甲磺酸帕珠沙星治疗呼吸道细菌性感染的临床研究

目的:评价国产注射用甲磺酸帕珠沙星治疗呼吸道细菌感染的疗效和安全性.方法:采用多中心双盲随机对照试验设计,共入选病例124例,脱落1例,剔除5例,可评价病例118例,试验组59例,对照组59例.试验组应用甲磺酸帕珠沙星注射剂0.5 g·次-1,bid,静滴;对照组应用盐酸左旋氧氟沙星注射剂0.3 g·次-1,bid,静滴,疗程7～14 d.结果:试验组与对照组的痊愈率分别是71.19%和66.10%,总有效率分别为98.31%和94.92%;两组细菌清除率分别为95.83%和93.62%;两组不良反应率分别为4.84%和3.23%.两组比较差异均无显著性(P＞0.05).结论:国产注射用甲磺酸帕珠沙星治疗呼吸道细菌性感染疗效确切,安全性好.     

甲磺酸帕珠沙星注射液治疗泌尿系统感染的疗效评价

目的分析和评价甲磺酸帕珠沙星注射液治疗泌尿系统感染的疗效及其安全性。方法选取50例泌尿系统诊断明确的患者,随机分成甲磺酸帕珠沙星组与左氧氟沙星组,分别以甲磺酸帕珠沙星注射液和左氧氟沙星作为对照治疗,治疗7～14d,观察其疗效及安全性。结果甲磺酸帕珠沙星组与左氧氟沙星组的痊愈率分别为72%和64%,显效率分别为28%和36%,甲磺酸帕珠沙星疗效有略升高优势,但没有统计学上的差异(P>0.05),表明两者在治疗泌尿系统的感染时具有相当的药理效能,其总有效率均为100%。结论甲磺酸帕珠沙星注射液的临床疗效确切,安全性高,适应于中、重度泌尿路感染,在临床值得推广和使用。     

注射用甲磺酸帕珠沙星与左旋氧氟沙星对照治疗呼吸道感染74例

目的:评价国产注射用甲磺酸帕珠沙星治疗呼吸道细菌感染的临床疗效和安全性。方法:采用随机对照试验设计,以注射用盐酸左氧氟沙星为对照药,试验组用甲磺酸帕珠沙星注射剂,每次0.3 g,bid,静脉滴注;对照组用盐酸左氧氟沙星注射剂,每次0.2 g,bid,静脉滴注,疗程7~14 d。结果:本研究共入选病例76例,剔除2例,可评价病例74例,试验组35例,对照组39例。试验组与对照组的痊愈率分别为65.7%(23/35)和56.4%(22/39),总有效率分别为94.3%(33/35)和97.4%(38/39),细菌清除率分别为74.2%(23/31)和74.3%(26/35),不良反应率分别为5.7%(3/35)和7.7%(3/39)。结论:国产注射用甲磺酸帕珠沙星治疗呼吸道细菌性感染疗效确切,安全性好。     

甲磺酸帕珠沙星治疗女性非淋菌性泌尿生殖道炎的临床观察

目的探讨甲磺酸帕珠沙星治疗女性非淋菌性泌尿生殖道炎的有效性和安全性。方法采用对照研究,试验组50例,采用甲磺酸帕珠沙星氯化钠注射液0.3g,静脉滴注,1日1次,共1周;对照组50例,盐酸左氧氟沙星注射液0.3g,静脉滴注,1日1次,共1周。结果两组痊愈、有效、无效病例分别为47、3、0和27、13、10例,经Ridit分析差异有统计学意义(P<0.05);不良反应发生率分别15.6%和18.7%,差异无统计学意义(P>0.05)。结论甲磺酸帕珠沙星治疗女性非淋菌性生殖道炎安全有效。     

帕珠沙星注射液治疗呼吸和泌尿系统细菌性感染的单盲随机对照试验

目的:评价帕珠沙星注射液治疗呼吸系统和泌尿系统急性细菌感染的有效性和安全性。方法:用随机单盲对照试验设计,试验组予帕珠沙星注射液,300mg,iv,gtt,bid,对照组予左氧氟沙星注射液,200mg,iv,gtt,bid,2组疗程均为7～14d。结果:试验组可评价病例为31例,对照组可评价病例为33例,试验组临床总有效率和痊愈率分别为94%和58%,细菌清除率为100%;对照组临床总有效率和痊愈率分别为94%和67%,细菌清除率为100%。试验组和对照组药物不良反应发生率分别为10%(3/31)和39%(13/33)。2组比较除不良反应发生率差异有显著意义外,其余差异均无显著意义(P>0.05)。结论:帕珠沙星注射液治疗呼吸系统和泌尿系统急性细菌感染疗效确切,使用安全、方便。     

