司氟沙星注射液治疗急性细菌感染60例

目的：观察国产司氟沙星注射液（SPFX）治疗急性细菌感染的疗效和不良反应。方法：共治疗60例患者,随机分为试验,对照及开放组各20例,试验及开放组静脉滴注SPFX200mg.d^-1,qd;对照组静脉滴注氧氟沙星注射液（OFX）400mg.d^-1,bid;疗程均为5－14d。结果：试验及开放组共40例,总有效率和细菌清除率为95％和93．5％;对照组20例,总有效率和细菌清除率为80％和88．9％。用药中不良反应较轻,试验及开放组发生率5％,对照组发生率10％,结论：本药治疗临床常见的中重度急性细菌性感染疗效高,不良反应小。     

盐酸左氧氟沙星治疗细菌性感染114例临床观察

目的：评价国产盐酸左氧氟沙星注射液治疗急性细菌性感染的有效性与安全性。方法：以盐酸左氧氟沙星注射液治疗急性细菌性感染，每次200mg，静脉滴注，每日2次，疗程7—14日。结果：治疗呼吸系统、泌尿生殖系统细菌性感染114例，临床治愈率与有效率分别为68．42％和88．60％，细菌清除率为94．57％。纸片药敏结果表明临床分离菌对左氧氟沙星、加替沙星、环丙沙星和司帕沙星的敏感率均较高。不良反应发生率为13．16％，主要为恶心、呕吐、头晕、皮疹、转氨酶升高等，试验中未见光敏反应及其他严重不良反应。结论：国产盐酸左氧氟沙星注射液抗菌谱广、抗菌活性强，治疗各种敏感菌所致的急性中、重度感染安全有效。     

甲苯磺酸托氟沙星与司帕沙星双盲双模拟多中心临床与实验研究

目的 本研究以司帕沙星为对照药，对国产二类新药甲苯磺酸托氟沙星进行临床研究，以评价后者的安全性与有效性。方法 采用前瞻性、双盲双模拟、多中心区组随机试验设计。托氟沙星胶囊150mgtid，餐后服用，司帕沙星胶囊300mg,qd，疗程均为7－14d。结果 试验组完成100例、对照组104例。两组各病种的临床有效率分别为88．00％与87．50％；细菌清除率分别为88．51％与86．59％。试验组与对照组各对应指标差异无统计学意义（P＞0．05）。体外抗菌活性研究结果表明，托氟沙星的抗菌活性与司帕沙星、氧氟沙星、环丙沙星相似，对革兰氏阳性菌的抗菌活性明显优于阿奇霉素。甲苯磺酸托氟沙星可引起轻微的消化道症状、短暂中枢兴奋症状及皮疹，其不良反应发生率为12．00％；司帕沙星可引起短暂中枢兴奋症状、轻微消化道症状、光敏反应及实验室肝功的异常，不良反应发生率为16．35％。各对应指标差异无统计学意义（P＞0．05），试验期间未出现严重不良反应。结论 甲苯磺酸托氟沙星作为一种广谱抗菌药物，抗菌活性较强，合理使用可安全有效地治疗由敏感菌引起的轻、中度细菌性感染。     

国产氧氟沙星注射液的临床观察

用国产氯氟沙星注射液治疗细菌性感染143例，临床有效率为94．4％，细菌清除率为91．2％．于下呼吸道及尿路感染中以诺氟沙星注射液作对照，氧氟沙星的疗效明显，优于诺氟沙星．细菌药敏试验提示。大多数临床检出菌对氧氟沙星是敏感的，且与临床疗效相符合。氧氟沙星注射液的血药峰浓度明显高于片剂口服者．     

氟罗沙星与氧氟沙星治疗泌尿生殖系统感染的比较

目的：观察评价氟罗沙星与氧氟沙星治疗泌尿生殖系感染的疗效及安全性。方法：76例病人随机分成2组,治疗组41例,用氟罗沙星0．2－0．4p,po,qd; 对照组35例,用氧氟沙星0．1－0．2g,po,bid,疗程均为7－14d。结果：治疗组临床有效率92．7％,细菌消除率90．4％;对照组分别为91．4％和93．2％;2组间差异间无显著性（P＞0．05）。结论：氟罗沙星治疗泌尿生殖系感染疗效满意,安全方便,无显著不良反应。     

