     

拉西地平与苯那普利对高血压患者24h血压的影响

目的比较拉西地平和苯那普利对高血压患者的疗效。方法60例高血压病Ⅰ期或Ⅱ期患者按服药情况分拉西地平组、苯那普利组，治疗8周进行24h动态血压（BP）监测。结果两药均能显著降压，两者降低偶测BP的幅度无显著差异，拉西地平降低24h平均压和白天平均压的幅度大于苯那普利。结论对轻中度高血压病拉西地平与苯那普利是一种安全的药物，每天给药一次能维持24h降压效应。     

拉西地平治疗轻、中度高血压病的疗效和安全性评价

目的：评价拉西地平（Lacidipine,Lac)治疗高血压病的疗效及安全性。方法：102例轻、中度高血压病患者,随机分类治疗组拉西地平组（n=51),对照组赖诺普利组（n=51),持续用药8周。结果：二组治疗前后降压有效率和降压幅度无显著性,P＞0．05,但咳嗽发生率拉西地平组明显低于赖诺普利,差异有显著性,P＜0．01。结论：拉西地平４－８mg,每日１次治疗国人轻、中度高血压疗效确切,耐受性好,干咳的不良反应明显低于赖诺普利。     

硝苯地平控释片与普通片治疗老年高血压病比较

目的 比较硝苯地平控释片与普通片对老年高血压患者的降压疗效。方法 采用随机、单盲的方法，对８４例老年高血压患者进行２４ｈ动态血压监测，比较其疗效及副反应。结果 两药均能显著降低老年高血压患者的偶测血压及２４ｈ平均血压（Ｐ〈０．０１）。两药在降低偶测压缩压、２４ｈ平均收缩压及白天平均血压幅度方面差异无显著性（Ｐ〉０．０５），硝苯地平控释片能明显降低患者的偶测舒张压（Ｐ〈０．０５）、２４ｈ平均舒张压（     

赖诺普利与依那普利对高血压的疗效比较

９２例原发性Ⅰ和Ⅱ期高血压病人采用随机、单盲方法，分２组治疗。一组用赖诺普利，ｐｏ，２０－８０ｍｇ／ｄ，另一组用依那普利，ｐｏ，１０－４０ｍｇ／ｄ，疗程均为４ｗｋ。降压总有效率和降压幅度：赖诺普利是８９％和２．９／２．０ｋＰａ，依那普利是９７％和３．１／２．１ｋＰａ，２药降压均显著（Ｐ＜０．０１），降压疗效相仿（Ｐ＞０．０５）。不良反应发生率是２９％和３４％，其中最多是干咳。结果提示赖诺普利治疗轻、中度高血压有效、安全。     

厄贝沙坦和赖诺普利联合应用对高血压病患者血管内皮功能的影响

目的探讨厄贝沙坦、赖诺普利单独与联合治疗对高血压患者血浆一氧化氮(NO)和内皮素(ET)的调节作用。方法选择156例高血压患者,随机分为3组,51例接受厄贝沙坦治疗;55例接受赖诺普利治疗;联合治疗组50例接受厄贝沙坦和赖诺普利治疗。均于治疗前后行血压及血浆NO、ET测定。并与50例健康者血浆NO、ET对照。结果3组高血压患者NO较对照组显著降低(P<0.01),ET显著升高(P<0.01)。3组治疗后血压均有显著下降(P<0.01),厄贝沙坦组及赖诺普利组降压幅度无差异,联合用药组降压幅度明显高于两单独治疗组(P<0.05);3组血浆NO水平均有显著升高(P<0.01);厄贝沙坦组及赖诺普利组血浆NO水平升高幅度无差异(P>0.05),联合用药组NO升高幅度明显高于两单独治疗组(P<0.05);3组血浆ET水平均有显著降低(P<0.01),厄贝沙坦组及赖诺普利组ET水平下降幅度无差异(P>0.05),联合用药组ET下降幅度明显高于两单独应用组(P<0.05)。结论厄贝沙坦、赖诺普利长期单独应用可明显降低血压,同时升高血浆NO水平、降低血浆ET水平、改善血管内皮素功能。两药联用治疗高血压对改善血管内皮功能效果更好。     

