左氧氟沙星、氧氟沙星和洛美沙星对小鼠呼吸道感染的治疗作用比较

用1.29×107CFUs肺炎杆菌滴鼻,引起小鼠呼吸道感染,未治疗组的动物大部分死亡。本文比较了左氧氟沙星、氧氟沙星和洛美沙星对小鼠呼吸道感染的治疗作用。结果发现感染20h后,40mgkg的左氧氟沙星可使小鼠肺研磨液中的细菌数由每毫升109.29减少到105.84,其ED50分别为氧氟沙星和洛美沙星的2.25和2.42倍,说明左氧氟沙星的疗效明显优于氧氟沙星和洛美沙星。     

氧氟沙星与左氧氟沙星不良反应个案调查与分析

目的分析氧氟沙星与左氧氟沙星近10年药物不良反应(ADR)的异同。方法从CNKI数据库和维普数据库中检索两药不良反应的个案报道,用Epi-data软件收集患者性别、年龄、用药原因、给药途径、给药剂量、不良反应发生时间及表现等并进行分析。结果本次调查共收集不良反应报道氧氟沙星48篇(54例),左氧氟沙星133篇(175例),用药病因均以呼吸系统感染为主(46.3%vs 41.7%)。2种药物相同ADR为癫痫大发作、抽搐、谵妄、震颤、过敏性休克等。结论氧氟沙星与左氧氟沙星的不良反应不尽相同。     

左氧氟沙星治疗细菌性感染的疗效观察

目的以左氧氟沙星注射液和洛美沙星注射液随机对照治疗中、重度急慢性呼吸道、泌尿道感染，评价左氧氟沙星的疗效和安全性。方法108例病人随机分成两组，左氧氟沙星组59例（男35例，女24例）用左氧氟沙星0．2g静脉滴注bid，洛美沙星组49例（男25例，女14例），用洛美沙星0．2g静脉滴注bid，5～8d为一疗程。结果左氧氟沙星有效率为92％，不良反应率为3．3％，洛美沙星组分别为84％、6.12％。两组相比差异无显著性意义（P〉0．05）。结论左氧氟沙星治疗细菌引起的各种感染疗效显著，不良反应少。     

输注氧氟沙星和左氧氟沙星致静脉炎的观察及防治措施

目的 观察输注氧氟沙星和左氧氟沙星致静脉炎的一般规律和特点,并探讨其原因和防治措施.方法 对2008-2011年静脉榆注氧氟沙星和左氧氟沙星致静脉炎病例进行回顾性分析.结果 氧氟沙星和左氧氟沙星所致静脉炎分别为39.80％和16.73％,并且氧氟沙星所致Ⅱ、Ⅲ级静脉炎的比例(20.41％)较左氧氟沙星(6.12％)为多,两药比较差异有统计学意义(P＜0.01).结论 输注氧氟沙星较左氧氟沙星所致静脉炎为多,且程度较重,提示临床选择两药时应首选左氧氟沙星;在输注两药过程中要加强巡视、控制滴速、注意保暖等,可预防或减少静脉炎的发生.     

左氧氟沙星治疗甲型副伤寒的临床用药分析

目的:探讨左氧氟沙星治疗甲型副伤寒的临床疗效。方法:对24例左氧氟沙星治疗组患者和19例洛美沙星对照组患者进行比较研究,比较用药前后两组患者体温、血尿常规、肝肾功能,治疗前及疗程结束后做血培养及免疫学检查。结果:左氧氟沙星用药5～7d内可见患者体温恢复正常,血培养未见活菌生长,免疫学检查阴性。结论:左氧氟沙星可有效治疗甲型副伤寒,疗效与洛美沙星相近。     