司帕沙星治疗下呼吸道细菌感染52例

目的：观察司帕沙星治疗下呼吸道感染的临床疗效,并与氧氟沙星进行比较。方法：下呼吸道感染患者114例随机分为治疗组,用司帕沙星胶囊300mg,qd;对照组用氧氟沙星胶囊300mg,bid,疗程均为7－14d。结果：两组的临床有效率、细菌清除率、不良反应发生率经统计学处理均差异不显著（P＞0．05）。结论：司帕沙星用于下呼吸道细菌感染的治疗安全有效。     

莫西沙星与司氟沙星治疗泌尿道感染的成本-效果比较

目的评价莫西沙星与司氟沙星治疗泌尿道的疗效．不良反应及成本-效果。方法采用随机．开放,平行对照试验设计。选择泌尿道惑染病例260例．其中可评价病例242例。莫西沙星组（治疗组）121例．蛤予莫西沙星400mg,1日1次,疗程5～10d;司氟沙星（对照组）121例,给予司氟沙星0．3g。1日1次,疗程5～10d。结果莫西沙星组临床总有效率95．07％。司氟沙星组95．9％。两组的细菌清除率分别为95．7％和96．7％．不良反应发生率分别为9．08％和9．09％,两组比较差异均无统计学意义（P〉0．05）,成本效果比分别为2．97和0．92（P〈0．01）。结论司氟沙星的治疗方案为治疗泌尿道感染的较佳方案。     

左旋氧氟沙星治疗老年下呼吸道感染的疗效观察

目的：探讨左旋氧氟沙星治疗老年下呼吸道感染的临床疗效及安全性。方法：左旋氧氟沙星组(50例)应用左旋氧氟沙星0．2g，1日1次，静滴，7—14天。头孢噻肟钠组(50例)应用头孢噻肟钠2．0g，1日2次，静滴，7—14天。结果：左旋氧氟沙星组临床治愈率、有效率，细菌清除株数及不良反应发生率与头孢噻肟钠组比较无显差异。结论：左旋氧氟沙星是有效和安全地治疗老年下呼吸道感染的抗菌药物。     

盐酸左氧氟沙星治疗下呼吸道感染的疗效观察

目的：观察左氧氟沙星治疗下呼吸道感染的临床疗效、细菌清除率和不良反应。方法：80例下呼吸道感染患者随机分为2组，治疗组用盐酸左氧氟沙星注射液0．2g／次，bid，对照组用注射用头孢哌酮钠，2g／次，bid，疗程均为7～14d。结果：治疗组和对照组的临床总有效率分别为90．0％和87．5％，细菌清除率分别为88．6％和88．2％，治疗组和对照组不良反应发生率分别为5.0％和2．5％。结论：左氧氟沙星治疗下呼吸道感染疗效确切、不良反应少而轻微，可作为治疗下呼吸道感染的理想用药。     

加替沙星氯化钠注射液治疗细菌性感染的临床分析

目的：评价加替沙星氯化钠注射液治疗细菌性感染的临床疗效和安全性。方法：以加替沙星氯化钠注射液为试验药，左氧氟沙星氯化钠注射液为对照药，用随机双盲对照的试验方法，治疗细菌性感染，加替沙星和左氧氟沙星剂量均为200mg／次，2次／d，静脉滴注，疗程5～10d。结果：加替沙星总有效率和痊愈率分别为95．1％和85．4％，细菌清除率为86．4％；左氧氟沙星总有效率和痊愈率分别为91．1％和80．2％，细菌清除率为82．2％。二者不良反应发生率分别为11．65％和12．87％，两组比较均无显著差异（P〉0．05）。结论：加替沙星氯化钠注射液治疗细菌性感染疗效确切，患者耐受性良好。     

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.     

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.     

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.