奥美沙坦酯对2型糖尿病高血压尿微量蛋白影响

目的探讨奥美沙坦酯对2型糖尿病患者的血压及尿微量白蛋白的影响。方法80例24小时尿微量白蛋白排泄量(UAE)在30～300mg的2型糖尿病患者随机分为两组:奥美沙坦酯组40例,口服奥美沙坦酯20mg/d;依那普利组40例口服马来酸依那普利10～20mg/d,疗程12周。分别测量两组治疗前后血压(BP)、尿微量白蛋白(ALB)、血肌酐(Scr)并计算内生肌酐清除率(Ccr)。结果两组治疗后BP、Scr及ALB均显著下降(P<0.05),Ccr明显上升(P<0.05),组间比较无显著性差异(P>0.05);依那普利组咳嗽发生率25%,其中有6例不能耐受咳嗽而退出试验,奥美沙坦酯组无咳嗽病例发生。结论奥美沙坦酯不仅能有效降低血压,而且能降低尿微量白蛋白,不良反应少,依从性好。     

坎地沙坦酯与培哚普利联合治疗对高血压患者尿微量白蛋白影响的临床观察

目的坎地沙坦酯与培哚普利联合治疗对高血压患者尿微量白蛋白的影响。方法选择90例原发性高血压合并有微量蛋白尿患者,随机分为坎地沙坦酯组、培哚普利组及坎地沙坦酯与培哚普利联合组,分别予以坎地沙坦酯8mg/d,培哚普利4mg/d,及坎地沙坦酯8mg/d联合培哚普利4mg/d口服,治疗8周,观察治疗前后3组血压及尿微量白蛋白、血肌酐值,并进行比较。结果培哚普利组和坎地沙坦酯组患者经8周治疗,血压降至正常,微量尿蛋白排泄量明显减少(P<0.01),联合组较其他组进一步下降(P<0.05)。培哚普利组有1例出现干咳而改用其他药物。结论坎地沙坦酯与培哚普利联合能更加有效减少高血压患者微量白蛋白尿排泄量,保护肾功能。     

坎地沙坦和氨氯地平对原发性高血压早期肾损害的影响

目的 旨在探讨坎地沙坦和氨氯地平对原发性高血压早期肾损害的疗效.方法 对83例门诊原发性高血压(1级、2级)伴尿微量白蛋白阳性的患者按就诊顺序用数字随机法分为氨氯地平组(5 mg·d-1)42例和坎地沙坦组(8 mg·d-1)41例,疗程3个月.观察治疗前后血压、血肌酐(Scr)、尿微量白蛋白(UMALB)、尿α1微球...     

高血压早期肾损害临床治疗

目的观察坎地沙坦酯和辛伐他汀滴丸合用对高血压早期肾损害的改善作用。方法高血压患者116例,随机分为观察组和对照组,每组58例,2组除常规治疗外,观察组每天口服坎地沙坦酯4～8mg,辛伐他汀滴丸10mg。对照组不加用辛伐他汀滴丸。测定治疗前和治疗180d后血压、血脂及肝、肾功能。晨尿微量白蛋白、β2微球蛋白、N-乙酰-β-D-氨基葡萄糖酐酶和内生肌酐清除率。结果2组血压均有显著下降（P〈0．05）;观察组血总胆固醇（TC）、低密度脂蛋白胆固醇（LDL-C）下降明显（P〈0．05）;2组治疗前后晨尿微量白蛋白、B2微球蛋白和N-乙酰-β—D-氨基葡萄糖酐酶均有明显下降,内生肌酐清除率明显改善（P〈0．05）,观察组较对照组变化更加显著,差异有统计学意义（P〈0．05）。结论坎地沙坦酯和辛伐他汀滴丸有良好协同改善肾功能作用,合用对高血压早期肾损害的改善作用更显著。     

坎地沙坦对原发性高血压患者肾功能的影响

目的:探讨血管紧张素Ⅱ受体拮抗剂坎地沙坦对原发性高血压患者肾功能的影响。方法:将88例原发性高血压患者随机分为对照组(44例)与治疗组(44例),治疗组口服坎地沙坦(剂量8~16m g.d-1),同时保留其他原有抗高血压药物;对照组保留原抗高血压药物治疗,除外坎地沙坦,疗程8周。治疗前后分别测定偶测血压以及血肌苷(C r)、尿微量白蛋白(U-M ALB)、2β微球蛋白(β2-M G)水平。结果:血压降低值的组间比较无明显差异(P>0.05),两组药物治疗前后血肌苷(C r)、尿微量白蛋白(ALB)、2β微球蛋白(2β-M G)水平检测结果为治疗组差异显著(P<0.05),对照组无显著差异(P>0.05)。结论:坎地沙坦不仅具有良好降压效果,还能降低尿微量白蛋白、2β微球蛋白的排泄,改善肾功能。     