门冬氨酸左氧氟沙星与其他左氧氟沙星盐的药动学比较

目的对门冬氨酸左氧氟沙星与其他左氧氟沙星盐在大鼠体内进行了药动学比较。方法以替硝唑为内标,血浆样品经乙腈沉淀蛋白后,采用高效液相的方法进行了测定。结果线性范围0.5~25μg/m l,日内、间精密度RSD均<6%,平均回收率大于89%。大鼠腹腔注射门冬氨酸左氧氟沙星、盐酸左氧氟沙星、乳酸左氧氟沙星和左氧氟沙星,测定不同时间的药物浓度,所得的主要药物动力学参数:门冬氨酸左氧氟沙星t1/2K a=7.461m in、t1/2α=16.499m in、t1/2β(m in)=218.989m in、tm ax=22.600m in、AUC=1202.262(μg.m in)/m l;盐酸左氧氟沙星t1/2K a=0.064m in、t1/2K e=24.155m in、tm ax=3.433m in、Cm ax=10.946μg/m l、AUC=420.925(μg.m in)/m l;乳酸左氧氟沙星t1/2K a=0.409m in、t1/2K e=13.576m in、tm ax=2.131m in、Cm ax=13.042μg/m l、AUC=282.797(μg.m in)/m l;左氧氟沙星t1/2K a=0.977m in、t1/2K e=8.519m in、tm ax=3.448m in、Cm ax=13.624μg/m l、AUC=221.667(μg.m in)/m l。结论门冬氨酸左氧氟沙星在大鼠体内的生物利用度比左氧氟沙星及其盐有所提高。     

左氧氟沙星片剂的溶出度考察

左氧氟沙星 (levofloxacin)为新的喹诺酮类抗菌药物 ,其抗菌作用强于氧氟沙星 ,临床使用越来越普遍。但由于左氧氟沙星片剂的来源不同 ,各厂家制剂的辅料及工艺不同 ,药物体外溶出速度就有所不同 ,同时各厂家产品的价格也有出入。为选择质好价廉的新药 ,我们采用高效液相色谱法 ,对左氧氟沙星的国产及进口片剂进行了体处溶出度测定。1　仪器与试剂1 .1仪器　WATERS- 51 5泵和 2 4 87紫外检测器 ,ZRS- 8型智能溶出试验仪 (天津大学无线电厂 )。1 .2试剂　左氧氟沙星标准品 (浙江省药品检验所 ) ;左氧氟沙星片 A(日本 ,分装批号 2 0 0 0 0…     

思密达对盐酸左氧氟沙星的体外吸附作用

目的探讨思密达对盐酸左氧氟沙星的体外吸附作用。方法采用不同剂量的盐酸左氧氟沙星与思密达混合于人工胃液和人工肠液中,在(37±0.5)℃水浴恒温,每隔15min振摇1次,2h后过滤,用紫外分光光度法测定盐酸左氧氟沙星的含量变化。结果在人工胃液和人工肠液中,思密达对盐酸左氧氟沙星的吸附率分别为(99.73±0.1)%和(99.71±0.1)%。结论思密达对盐酸左氧氟沙星有极强的吸附作用,因此应避免两种药物同时服用。     

复方左氧氟沙星锌洗剂的制备及临床应用

目的 制备左氧氟沙星锌与氧化锌组成的复方洗剂。方法 利用左氧氟沙星为两性物质,能与锌离子结合成左氧氟沙星锌的金属盐,采用氢氧化钠法制备左氧氟沙星锌,并利用紫外分光光度法测定左氧氟沙星的含量。结果 左氧氟沙星的平均回收率为100．51％,RSD为0．38％(n=3)。结论 本法操作简便,结果准确。     

蒙脱石散对盐酸左氧氟沙星体外吸附的影响

目的: 探讨蒙脱石散对盐酸左氧氟沙星体外吸附的影响.方法: 采用不同剂量的盐酸左氧氟沙星分别与3 g蒙脱石散混合,加入0.1 mol·L-1盐酸溶液中,在(37±0.5)℃水浴中恒温2 h后过滤,用紫外分光光度法测定盐酸左氧氟沙星的含量变化.结果: 蒙脱石散对盐酸左氧氟沙星的吸附率为(98.37±0.03)%.结论: 蒙脱石散对盐酸左氧氟沙星有极强吸附,因此应避免两种药物同时服用.     

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.