氨苄青霉素钠与氨茶碱注射液在氯化钠注射液中的配伍实验

本文将氨苄青霉素钠与氨茶碱注射液在0．9％氯化钠注射液中配伍实验,从物理变化方面观察4h,外观无变化。混合后不同时间测其pH值,略有下降。从化学变化方面,经过4h的紫外测定,单独组与混合组中的氨茶碱在274am处的吸收值基本不变,其氨茶碱青霉素钠在325nm的吸收值略有下降,但P〉0．05,差异无统计学意义。     

盐酸氨溴索注射液与16种常用药物配伍稳定性考察

目的考察室温条件下盐酸氨溴索注射液与16种临床常用药物配伍的稳定性。方法模拟临床应用,按比例将盐酸氨溴索注射液与药物混合,在即刻、2h、6h三个时间点观察配伍溶液外观变化,测定pH值及微粒,对于理化性质未发生明显改变的混合药液进一步用高效液相色谱法测定盐酸氨溴索的含量变化。结果盐酸氨溴索注射液与碳酸氢钠注射液及头孢曲松、头孢哌酮、头孢噻肟配伍时,均立即产生白色浑浊。盐酸氨溴索注射液与替硝唑注射液、氨茶碱注射液、鱼腥草注射液及青霉素配伍后,含量均明显下降。盐酸氨溴索注射液与鱼腥草注射液及丹参注射液配伍后微粒显著增加。结论盐酸氨溴索注射液不宜与碳酸氢钠注射液、替硝唑注射液、氨茶碱注射液、鱼腥草注射液、丹参注射液以及头孢曲松、头孢哌酮、头孢噻肟、青霉素配伍。     

磷酸氯洁霉素与头孢唑肟钠、头孢西丁钠、头孢孟多甲酸酯钠或头孢唑啉钠配伍时注射液的稳定性

作者对磷酸氯洁霉素与头孢唑肟钠,头孢西丁钠,头孢孟多甲酸酯钠或头孢唑啉钠中的一种混合后制成的注射液的稳定性,进行了研究。上述每种抗生素单独,或将氯洁霉素与四种头孢菌素中的一种制成的混合注射液进行了试验。将抗生素与5％葡萄糖和0.9％氯化钠注射液混合,在混合后1、4、8、12、24和48小时测定抗生素的浓度、pH,并目测外观变化。结果表明,上述抗生素单独在o.9％氯化钠或5％葡萄糖注射液中,48小时后其含     

注射用磷霉素钠与多种临床常用注射剂配伍的稳定性

目的:考察注射用磷霉素钠(P-Na)与临床常用药物配伍后的稳定性.方法:将P-Na与51种临床常用药物按临床用药浓度以等体积混合后,观察其0,2,6h外观性状变化,测定pH值.对于理化性质未发生明显改变的混合药液进一步用微生物检定法测定其含量变化.结果:P-Na与盐酸肾上腺素、盐酸氯丙嗪、双嘧达莫、氨基己酸、氯化钙、酚磺乙胺、盐酸多巴胺注射液配伍后出现外观变化.与P-Na配伍后pH值变化≥0.1的有:注射用碳酸氢钠、氨茶碱注射液.贝美格和盐酸精氨酸注射液与P-Na配伍后6 h内P-Na含量降至90%以下.结论:P-Na与盐酸肾上腺素、盐酸氯丙嗪、双嘧达莫、氨基己酸、氯化钙、酚磺乙胺、盐酸多巴胺、碳酸氢钠、氨茶碱、贝美格、盐酸精氨酸注射液不宜配伍使用.     

甲硝唑注射液与三种抗生素的配伍变化

本文将甲硝唑注射液分别与柱晶白霉素,盐酸洁霉素,氯霉素注射液混合,通过薄层层析,紫外分光光度法及旋光法测定。结果表明:混合液在4h 内均无理化配伍禁忌。     

注射用盐酸雷莫司琼与4种输液配伍的稳定性考察

目的考察注射用盐酸雷莫司琼在5％葡萄糖注射液等4种输液中的稳定性。方法在25℃,将注射用盐酸雷莫司琼加入到4种输液中,模拟临床用药浓度,用高效液相色谱法测定配伍后不同时间配伍液的含量,同时检查配伍液的pH值和外观变化。结果注射用盐酸雷莫司琼与4种输液配伍后在25℃放置10h其外观、pH值和含量基本不变。结论注射用盐酸雷莫司琼与4种输液配伍,在10h内基本稳定。     

注射用磷霉素钠与盐酸山莨菪碱注射液配伍的稳定性考察

目的：考察磷霉素钠和盐酸山莨菪碱注射液（654-2）在5％葡萄糖注射液中的配伍稳定性。方法：室温下（10℃）以分光光度法测定两者在5％葡萄糖注射液中2h内吸收曲线、含量变化，同时观察外观、测定pH值。结果：2h内配伍液吸收曲线不变，吸收峰无位移，外观、pH值、含量基本稳定。结论：室温下（10℃）磷霉素钠和654-2在5％葡萄糖注射液中配伍2h是稳定的。     

盐酸溴己新葡萄糖注射液与几种弱碱性药物注射液的配伍变化

目的：考察盐酸溴己新葡萄糖注射液与几种碱性药物注射液混合后的配伍变化。方法：选取临床常用几种不同pH值的弱碱性药物注射液,分别与盐酸溴己新葡萄糖注射液（pH4．2）进行混合实验,观察混合溶液的性状变化,测定其pH值并用高效液相色谱法测定其中盐酸溴己新的含量。结果：盐酸溴己新在碱性条件下极不稳定,与pH较高的常用药物输液如阿莫西林钠／克拉维酸钾输液、阿莫西林钠／氟氯西林钠输液、地塞米松磷酸钠注射液等混合后可产生白色浑浊,使其含量下降。结论：盐酸溴己新葡萄糖注射液（pH4．2）与pH较高的药物输液连续静脉输液时,中间应用5％葡萄糖注射液冲管或分开注射。     

炎琥宁注射液与氨茶碱配伍的稳定性考察

目的：考察室温下，炎琥宁注射液与氨茶碱在0.9%氯化钠溶液中的配伍稳定性。方法：采用新Vierordt法测定炎琥宁与氨茶碱在0.9%氯化钠溶液中配伍24 h内各时间段的含量，同时测定pH值、微粒，观察配伍液的外观变化。结果：室温4 h内，炎琥宁与氨茶碱配伍后pH值、微粒、含量均无明显变化，但溶液呈淡黄色；6 h时，炎琥宁含量、pH值、微粒变化较大，配伍液呈黄色。结论：炎琥宁注射液与氨茶碱可在0.9%氯化钠溶液中配伍，但应现配现用，并且应在配伍后4 h内使用。     

注射用盐酸头孢替安在果糖等4种注射液中的稳定性考察

目的考察注射用盐酸头孢替安在、果糖、转化糖电解质、甘油果糖和混合糖电解质注射液中的稳定性。方法在室温（25℃）条件下,将注射用盐酸头孢替安按临床用药浓度与4种注射液配伍,于不同时间用紫外分光光度法测定配伍液中头孢替安的含量,并观察外观、测定pH值的变化。结果头孢替安与果糖等4种注射液配伍后4h内其外观、pH值及含量均无明显变化。结论室温（25℃）下头孢替安与果糖等4种注射液配伍后4h内稳定。     

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.

     

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.     

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.     

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.