缬沙坦与硝苯地平控释片逆转原发性高血压左心室肥厚的效果观察

目的比较缬沙坦与硝苯地平控释片治疗原发性高血压（EH）逆转左心室肥厚（LVH）的作用。方法选择100例EH伴LVH患者，随机分为缬沙坦组（A组）及硝苯地平控释片（B组）各50例。全组患者未接受降压治疗（或仅用过利尿剂）或已停用降压药物2周以上。A组服用缬沙坦80～160mg，1次／d；B组服用硝苯地平控释片30～60mg，1次／d。全组疗程24周。观察治疗前后血压及超声心动图变化。结果两组患者治疗后血压均显著降低（P〈0．01），组间降压幅度差异元统计学意义（P〉0．05）。两组患者治疗后舒张期左室后壁厚度（LVPWT）、舒张期室间隔厚度（IVST）及左室重量指数（LVMI）均有显著改善（P〈0．01）。而且A组LVMI下降优于B组（P〈0．05）。结论缬沙坦与硝苯地平控释片在有效降压的同时均可逆转LVH，但缬沙坦对LVH的逆转作用优于硝苯地平控释片。     

两种不同联合降压方案对轻中度原发性高血压患者血压变异性及肌酸激酶的影响

目的比较硝苯地平控释片联合美托洛尔缓释片和厄贝沙坦片联合美托洛尔缓释片对轻中度原发性高血压患者血压变异性(BPV)和肌酸激酶(CK)的影响。方法①入选2017年6月—2018年5月门诊和住院年龄在18～65岁且静息心率≥80次·min~(-1)的初诊为轻中度原发性高血压患者52例为高血压组,选择同期体检的正常人60例为正常血压组,比较两组一般资料的差异;②将52例高血压患者随机分为两组:硝苯地平组(27例,硝苯地平控释片联合美托洛尔缓释片)及厄贝沙坦组(25例,厄贝沙坦片联合美托洛尔缓释片),比较两组治疗前及治疗12周后常规生化和部分24 h动态血压监测指标。结果①高血压组CK、尿酸(UA)与体质量指数(BMI)明显高于正常血压组(P <0.05,P <0.01);②治疗12周后,硝苯地平组及厄贝沙坦组较治疗前平均血压均明显降低(P <0.01),硝苯地平组24 h收缩压标准差(24 h SBPSD)、白昼收缩压标准差(d SBPSD)、夜间收缩压标准差(n SBPSD)较治疗前明显降低(P<0.05);③治疗12周后硝苯地平组及厄贝沙坦组CK、UA等较治疗前均无明显差异(P> 0.05),但硝苯地平组CK有下降趋势。结论①硝苯地平组及厄贝沙坦组对轻中度原发性高血压患者降压疗效相当,但硝苯地平组在降低轻中度原发性高血压患者收缩压变异性方面优于厄贝沙坦组;②硝苯地平组与厄贝沙坦组对CK均无明显影响。     

厄贝沙坦联合硝苯地平控释片治疗高血压的效果

目的：探讨厄贝沙坦联合硝苯地平控释片治疗高血压的效果。方法选择原发性高血压患者80例,随机分为两组,观察组采用厄贝沙坦联合硝苯地平控释片治疗,对照组采用美托洛尔联合硝苯地平控释片治疗,比较两组治疗后肾功能、平均动脉压及超声心动图的改变。结果治疗后观察组尿素氮、肌酐水平及平均动脉压显著低于对照组,差异有统计学意义（P〈0.05）;治疗后观察组室间隔厚度和左室舒张末期内径均显著小于对照组,左室射血分数高于对照组,差异有统计学意义（P〈0.05）。结论厄贝沙坦联合硝苯地平控释片对高血压左心室肥厚具有明显的逆转作用,同时能够更好地控制患者血压及保护其肾功能。     

厄贝沙坦对高血压左室肥厚患者QT离散度的影响

目的　观察厄贝沙坦对高血压患者左室肥厚 (LVH)的逆转作用及对QT离散度 (QTd)和校正QTd(QTcd)的影响。方法　 6 8例高血压患者分为LHV组 38例和非LHV组 30例 ,口服厄贝沙坦 15 0mg/d治疗后 6个月观察治疗前后左室重量指数 (LVMI)、QTd和QTcd的改变。结果　两组患者用药后收缩压(SBP)和舒张压 (DBP)显著降低 (P <0 0 1) ,LHV组治疗后较治疗前室性心律失常 (VA)明显改善 ,LVMI显著降低、QTd和QTcd显著缩短 (P <0 0 1)。结论　厄贝沙坦具有良好的降压效果 ,还可逆转心肌肥厚 ,降低QTd和QTcd ,减少恶性心律失常的发生 ,从而改善高血压LVH患者的预后     

厄贝沙坦/氢氯噻嗪与硝苯地平控释片联合应用对老年性高血压的临床疗效观察

目的:探讨厄贝沙坦/氢氯噻嗪联合硝苯地平控释片治疗老年性高血压的临床效果.方法:78例老年性高血压患者随机分为对照组和实验组,每组39例.对照组口服硝苯地平控释片30mg,1次/d,实验组晨服厄贝沙坦/氢氯噻嗪片150mg,睡前服用硝苯地平控释片30mg,1次/d,疗程10周.比较两组临床疗效以及治疗前后SBP、DBP和心率.结果:治疗后实验组总有效率(92.30%)明显优于对照组(74.36%)(P<0.05);实验组治疗后SBP、DBP和心率降低较对照组显著,差异有统计学意义(P<0.01).无明显的不良反应.结论:厄贝沙坦/氢氯噻嗪联合硝苯地平控释片治疗老年性高血压可以更好地改善血压,取得理想的治疗效果,值得推广.     

