头孢匹胺与头孢哌酮随机对照治疗细菌性感染127例临床研究

为评价头孢匹胺治疗细菌性感染的疗效和安全性,以头孢匹胺与头孢哌酮随机对照治疗１２７例患者,主要为下呼吸道,尿路等细菌性感染。两药剂量均每日２－４ｇ,疗程７－１４ｄ,头孢匹胺组６３例,头孢哌酮组６４例,两组有效率分别为８７．３％和９０．６％,愈率为５５．６％和６０．９％,细菌清除率为８４．７％和８９．７％。     

头孢吡肟与头孢他啶治疗细菌性感染的药物经济学评价

目的：比较头孢吡肟与头孢他啶治疗细胞性感染的经济效益和安全性，方法：选择120例细菌性感染病人，进行随机对照治疗观察，头孢吡肟组，头孢他啶组各60例，给药方案为：治疗尿道感头孢吡肟每次1g，2次／d，头孢他啶每次1g，3次／d；其他感染头孢吡肟每次2g,2次／d，头孢他啶每次2g,3次／d；静脉滴注，疗程均为7－14d。采用药物经济学中的成本－效果分析方法。结果：头孢吡肟，头孢他啶治疗细菌性感染有效率分别为91．67％，90．00％，痊愈率分别为70．00％，66．67％。两组药物不良反应发生率分别为8．33％，10．00％，3种细菌性感染类型头孢吡肟的成本－效果比均低于头孢他啶，结论：头孢吡肟治疗细菌性感染的经济效果优于头孢他啶。     

头孢硫脒治疗小儿急性细菌性呼吸道感染疗效观察

目的 观察头孢硫脒治疗小儿急性细菌性呼吸道感染的疗效。方法 129例经临床确诊为急性细菌性呼吸道感染病儿，随机分成两组。观察组84例应用头孢硫脒治疗，按每日每公斤50mg，一日一次静脉滴注；对照组45例，应用头孢呋辛治疗，按每日每公斤50mg，一日两次静脉滴注；观察期间不并用其他抗生素，疗程为5～7d。结果 头孢硫脒治疗组总有效率为95．2％，细菌清除率为75％；头孢呋辛治疗组总有效率为75．5％．细菌清除率为42．86％，观察组痊愈率优于对照组（P〈0．01）。结论 头孢硫脒适用于小儿急性细菌性呼吸道感染，疗程短，不良反应少，值得推广应用。     

注射用盐酸头孢甲肟与头孢哌酮治疗急性细菌性感染随机对照临床研究

目的 评价盐酸头孢甲肟注射剂治疗急性细菌性呼吸道和泌尿道感染的有效性和安全性。方法 用双盲随机平行对照试验方法，以头孢哌酮为对照药，头孢甲肟和头孢哌酮用量均为2．0～4．0g，每日2次静滴，疗程7～14天。结果头孢甲肟入选72例，疗效评价64例，安全性评价72例；头孢哌酮入选72例，疗效评价69例，安全性评价72例。头孢甲肟和头孢哌酮临床总有效率分别为96．9％，91．3％；治疗各种致病菌感染临床有效率分别为98．3％，93．4％；细菌清除率分别为94．9％，91．8％。药物不良反应发生率均为5．6％。结论 注射用头孢甲肟治疗急性细菌性呼吸道和泌尿道感染有效、安全，优于头孢哌酮。     

阿奇霉素治疗下呼吸道感染疗效观察

目的 观察阿奇霉素对下呼吸道感染的疗效。方法 300例下呼吸道感染患者分为两组：阿奇霉素组150例，用阿奇霉素0．5g，每日1次静滴连续5天；另150例用头孢唑林2g，每日2次静滴连续5天。结果 总有效率分别为96．7％和98．7％，不良反应发生率分别为14％和16％。结论 阿奇霉素对治疗下呼吸道感染具有良好的疗效，与茶碱药有协同作用，对耐药菌导致感染有补充替代治疗作用，不良反应少。     

头孢克洛缓释胶囊治疗呼吸道感染189例观察

目的 观察头孢克洛缓释胶囊（曼宁）治疗呼吸道感染的临床疗效和安全性。方法 口服头孢克洛缓释胶囊0．5g／次，2次／d，疗程7～10d。结果 总有效率86．2％，细菌清除率83．8％，不良反应发生率1．6％。结论 头孢克洛缓释胶囊治疗下呼吸道感染安全有效。     

头孢呲肟与头孢噻肟治疗老年细菌性下呼吸道感染的随机对比研究

目的 :评价头孢吡肟治疗老年细菌性下呼吸道感染的临床疗效和安全性。方法 :将 68例老年细菌性下呼吸道感染患者随机分为试验组和对照组 ,分别给头孢吡肟静滴 1g ,每日二次或头孢噻肟静滴 2g ,每日二次 ,疗程均为 7～ 10d。结果 :两组痊愈率分别为 5 8.8%和 2 6.5 %,总有效率分别为 91.2 %和 67.6%;治疗后细菌清除率分别为 89.7%和 63 .3 %;以上结果均有显著性差异。不良反应发生率分别为 5 .9%和 8.8%,两组比较无显著性差异。结论 :头孢吡肟抗菌谱广 ,疗效好 ,不良反应轻微 ,对治疗老年细菌性下呼吸道感染是一个安全、有效的抗感染经验治疗药物     

头孢呋辛酯头孢他美酯治疗急性细菌性感染

目的：比较头孢呋辛酯与头孢他美酯治疗急性细菌性感染的安全性。方法：119例患者随机分成两组，头孢呋辛酯组60例，用头孢呋辛酯0．25g，口服，一日两次；头孢他关酯组59例，用头孢他美酯0.25g，口服，一日两次，疗程均为7～14d。结果：两组临床总有效率分别为96％、95％，细菌清除率分别为95％、95％，不良反应发生率分别为6％、5％。结论：头孢呋辛酯与头孢他美酯治疗急性细菌性感染安全、有效。     

121例头孢匹胺治疗细菌性感染临床疗效及安全性评价

目的：观察头孢匹胺治疗细菌性感染临床疗效和安全性。方法：121例细菌性感染患者,采用注射用头孢匹胺钠1.0～2.0g,加入9.0mg/mL氯化钠注射液250mL,q12h,静滴,疗程7～14d。结果：治疗细菌性感染121例患者痊愈78例,显效32例,进步5例,无效6例,平均痊愈率与有效率分别为64.46%,90.91%;ADR发生率为7.44%（9/121）,未发现严重ADR。结论：头孢匹胺钠对细菌性感染疗效好,安全性高。     

国产头孢泊肟酯片治疗下呼吸道细菌性感染40例

目的评价国产头孢泊肟酯片治疗下呼吸道细菌性感染的有效性和安全性。方法将78例轻度及中度下呼吸道细菌性感染患者随机分为2组，治疗组40倒口服头孢泊肟酯片200mg（2次／d），对照组38例口服头孢克洛片500mg（3次／d），疗程均为7～14d。结果治疗组与对照组临床有效率分别为87.5％与81．6％，细菌清除率分别为89.2％与85.0％，两组均无明显不良反应。结论采用头孢泊肟酯片治疗下呼吸道细菌性感染安全、有效。     

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.

---

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.     

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.     

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.     

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.