头孢丙烯治疗呼吸道感染的临床研究

目的 :评价国产头孢丙烯片剂治疗呼吸道感染的疗效与安全性。方法 :头孢丙烯片与头孢克洛胶囊随机对照治疗下呼吸道感染 10 1例 ,头孢丙烯组 5 1例 (男性 33例 ,女性 18例 ,年龄 5 0a±s 13a) ,头孢克洛组 5 0例 (男性 2 9例 ,女性 2 1例 ,年龄4 9a± 15a)剂量分别均为 5 0 0mg ,po ,bid及tid ;另用头孢丙烯片 5 0 0mg ,po ,qd开放治疗上呼吸道感染 5 5例 ;疗程均 7～ 14d。结果 :头孢丙烯和头孢克洛治疗下呼吸道感染的有效率分别为 94 %及92 % ,细菌清除率均为 93% ,不良反应发生率分别为 10 %及 8% ,2组比较差异均无显著意义 ,P >0 .0 5。头孢丙烯开放治疗上呼吸道感染 5 5例的有效率为 94 % ,细菌清除率为 90 % ,不良反应发生率为4 %。结论 :头孢丙烯片剂治疗呼吸道感染疗效确切 ,不良反应少见而轻微     

头孢丙烯治疗急性细菌性下呼吸道感染的临床疗效评价

目的 :评价头孢丙烯治疗急性细菌性下呼吸道感染的临床有效性、安全性。方法 :轻、中度急性细菌性下呼吸道感染病人 115例随机分成 2组 ,头孢丙烯组 5 8例 (男性 37例 ,女性 2 1例 ;年龄 4 7a±s 13a)予头孢丙烯 5 0 0mg ,po ,bid ;头孢克洛组5 7例 (男性 34例 ,女性 2 3例 ;年龄 4 9a± 12a)予头孢克洛 5 0 0mg ,po ,tid。 2组均以 7～ 14d为一个疗程。结果 :头孢丙烯组与头孢克洛组的临床有效率分别为 93%与 91% (P >0 .0 5 ) ,细菌清除率为92 %与 89% (P >0 .0 5 ) ,2组均无明显不良反应。结论 :头孢丙烯可作为治疗轻、中度急性细菌性下呼吸道感染有效和安全的抗生素     

头孢克肟治疗小儿呼吸道感染

目的探讨头孢克肟和头孢克洛治疗小儿呼吸道感染的临床疗效。方法将60例呼吸道感染患儿随机分为治疗组和对照组，分别口服头孢克肟颗粒剂（1．5—3mg/kg，tid）和头孢克洛干混悬剂（20mg／kg，tid），比较两者的疗效和安全性。结果治疗组和对照组的总有效率分别为90．0％和80．0％，细菌清除率分别为80．8％和64．0％，不良反应两组无统计学差异。结论头孢克肟治疗小儿呼吸道感染效果佳，安全性高。     

头孢丙烯治疗细菌性感染31例

目的:评价头孢丙烯的疗效及安全性.方法:以头孢丙烯和头孢克洛随机对照治疗急性轻、中度呼吸道及皮肤软组织感染,31例患者接受头孢丙烯(250～500 mg,2次/d)、35例患者接受头孢克洛(250～500 mg,3次/d)治疗,疗程7～14 d.结果:治疗组和对照组的痊愈率和总有效率分别为77.4%,80.0%(P＞0.05)与96.8%,94.3%(P＞0.05);细菌阳性率、清除率分别为87.1%,88.6%(P＞0.05)和96.3%,93.5%(P＞0.05);不良反应发生率分别为4.7%和4.3%(P＞0.05).结论:头孢丙烯治疗轻、中度细菌感染安全、有效.     

头孢克洛缓释片与头孢丙烯片对照治疗慢性支气管炎急性发作

目的: 比较头孢克洛缓释片与头孢丙烯片治疗慢性支气管炎急性发作(AECB)的有效性和安全性。方法:多中心随机单盲平行对照设计。缓释头孢克洛组予头孢克洛缓释片750mg,bid;头孢丙烯组予头孢丙烯500mg,bid,疗程均为7d。结果:202例AECB病人入选,缓释头孢克洛组102例,头孢丙烯组100例。治疗前2组基础情况、症状、体征和峰流速均具可比性。治疗后按意向性分析(ITT)和按方案分析(PP)缓释头孢克洛组和头孢丙烯组的临床有效率分别为84. 0 %, 74. 5 %和85. 4 %,74. 7 %,细菌学清除率分别为83 %和79 %, 2组间比较差别无显著意义(P>0. 05 );不良事件发生率缓释头孢克洛组7. 8 %,头孢丙烯组为6. 0 %, 2组比较差别无显著意义(P>0. 05)。结论:AECB病人应用头孢克洛缓释片750mg,bid,连续7d治疗,疗效确切,不良反应发生率低,与头孢丙烯相仿。     

