环丙沙星对老年患者茶碱稳态动力学的影响及不良反应观察

本文应用均相酶免疫法分别测定了６名老年慢性阻塞性能肺病患者口服氨茶碱达稳态及稳态后合用环丙沙星３ｄ，对合用前后茶碱的血药浓度及不良反应进行同步观察，以ＰＫＢＰ－Ｎ１程序包按一室模型对数据进行处理，并对结果进行统计分析，结果：环丙沙星使茶碱消除半衰期明显延长（Ｐ＜０．０５），导致血药浓度明显升高（Ｐ＜０．０５），而对分布容积及清除率均无明显影响（Ｐ＞０．０５）。二药合用期间患者出现茶碱不良反应。实验结果提示：环丙沙星抑制茶碱正常代谢，二者合用，应考虑减少茶碱的用量。     

醋酸泼尼松对茶碱药物动力学和唾液监测的影响

采用ＵＶ法测定７名哮喘患者单用氨茶碱和合用醋酸泼尼松后的稳态血清和唾液茶碱浓度。结果显示合用组与单用组茶碱的药动学参数分别为：Ｋ：０．１２８和０．０９９（Ｐ＜０．０１）；Ｔ１／２：６．３和８．６（Ｐ＜０．０５）；ＡＵＣ：５１．４０和７７．０１（Ｐ＜０．０５）；合用组Ｖｄ的ＳＤ较大（Ｐ＜０．００１）。泼尼松使唾液／血清浓度比值不稳定。提示泼尼松使茶碱代谢加快，分布改变。     

倍他乐克对家兔氨茶碱药物动力学参数的影响

本文采用荧光偏振免疫分析法（ＦＰＩＡ）在健康家兔体内考察了倍他乐克对氨茶碱药动学参数的影响。结果表明，倍他乐克可使氨茶碱的分布容积减少（Ｐ＜０．０１），而对茶碱的消除速率常数Ｋ，血药浓度曲线下面积ＡＵＣ未见影响（Ｐ＞０．０５）。     

乳酸左氧氟沙星对肺心病人体内茶碱药动学的影响

应用紫外分光光度法分别测定8例肺心病患者单独静脉滴注氨茶碱及合用乳酸左氧氟沙星达稳态后茶碱的血药浓度,发现乳酸左氧氟沙星明显延长了茶碱的半衰期(P＜0.01),使茶碱达稳态时血药浓度明显升高(P＜0.01),清除率(CL)下降(P＜0.01).提示临床两药合并应用时,应加强茶碱的血药浓度监测,调整用药剂量.     

氟罗沙星葡萄糖注射液治疗细菌感染性疾病150例

目的：验证氟罗沙星葡萄糖注射液对细菌性感染性疾病的疗效及其人安全性。方法：采用随机对照开放试验方法，选用氧氟沙星葡萄糖注射液作对照药。结果；氟罗沙星葡萄糖注射液与氧氟沙星葡萄糖注射液的有效率分别为８７．９％与７４％，差异显著（Ｐ〈０．０１），两组患者细菌清除率为８８．８％和８５．７％（Ｐ〉０．０５）。两组患者不良反应发生率分别为１５．０％和１６．０％，无显著差异（Ｐ〉０．０５）。结论：氟罗沙星葡萄     

氟罗沙星与环丙沙星治疗细菌性感染的比较

目的：评价氟罗沙星注射液对细菌性感染的疗效及安全性。方法：１６２例病人随机分为氟罗沙星治疗组、环丙沙星对照组各６１例和氟罗沙星开放组４０例。氟罗沙星治疗和开放组用氟罗沙星０．２～０．４ ｇ,静脉滴注,ｑｄ;环丙沙星对照组用环丙沙星,０．２～０．４ ｇ,静脉滴注,ｂｉｄ;疗程均为 ７～１４ｄ。结果：氟罗沙星注射液治疗总有效率为 ９３．１％（９３／１０１）与环丙沙星相当,治疗组有效率为９２％（５６／６１）与对照组８２％（５０／６１）相似（Ｐ＞０．０５）;但前者的细菌清除率（９４％）高于后者（８６％, Ｐ＜０． ０５）;不良反应发生率氟罗沙星（６％）也与环丙沙星（８％）相似（Ｐ＞０．０５）。结论：氟罗沙星注射液对细菌性感染有效而安全。     

左氟沙星对健康志愿者和慢性阻塞性肺病患者茶碱药物动力？…

目的：研究左氟沙星（ＬＶＦＸ）对人体茶碱药物动力学的影响。方法：应用均相酶免疫法,通过测定８名健康志愿者、６名慢性阻塞性肺病患者全用ＬＶＦＸ扯前后ｐｏ氨茶碱片的血药浓度,对合用ＬＶＦＸ前后茶碱药物动力学进行对比。结果：合用ＬＶＦＸ前后除患者组茶碱ｔｍａｘ均无显著差异（Ｐ〉０．０５）。结论：ＬＶＦＸ不影响人体茶碱的分布和清除,临床上可与氨茶碱安全合用。     

氟罗沙星注射剂治疗40例尿路感染的临床疗效

目的：比较氟罗沙星与氧氟星注射剂治疗尿路的感染的临床疗效。方法：将８０例尿路感染病例随机分为两组，分别应用氟罗沙星（０．２￣０．４ｇ／ｄ）和氧氟沙星（０．２￣０．４ｇ／ｄ）。结果：氟罗沙星组和氧氟沙星组的总有效率分别为８５％和８０％，细菌清除率分别为９２．５％和８７．５％，两组间无显著差异（Ｐ〉０．０５）。不良反应发生率分别为１２．５％和７．５％（Ｐ〈０．０５）。结论：氟罗生注射剂治疗尿路感染用药     

氟罗沙星葡萄糖注射液的临床疗效观察

目的：将氟罗沙星葡萄糖注射液与氧氟沙星注射液作对比研究。方法：随机选取涉及消化、呼吸、泌尿系统感染的３０例患者，随机分组作对照试验。结果：氟罗沙星注射液与氧氟沙星相比疗效相似，对细菌清除率高，总有效率达到７３．３％（Ｐ〈０．０１）。结论：氟罗沙星葡萄糖注射液疗效确切、不良反应小、使用方便、值得临床推广应用。     

地尔硫卓对兔体内茶碱药物动力学参数的影响

本文采用荧光偏振免疫分析法（ＦＰＩＡ）对单用氨茶碱及氨茶碱与地尔硫合用后，家兔体内茶碱血清药物浓度进行了测定，并对两组药动学参数进行了统计学处理，结果表明，地尔硫略使氨茶碱血药浓度升高，ＡＵＣ合并用药组与对照组有显著差异（Ｐ＜０．０５），其余药动学参数无显著变化。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

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.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.     

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.