氯沙坦治疗老年高血压及其对心脏保护作用

目的：探讨血管紧张素Ⅱ受体拮抗剂氯沙担治疗老年高血压病的治疗及其对心脏保护作用。方法：３２例老年高血压病患者，在停服降压药１周后，口服氯沙坦５０～１００ｍｇ／ｄ，并于治疗前后分别接受２４ｈ动态血压监测及超声心动图检查。结果：服药１２周后，该组患者２４ｈ动态血压显著降低，左室肥厚明显减轻，左室舒张功能显著改善。结论：对于老年高血压患者，氯沙坦能有效降低２４ｈ血压，同时具有心脏保护作用，是较为理想的降     

苯那普利与卡托普利治疗原发性高血压的疗效

目的；观察苯那普利与卡托普利治疗原发性高血压病的疗效，方法：采用随机，单盲，平行对照将６０例原发性高血压病患者分苯那普利治疗组（ｎ＝３０）和卡托普利（ｎ＝３０）对照组，观察降压效果。结果：苯那普利与卡托普利两药的降压有效率相似（Ｐ〉０．０５），但前者在控制２４ｈ血压较后者为优，结论：苯那普利半衰期较长，一次ｐｏ即可达到满足降压效果，是一种不良反应少，安全有效的抗高血压病药物。     

赖诺普利对高血压患者左心室肥厚的逆转作用

目的：探讨赖诺普利对原发性高血压患者左心室肥厚逆转及对C-反应蛋白、尿酸水平的影响。方法：83例原发性高血压1、2级患者，给予赖诺普利10～20mg，每天1次口服，把血压控制到〈18．62／11．97kPa，疗程为16wk，监测治疗前后收缩压、舒张压、C-反应蛋白、尿酸、舒张期室间隔厚度、舒张末期左室后壁厚度、左室舒张末内径、左心室质量指数变化。结果：用赖诺普利治疗16wk后，患者血压、C-反应蛋白和尿酸水平明显降低；经赖诺普利治疗后，室间隔厚度、左心室后壁厚度和左心室质量指数均有明显改善。结论：赖诺普利能够显著降低血压，干预和逆转左心室肥厚，降低C-反应蛋白和尿酸水平，是治疗原发性高血压安全有效的药物。     

马尼地平与赖诺普利对糖尿病合并高血压患者尿白蛋白排泄率和左心室质量指数的效应比较

目的:评估马尼地平与赖诺普利对糖尿病合并高血压患者尿白蛋白排泄率(AER)和左心室质量指数(LVMI)的效应。方法:将我院174例患有高血压的2型糖尿病患者随机均分为马尼地平组和赖诺普利组,两组患者在停用4周降压药后分别开始口服马尼地平片(每次10mg,每日1次)或赖诺普利片(每次10mg,每日1次);8周后,无效应者[舒张压(DBP)>80mmHg]剂量加倍;3个月后,无效应和伴发副作用的患者终止治疗,剩下的患者继续接受马尼地平或赖诺普利治疗,直至完成24个月的疗程(共有121例患者完成了研究,马尼地平组60例、赖诺普利组61例)。在治疗过程中,每3个月监测患者血压并评估AER、肌酐清除率、糖化血红蛋白(HbA1c)、体质量指数(BMI)以及LVMI,同时观察两组患者的不良反应情况。结果:马尼地平和赖诺普利均能显著降低收缩压(SBP)和DBP[第24个月后,血压下降水平分别为22.3/15.5mmHg(P<0.001)、21.4/15.7mmHg(P<0.01)];且两药均能显著降低AER,但赖诺普利的效果比马尼地平更加显著,并且显效更快(赖诺普利在治疗3个月后显效,而马尼地平在治疗6个月后显效);另外,马尼地平降低LVMI的效应要强于赖诺普利,且对于左心室肥厚患者效应更加显著。结论:尽管两种药物对糖尿病合并高血压患者降血压的效应相似,但对AER和LVMI的效应有所不同,应根据患者的疾病情况选择个体化用药。     

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.     

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.