厄贝沙坦治疗原发性高血压并左室肥厚患者的疗效观察

目的观察厄贝沙坦治疗原发性高血压并左室肥厚的疗效。方法将原发性高血压并左室肥厚患者60例,随机分为厄贝沙坦组(30例,150mg/d)和贝那普利组(30例,10mg/d)。疗程为6个月,服药前后测血压和用超声心动图检测左心室舒张末期内径(LVDD)、左心室舒张末期室间隔厚度(LVDST)、左心室舒张末期后壁厚度(LVPWT)和左室质量指数(LVMI)。结果治疗6个月后,血压较治疗前有明显下降(P<0.05),且厄贝沙坦组血压明显低于依那普利组,差异有统计学意义(P<0.05)。治疗后的LVDD、LVST、LVPWT和LVMI均比治疗前的显著降低(均P<0.05)。且厄贝沙坦组LVD、LVST、LVPWT及LVMI稍低于贝那普利组,差异有统计学意义(P<0.05)。两组不良反应发生率均较低。结论贝沙坦能有效降低高血压、逆转左室肥厚,不良反应少。     

厄贝沙坦联合吲达帕胺治疗老年高血压并逆转左室肥厚的临床观察

目的:观察厄贝沙坦联合吲达帕胺对老年原发性高血压的降压效果及对左室肥厚(LVH)的逆转作用。方法:将86例老年原发性高血压并左室肥厚患者随机分为厄贝沙坦+吲达帕胺组(A组)和氨氯地平+吲达帕胺组(B组),治疗前后分别行24小时动态血压监测和超声心动图、血尿常规、肝肾功能、血脂、血糖等生化检查,同时观察药物不良反应。结果:①两组治疗1个月后,收缩压、舒张压及血压负荷均明显降低(P<0.01),降压谷/峰比率>50%;②A组治疗6个月后,左室舒张末期内径、左室后壁与舒张期室间隔厚度、左室重量指数较治疗前明显下降(P<0.05～0.01),B组治疗6个月后,左室重量指数有所下降(P<0.05),左室后壁与室间隔厚度略有下降,但与治疗前比较差异无显著性;③A组治疗6个月后,患者24小时尿蛋白排泄量明显减少(P<0.05)。结论:老年原发性高血压患者长期应用厄贝沙坦,能显著平稳降低血压,逆转左室肥厚,减少蛋白尿,不良反应轻。     

厄贝沙坦联合硝苯地平控释片治疗社区高血压的效果观察

目的探讨厄贝沙坦联合硝苯地平控释片治疗社区高血压的效果。方法420例高血压患者,采用随机法分为厄贝沙坦组、硝苯地平组、联合组,各140例。厄贝沙坦组采用厄贝沙坦片口服治疗,硝苯地平组采用硝苯地平控释片口服治疗,联合组采用厄贝沙坦片联合硝苯地平控释片口服治疗。比较三组患者血压控制效果、不良反应发生情况以及治疗前后的血压、心率、血管内皮生长因子(VEGF)、血清同型半胱氨酸(Hcy)水平。结果联合组血压控制总有效率97.86%均高于厄贝沙坦组的89.29%、硝苯地平组的88.57%,差异均具有统计学意义(P<0.05)。治疗后,三组患者收缩压(SBP)、舒张压(DBP)、心率(HR)水平均显著降低,且联合组患者SBP、DBP、HR水平均显著低于厄贝沙坦组、硝苯地平组,差异均具有统计学意义(P<0.05)。治疗后,联合组患者VEGF(90.24±6.33)pg/ml均低于厄贝沙坦组的(110.36±11.33)pg/ml、硝苯地平组的(110.25±11.29)pg/ml,Hcy(12.07±1.33)μmol/L均低于厄贝沙坦组的(17.51±1.26)μmol/L、硝苯地平组的(17.56±1.17)μmol/L,差异均具有统计学意义(P<0.05)。厄贝沙坦组与硝苯地平组血压控制效果、SBP、DBP、HR、VEGF、Hcy比较,差异均无统计学意义(P>0.05)。结论厄贝沙坦联合硝苯地平控释片治疗社区高血压控制血压及心率效果优于单种药物治疗,安全性高,值得在临床推广应用。     

厄贝沙坦和阿替洛尔治疗原发性高血压疗效观察

目的:比较厄贝沙坦片和阿替洛尔片治疗原发性高血压合并左室肥厚患者的降压逆转左室肥厚的效果。方法:将73例中度高血压合并LVH患者随机分为两组,分别服用厄贝沙坦片(厄贝沙坦组)和阿替洛尔片(阿替洛尔组)。比较治疗前及治疗8周后对血压(坐位)、超声心动图中LVH的影响。结果:服药8周后,两组血压均显著降低。两药均能逆转LVH,而阿替洛尔组的逆转出现在用药后8周。结论:厄贝沙坦和阿替洛尔均有较好的降压作用,厄贝沙坦对LVH的逆转效应优于阿替洛尔。     

非洛地平缓释片对原发性高血压左室肥厚的影响

目的：观察非洛地平缓释片对高血压左室肥厚的逆转作用。方法：应用动脉血压及彩色多普勒超声心动图测定26例高血压并左室肥厚患者口服非洛地平缓释片（5～10mg/d),24周后血压及左室形态结构变化。结果：治疗后血压明显下降（P＜0．01）,舒张期室间隔厚度及左室后壁厚度,左室重量指数均明显减少（P＜0．01）。结论：非洛地平缓释片不但能有效降低血压,而且能逆转左室肥厚。     

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.