奥曲肽联合抗生素治疗肝硬化食管静脉曲张出血

目的　观察奥曲肽联合抗生素治疗肝硬化食管静脉曲张出血 (EVB) ,探讨抗生素对奥曲肽止血效果的影响及其机理。 方法　10 0例肝硬化食管静脉曲张出血患者 ,随机分为二组 ,分别为奥曲肽和奥曲肽联合抗生素组 ,进行临床疗效的对比观察。 结果　奥曲肽组患者 6h、12h、2 4h止血率分别为 30 %、4 2 %、70 % ,奥曲肽联合抗生素组 6h、12h、2 4h止血率分别为 4 8%、72 %、94 % ,两组间比较 ,12h、2 4h止血率均存在显著差异 (P <0 .0 1) ;治疗前后患者血清一氧化氮 (NO)含量分别为 :奥曲肽组 (7.0± 0 .81) μmol/L、(6 .4 %± 0 .91) μmol/L ,奥曲肽联合抗生素组 (7.2± 0 .6 6 ) μmol/L、(5 .5± 0 .83) μmol/L(P <0 .0 1)。 结论　奥曲肽联合抗生素能显著提高肝硬化食管静脉曲张出血的止血效果 ,其机理可能与抗生素减轻肝硬化患者内毒素血症 ,降低血清NO含量有关。     

丙氟沙星对奥曲肽治疗食管静脉曲张出血的影响

目的 :探讨丙氟沙星对奥曲肽治疗食管静脉曲张出血 (EVB)的影响及其机理 :方法 :6 0例EVB患者 ,随机分 2组 ,分别给予奥曲肽、奥曲肽联合丙氟沙星治疗。结果 :EVB患者 6、12、2 4h止血率、治疗前后血清一氧化氮 (NO)含量 ,奥曲肽组分别为 2 7%、40 %、6 3%、(6 9± 0 8)umol L、(5 6± 0 9)umol L(P <0 .0 5 ) ;奥曲肽联合丙氟沙星组分别为 5 0 %、70 % (P <0 .0 5 )、93% (P <0 .0 5 )、(7.3± 0 .6 )umol L、(4.3± 0 .7)umol L(P<0 .0 5 )。结论 :丙氟沙星明显提高奥曲肽治疗EVB的疗效 ,其机理可能与降低血清NO含量有关。     

国产醋酸奥曲肽注射液治疗食管胃静脉破裂出血的疗效

目的:评价国产醋酸奥曲肽注射液治疗食管胃静脉曲张破裂出血的有效性和安全性.方法:采用随机、单盲、平行对照、多中心临床研究.入选97例患者随机分为试验组66例和对照组31例,分别用醋酸奥曲肽注射液和善宁注射液,用法均为0.1mg静脉推注,随后以0.6mg溶于5%葡萄糖注射液500mL中静脉滴注,q12h,24h内出血停止者,再连续用4d.结果:24h止血试验组53例,止血成功率为80.30%;对照组止血27例,止血成功率为90.0%,两组比较差异无显著性(P=0.381 5).治疗期间再出血率试验组和对照组分别为17.0%和7.4%,差异无显著性(P=0.225 2).试验组3,6,12,24h止血率分别为6.06%,27.27%,48.48%,80.30%;对照组分别为0%,23.33%,50.00%,90.00%,差异无显著性(P=0.599 3).试验组给予输血31例,最大输血量为2 800mL,平均输血量为725.16mL.对照组输血人数为17例,最大输血量为800mL,平均输血量为480.00mL,差异无显著性.在研究过程中未发现与药物有关的不良反应.结论:国产醋酸奥曲肽注射液是治疗食管胃静脉曲张破裂出血的安全有效的药物.     

两种奥曲肽治疗食管 胃底 静脉曲张破裂出血的疗效比较

［摘要］目的比较国产奥曲肽和进口奥曲肽治疗食管 胃底静脉曲张破裂出血（EGVB）的疗效。方法肝硬化EGVB患者48例，随机分成治疗组和对照组各24例。治疗组给予国产奥曲肽0.1 mg 静脉注射，之后以25 μg&#8226;h-1持续静脉泵入5 d；对照组给予进口奥曲肽0.1 mg 静脉注射，之后以25 μg&#8226;h-1持续静脉泵入5 d。结果治疗组72 h止血率、平均止血时间、再出血率、病死率分别为83.33%，（12.0±2.3） h，25.00%，8.33%，对照组分别为87.5%，（12.0±7.6） h，29.17%，4.17% 。结论国产奥曲肽和进口奥曲肽治疗肝硬化EGVB患者疗效相似。     

国产奥曲肽治疗肝硬化食管胃底静脉曲张破裂出血的疗效观察

目的:观察国产奥曲肽治疗肝硬化食管胃底静脉曲张破裂出血的临床疗效。方法:218例患者随机分为治疗组(110例)和对照组(108例),分别给予国产奥曲肽和进口醋酸奥曲肽100μg缓慢静脉推注后以25μg·h-1的速度静脉微量泵持续泵入。结果:治疗组显效率为50.90%,有效率为32.72%,总有效率为83.62%;对照组显效率为50.00%,有效率为34.26%,总有效率为84.26%。2组有效率比较无显著性差异(P>0.05)。结论:国产奥曲肽在治疗肝硬化食管胃底静脉曲张破裂出血方面可达到进口奥曲肽水平。     