注射用甲磺酸帕珠沙星与左旋氧氟沙星对照治疗呼吸道感染74例

目的：评价国产注射用甲磺酸帕珠沙星治疗呼吸道细菌感染的临床疗效和安全性。方法：采用随机对照试验设计,以注射用盐酸左氧氟沙星为对照药,试验组用甲磺酸帕珠沙星注射剂，每次0.3g，bid,静脉滴注;对照组用盐酸左氧氟沙星注射剂，每次0.2g, bid,静脉滴注,疗程7～14d。结果：本研究共入选病例76例,剔除2例,可评价病例74例,试验组35例,对照组39例。试验组与对照组的痊愈率分别为65.7%（23/35）和56.4%（22/39）,总有效率分别为94.3%（33/35）和97.4%（38/39）,细菌清除率分别为74.2%（23/31）和74.3%（26/35）,不良反应率分别为5.7%（3/35）和7.7%（3/39）。结论：国产注射用甲磺酸帕珠沙星治疗呼吸道细菌性感染疗效确切,安全性好。     

甲磺酸帕珠沙星治疗急性呼吸道感染的疗效观察

目的评价甲磺酸帕珠沙星治疗急性呼吸道感染的疗效。方法选择符合诊断标准的患者122例,随机分为2组(各61例),实验组应用甲磺酸帕珠沙星注射液,对照组应用盐酸左氧氟沙星氯化钠注射液。结果实验组的痊愈率、有效率为70.49%、98.36%,对照组为63.93%、93.44%;实验组的细菌清除率为100%,对照组为98.04%;实验组的不良事件发生率为8.2%,对照组为3.28%,均无显著性差异(P>0.05)。结论甲磺酸帕珠沙星在治疗急性呼吸道感染中有较好的临床疗效和安全性。     

帕珠沙星注射液治疗急性细菌性感染104例的多中心随机对照试验

目的:评价国产帕珠沙星注射液治疗急性细菌性感染的有效性和安全性。方法:采用多中心、双盲、随机对照研究方法,试验组104例,给予帕珠沙星500mg,对照组103例,给予左氧氟沙星200mg,均bid,疗程7～14d。结果:本研究共纳入207例病人,帕珠沙星组104例,男性28例,女性76例,年龄(38±14)a;左氧氟沙星组103例,男性40例,女性63例,年龄(41±15)a。试验组总痊愈率和有效率分别为84.6%和95.2%;对照组分别为79.6%和89.3%,2组细菌清除率分别为97%和91%,2组比较差异均无显著意义(P>0.05)。2组不良反应发生率分别为7.3%和7.3%,主要表现为转氨酶升高、局部刺激、恶心、呕吐、头痛、头晕、失眠、皮疹。结论:帕珠沙星注射液治疗急性细菌性感染临床疗效确切,安全性较好。     

帕珠沙星与左氧氟沙星治疗尿路感染的疗效比较

目的比较帕珠沙星与左氧氟沙星治疗尿路感染的疗效。方法尿路感染患者60例随机分成帕珠沙星组与左氧氟沙星组各30例,分别给予帕珠沙星300mg,左氧氟沙星200mg,均为静脉滴注,bid,疗程5~14d。结果帕珠沙星组与左氧氟沙星组的有效率分别为96.4%和92.6%,痊愈率分别为85.7%和70.3%,均差异无显著性(P>0.05)。结论帕珠沙星与左氧氟沙星治疗尿路感染的临床疗效相当。     

甲磺酸帕珠沙星氯化钠注射液治疗急性细菌性感染多中心临床研究

目的 评价甲磺酸帕珠沙星氯化钠注射液治疗临床常见细菌性感染的安全性和有效性。方法 用随机单盲平行对照多中心同步试验法。甲磺酸帕珠沙星氯化钠注射液(试验组)每次500mg，盐酸左氧氟沙星氯化钠注射液(对照组)每次400mg，均每日1次，静脉滴注，疗程均7～14天。共入选病例251例，其中：试验组122例，临床疗效评价病例115例，安全性评价例数122例；对照组129例，临床疗效评价病例122例，安全性评价例数129例。结果 2组临床总有效率分别为96．5％和98．4％；细菌清除率分别为98．9％和98．0％；药物不良反应发生率分别为11．5％和9．35％。结论 甲磺酸帕珠沙星氯化钠注射液治疗临床常见细菌性感染安全、有效。     

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.     

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.     

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.