坎地沙坦酯治疗高血压合并早期糖尿病肾病的临床研究

目的观察坎地沙坦酯治疗高血压合并早期糖尿病肾病的疗效。方法选择50例高血压合并早期糖尿病肾病患者，在常规降糖药物治疗同时应用坎地沙坦酯4～12mg／d，12周后比较治疗前后血压、尿微量白蛋白、血尿素氮、血肌酐、血糖、糖化血红蛋白等的变化。结果治疗后，收缩压和舒张压明显降低（P〈0．01），尿微量白蛋白显著减少（P〈0．05）。结论坎地沙坦酯能够在有效控制血压的同时降低尿微量白蛋白的排泄，对于高血压合并早期糖尿病肾病患者的肾脏具有保护作用。     

胰激肽原酶联合坎地沙坦酯治疗早期2型糖尿病肾病108例疗效观察

目的观察胰激肽原酶联合坎地沙坦酯治疗早期糖尿病肾病的效果。方法采用随机分组法将108例糖尿病肾病患者分成3组,每组36人;对照组常规降糖治疗,合并高血压者采用钙离子拮抗剂,苯磺酸氨氯地平治疗;坎地沙坦酯组在降糖的基础上采用坎地沙坦酯替代钙离子拮抗剂,（有高血压者每天4-8 mg,无高血压者每天2 mg）：胰激肽原酶组是在坎地沙坦组的基础上加用胰激肽原酶肌肉注射每天40单位,10周为一疗程。10周后观察前后收缩压,舒张压,甘油三酯,胆固醇,糖化血红蛋白,血肌酐,24 h尿微量白蛋白的变化。结果对照组与坎地沙坦酯组在前后收缩压,舒张压,甘油三酯,胆固醇,糖化血红蛋白,血肌酐,而在24 h尿微量白蛋白的变化在统计学上有统计学差异,（P〈0.05）,胰激肽原酶组与坎地沙坦酯组相比治疗前后24 h尿微量白蛋白的变化也有统计学差异（P〈0.05）。结论胰激肽原酶联合坎地沙坦酯治疗糖尿病早期肾病在治疗早期糖尿病肾病时能显著减少尿微量白蛋白的生成,从而更有效的保护糖尿病患者肾脏。     

贝那普利联合缬沙坦治疗高血压合并糖尿病肾病的临床观察

目的观察贝那普利联合缬沙坦治疗高血压、糖尿病肾病的疗效。方法 28例高血压、糖尿病肾病老年患者平均分成两组,对照组单用缬沙坦;治疗组联合应用贝那普利,共8周。比较两组治疗前后24h尿微量白蛋白、内生肌酐清除率、血钾及血压变化。结果治疗组24h微量白蛋白对照组显著下降(P<0.01)。两组内生肌酐清除率及血钾无明显变化(P>0.05)。结论贝那普利和缬沙坦联合应用可明显减少高血压、糖尿病肾病老年患者的尿白蛋白。     

坎地沙坦酯对轻中度高血压患者早期肾脏保护作用探讨

目的探讨坎地沙坦酯对轻中度高血压患者早期肾脏保护的作用。方法选取高血压1、2级患者188例予坎地沙坦酯片8mg口服,每天1次,连用8周。观察治疗效果及治疗前后血压、尿微量白蛋白(mAlb)、血清胱抑素C(CysC)、尿素氮(BUN)、肌酐(Scr)水平的变化情况。结果坎地沙坦酯对轻中度高血压患者的降压总有效率为90.43%。治疗后,mAlb及CysC水平均低于治疗前,差异均有统计学意义(P<0.05)。治疗前后,BUN及Scr水平差异无统计学意义(P>0.05)。结论坎地沙坦酯不仅有较好的降压作用,且有明显的肾脏保护作用,可作为轻中度高血压患者的首选药物。     

坎地沙坦酯与左旋氨氯地平合用对原发性高血压微量蛋白尿的影响

目的研究坎地沙坦酯与左旋氨氯地平对原发性高血压微量蛋白尿的影响。方法105例原发性高血压伴微量蛋白阳性门诊或住院患者,按就诊顺序随机分三组,分别用坎地沙坦酯（坎地）、左旋氨氯地平（左氨）、坎地沙坦酯＋左旋氨氯地平联合（联合）治疗,剂量分别为每天4mg、2.5mg和4mg＋2.5mg,疗程6个月,观察治疗前后血压、尿微量白蛋白（UMALB）及尿β2-微球蛋白（Uβ2-MG）及血清肌酐（Scr）变化。结果三组血压均较治疗前明显降低,具有统计学意义（P〈0.05）,但治疗后三组间比较无显著统计学差异;尿UMALB及Uβ2-MG三组均较治疗前减少,且具统计学意义（P〈0.01）,而联合治疗组比两药单用组比较下降更明显,且具有统计学意义差异（P〈0.05）。结论坎地沙坦酯及左旋氨氯地平能有效降压,同时能改善高血压早肾损害,而联合用药时效果更明显,能更有效地发挥肾脏保护作用。早期联合坎地沙坦酯及左旋氨氯地平是治疗高血压早期肾损害的有效措施之一。     

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.