醋酸奥曲肽与奥曲肽治疗食管静脉曲张破裂出血的疗效比较

目的: 观察醋酸奥曲肽治疗食管静脉曲张破裂出血的疗效.方法: 90例食管静脉曲张破裂出血患者分为两组,治疗组60例用醋酸奥曲肽治疗,对照组30例用奥曲肽治疗,观察并比较两组的疗效、止血时间、输血量.结果: 治疗组总有效率为95%,对照组总有效率为90.0%.两组间无统计学差异(P>0.05).两组止血成功患者在24,48 h的输血量分别为:治疗组(314.3±129.5) ml,(445.2±312.9)ml;对照组(460.0±250.3)ml,(661.5±386.3)ml,两组比较在统计学上有明显差异(P<0.05).结论: 醋酸奥曲肽的临床疗效优于奥曲肽,醋酸奥曲肽能有效、安全地治疗食管静脉曲张破裂出血.     

国产醋酸奥曲肽治疗食管胃底静脉曲张破裂出血31例临床观察

目的评价国产醋酸奥曲肽治疗肝硬化食管胃底静脉曲张破裂出血的临床疗效。方法64例食管胃底静脉曲张破裂出血患者随机分成两组,治疗组首次静脉推注国产醋酸奥曲肽0.1 mg,继以0.05 mg/h连续静脉滴注72～96 h对照组给予垂体后叶素0.2～0.4u/min持续静脉滴注72～96h,高龄或伴有冠心病患者联合应用硝酸甘油0.8 mg/h,观察2组的止血率及不良反应。结果治疗组止血率为93.8%,不良反应率为9.7%,对照组止血率为53.6%,不良反应率为42.2%,两组止血率及不良反应率差异有统计学意义(P<0.01)。结论国产醋酸奥曲肽治疗食管胃底静脉曲张破裂出血的疗效明显高于垂体后叶素,且不良反应少,有很高的临床价值。     

醋酸奥曲肽联合奥美拉唑钠治疗上消化道出血的疗效评价

目的探讨醋酸奥曲肽联合奥美拉唑钠治疗上消化道出血的临床疗效。方法40例上消化道出血患者,分为观察组和对照组。对照组给予奥美拉唑钠,观察组给予奥美拉唑钠联合醋酸奥曲肽。结果观察组显效率为90．00％,高于对照组的显效率60．00％,差异有统计学意义（P〈0．05）。结论奥美拉唑钠联合醋酸奥曲肽治疗上消化道出血疗效可靠。     

不同剂量醋酸奥曲肽治疗肝硬化食管胃静脉曲张破裂出血的临床观察

目的:观察不同剂量醋酸奥曲肽治疗肝硬化食管胃静脉曲张破裂出血的临床疗效和安全性。方法:46例肝硬化食管胃静脉曲张破裂出血患者按随机数字表法均分为观察组和对照组。两组患者均给予常规治疗后,对照组患者给予醋酸奥曲肽0.1mg缓慢静脉推注,再给予醋酸奥曲肽0.3 mg加入5%葡萄糖注射液500 ml中以25μg/h的速度连续静脉滴注,bid;观察组患者给予醋酸奥曲肽0.2 mg缓慢静脉推注,再给予醋酸奥曲肽0.6 mg加入5%葡萄糖注射液500 ml中以50μg/h的速度连续静脉滴注,bid。两组患者疗程均为5 d。观察两组患者的临床疗效,治疗前后门静脉内径(PVD)、门静脉平均流速(PVV),记录需要接受输血的例数、平均输血量、病死率及不良发生情况。结果:观察组患者总有效率显著高于对照组患者,观察组患者接受输血例数和平均输血量均显著低于对照组患者,两组比较差异均有统计学意义(P<0.05);治疗后两组患者PVD均显著低于同组治疗前,PVV均显著高于同组治疗前,差异有统计学意义(P<0.05),但两组间比较差异无统计学意义(P>0.05);两组患者病死率及不良反应发生率比较差异均无统计学意义(P>0.05)。结论:不同剂量醋酸奥曲肽治疗肝硬化食管胃静脉曲张破裂出血均有显著疗效,但高剂量组疗效更好,且安全性相当。     

醋酸生长抑素与醋酸奥曲肽治疗食管-胃底静脉曲张破裂出血的成本-效果分析

目的:评价醋酸生长抑素与醋酸奥曲肽治疗食管-胃底静脉曲张破裂出血的成本-效果。方法:采用回顾性调查方法,对醋酸生长抑素与醋酸奥曲肽治疗61例食管-胃底静脉曲张破裂出血的患者进行成本-效果分析。结果:醋酸生长抑素组与醋酸奥曲肽组的总成本分别为11141.00、9325.30元,总有效率分别为83.87%、86.67%(P>0.05),成本-效果比分别为13283.65、10759.55。结论:相对于醋酸生长抑素,醋酸奥曲肽无论从有效率还是药物经济学角度分析都占优势。     

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.

     

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.     

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.