头孢丙烯和头孢克洛治疗轻中度社区获得性下呼吸道感染的药物经济学分析

社区获得性下呼吸道感染中常见的疾病有急性支气管炎、慢性支气管炎急性加重、社区获得性肺炎及其他疾病合并肺部感染等.其主要致病菌为肺炎链球菌,其次为流感嗜血杆菌.头孢丙烯(cefprozil)和头孢克洛(cefaclor)均为第二代口服头孢菌素,对肺炎链球菌、流感嗜血杆菌等所致的下呼吸道细菌性感染有很好的抗菌作用.本文根据蔡柏蔷等[1]治疗158例社区获得性下呼吸道感染病人的研究进行成本-效果分析,旨在为临床合理用药和治疗决策提供客观依据.     

头孢丙烯及头孢克洛治疗下呼吸道感染的药物经济学

目的:从医疗服务供给者的角度分别评价头孢丙烯及头孢克洛用于治疗社区获得性轻、中度下呼吸道感染的药物经济学特性.方法:采用前瞻性、多中心、开放式、随机对照的临床研究方法验证药物临床疗效及安全性.采用药物经济学中的最小成本分析法对药物的治疗成本及效果进行经济学评价.结果:在所采用的治疗方案条件下,实验组头孢丙烯与对照组头孢克洛相比,在临床疗效、细菌清除率及不良反应发生率方面,差异无显著性(P>0.05),但头孢丙烯组的治疗总费用及抗生素费用均明显低于对照组(P<0.01).结论:头孢丙烯用于治疗社区获得性轻、中度下呼吸道感染是有效、安全且经济的.     

头孢呋辛酯治疗下呼吸道感染45例

目的 观察头孢呋辛酯治疗下呼吸道感染的疗效。方法 将90倒下呼吸道感染患者随机均分为两组，治疗组45例口服头孢呋辛酯（250HIg／次，2次L／d），对照组45例口服头孢克洛（250mg／次，3次L／d），疗程均为5-10d。结果 治疗组和对照组的治愈率分别为57，78％和37-78％（P〈O．05），总有效率分别为88．89％和84．44％（P〉0．05），细菌清除率分别为87．80％和85．00％（P〉0．05），不良反应发生率均为4．44％。结论 头孢呋辛酯治疗细菌性下呼吸道感染安全、有效。     

法罗培南钠片治疗细菌性感染的随机双盲对照临床研究

目的评价国产法罗培南钠片治疗细菌性感染的临床疗效与安全性。方法采用多中心、双盲、随机对照试验设计，以头孢克洛为对照药，两组均口服，每次2片，tid，疗程5～10d。结果本研究共纳入60例，法罗培南组和头孢克洛组各30例，其中法罗培南组及头孢克洛组纳入ITT分析均为30例，PP分析分别为28和30例。疗程结束时，呼吸系统PP人群中，法罗培南组与头孢克洛组治疗后总痊愈率和有效率分别为71．43％与47．67％和92．86％与93．33％，泌尿道PP人群中，法罗培南组与头孢克洛组总痊愈率和有效率分别为85．71％与73．33％和100％与93．33％。疗程结束时两组细菌清除率均分别为83．33％和79．17％，法罗培南组和头孢克洛组的不良反应发生率分别为10．71％和20％，主要表现为恶心、呕吐、头晕、皮疹、腹泻等。以上结果两组比较无统计学差异（P〉0．05）。结论国产法罗培南钠片治疗呼吸道感染和泌尿道感染疗效确切，安全性较好。     

多药联合治疗老年细菌性下呼吸道感染的对照观察

目的：评价头孢哌酮,舒巴坦和头孢哌酮,舒巴坦加头孢克洛序贯疗法治疗老年细菌性下呼吸道感染的临床疗效及成本效果分析。方法：将75例老年细菌性下呼吸道感染患者随机分为治疗组和对照组,治疗组予头孢哌酮,舒巴坦2g静滴,然后给予头孢克洛250mg,po,bid;对照组予头孢哌酮,舒巴坦2g静滴,bid,治疗组和对照组均治疗8～10d。结果：对照组和治疗组痊愈率分别为62．1％和63．2％,总有效率分别为91．9％和92．1％,治疗后细菌清除率分别为84．8％和86．6％;两组以上结果差异均无统计学意义（P〉0．05）。序贯疗法整个疗程平均节省1193元。结论：头孢哌酮／舒巴坦加头孢克洛序贯疗法治疗老年细菌性下呼吸道感染．临床疗效显著,比单用头孢哌酮／舒巴坦更具成本效果,患者依从性好。     

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.

     

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.     

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.     

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.