非苯二氮(艹卓)类镇静催眠药的研发进展与临床评价

目的:介绍非苯二氮(艹卓)类镇静催眠药的研究进展与临床评价.方法:通过查阅国内、外近期有关文献进行评述.结果与结论:近年来,非苯二氮()类镇静催眠药进展迅速,其耐药性和依赖性很小,几乎无反跳性失眠现象.此类药物是目前镇静催眠药的重要研发领域.     

非苯二氮Zhuo类镇静催眠药的研发进展与临床评价

目的：介绍非苯二氮Zhuo类镇静催眠药的研究进展与临床评价。方法：通过查阅国内、外近期有关文献进行评述。结果与结论：近年来，非苯二氮Zhuo类镇静催眠药进展迅速，其耐药性和依赖性很小，几乎无反跳性失眠现象。此类药物是目前镇静催眠药的重要研发领域。     

扎来普隆的研究现状和应用前景

扎来普隆(zaleplon)是一种吡唑并嘧啶类化合物,属于新型非苯二氮艹卓类镇静催眠药,用于失眠的短效治疗。与苯二氮艹卓类的传统镇静催眠药不同,它选择性作用于BZ_1(ω_1)受体,无其它镇静催眠药所具有的诸多不良反应,且半衰期短,疗效好,无蓄积作用。 1 作用机理 在中枢神经系统中存在两种苯二氮艹卓受体亚型(BZ_1/BZ_2或ω_1/ω_2),BZ_1受体主要位于与镇静作用有关的大脑区     

镇静催眠药的研究进展及临床应用

镇静催眠药的使用由早期的苯巴比妥类向苯二氮革类、由苯二氮革类向非苯二氮革类发展.本文通过对三类镇静催眠药的作用机理、药动学、不良反应、适用人群,注意事项做一简要的对比、阐述,为临床更加合理的使用镇静催眠药物提供参考.     

2007—2012年天津医科大学第二医院口服镇静催眠药应用分析

了解2007-2012年我院口服镇静催眠药的使用情况及用药趋势,为临床合理用药提供依据。方法：根据我院医院信息系统（CHIS）中2007-2012年口服镇静催眠药的原始数据资料,采用世界卫生组织（WHO）推荐的限定日剂量（DDD）分析法,对各年口服镇静催眠药的销售金额、用药频度（DDDs）、限定日费用（DDC）等进行比较分析。结果：2007-2012年我院口服镇静催眠药的销售金额和DDDs基本呈增长趋势,DDC稳中有降。艾司唑仑、劳拉西泮、氯硝西泮等苯二氮蕈类药的DDDs均较高,以唑吡坦为代表的新型非苯二氮革类药用量增长迅速。结论：我院口服镇静催眠药应用基本合理,其中苯二氮革类药占主导地位,新型非苯二氮革类药用量也有逐年上升趋势,前景广阔。进一步加强精神药品的监督管理仍是今后工作的重点。     

住院精神科患者镇静催眠药的用药分析

目的:了解本院住院精神科患者镇静催眠药的使用情况,防止滥用镇静催眠药引起的药害。方法:调查、分析本院2005年9月—11月住院患者864例使用镇静催眠药的情况。结果:本院住院患者使用的镇静催眠药以苯二氮艹卓类为主,构成比为63.69%;使用频度为33.10%,男性居多。其中阿普唑仑最为常用,使用频度为26.62%,构成比为51.22%。结论:本院住院患者中,多使用以阿普唑仑为主的苯二氮艹卓类镇静催眠药,具有该类药物滥用的可能性,须引起临床的高度重视。     

右旋佐匹克隆——新型镇静催眠药

化药3.1类原料,片剂3mg镇静催眠药,用于治疗失眠右旋佐匹克隆(Esopiclone)是由美国Sepracor公司开发的快速短效非苯二氮卓类镇静安眠药,为佐     

失眠及临床药物治疗

本文将失眠及失眠的临床药物治疗结合近年的研究进展进行了综述,主要阐述了苯二氮艹卓类抗失眠药物的临床应用及注意事项,尤其介绍了非苯二氮艹卓类即新型镇静催眠药在临床上的应用及展望。     

药物治疗失眠

目的:综述各类药物在治疗失眠中的应用,为开发和应用催眠药提供参考。方法:通过光盘检索并查阅相关文献,进行综述。结果与结论:镇静催眠药正逐步从苯二氮(艹卓)类药物向非苯二氮(艹卓)类药物。从非选择性向高效、高选择性、副作用小的方向发展。此外,天然药物也是人们的研究热点之一,具有广阔的应用前景。     

非苯二氮(艹卓)类催眠药作用靶位的特异性与评价

目的:评价非苯二氮类催眠药作用研究和临床应用,反映催眠药进展的侧面。方法:查阅近期国内、外有关文献,进行分析。结果与结论:非苯二氮类催眠药的进展迅速,有别于传统的催眠药,对受体亚型的选择性强、血浆半衰期短、不良反应小,缩短睡眠的潜伏期,改善睡眠维持和提高睡眠质量,增加睡眠总时间,标志一个新的里程的开始。成为开启解脱失眠痛苦的治疗之门的一把金“药匙”。     

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.

---

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.     

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.     

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.