盐酸羟考酮缓释片联合复方苦参注射液治疗肺癌疼痛的疗效观察

目的观察盐酸羟考酮缓释片联合复方苦参注射液治疗肺癌疼痛患者的临床疗效。方法将54例肺癌疼痛患者随机分为治疗组与对照组各27例,治疗组给予盐酸羟考酮缓释片联合复方苦参注射液,对照组仅单用盐酸羟考酮缓释片。结果治疗组总有效率为92.6%明显高于对照组的77.8%,2组比较差异有统计学意义（P〈0.05）。结论盐酸羟考酮缓释片联合复方苦参注射液对缓解肺癌患者疼痛优于单用盐酸羟考酮缓释片。     

复方苦参注射液联合羟考酮缓释片治疗中晚期癌痛的疗效观察

目的观察复方苦参注射液联合羟考酮缓释片治疗中晚期癌痛的临床疗效。方法将60例中重度癌痛患者随机分为治疗组和对照组各30例。治疗组予复方苦参注射液联合羟考酮缓释片治疗,对照组仅予羟考酮缓释片治疗。观察2组镇痛效果、生活质量评分及不良反应情况。结果治疗组疼痛缓解率为90．0％高于对照组的66．7％,差异有统计学意义（P〈0．05）。治疗后,2组生活质量评分均高于治疗前,且治疗组高于对照组,差异均有统计学意义（P〈0．05）。治疗组不良反应发生率低于对照组,差异有统计学意义（P〈0．05）。结论复方苦参注射液联合羟考酮缓释片能有效缓解中重度癌痛,明显改善患者的生活质量,不良反应较单用羟考酮缓释片明显减少,值得临床推广应用。     

复方苦参注射液治疗骨转移癌性疼痛的临床效果研究

目的分析探讨复方苦参注射液治疗骨转移癌性疼痛(癌痛)的临床效果。方法80例骨转移癌性疼痛患者,随机分为观察组与对照组,各40例。对照组给予硫酸吗啡缓释片治疗,观察组给予硫酸吗啡缓释片联合复方苦参注射液治疗。对比两组治疗前后各项评分、临床疗效。结果治疗后,观察组疼痛数字分级量表(NRS)评分(1.87±0.42)分低于对照组的(3.67±0.34)分,生活质量量表(QOL)评分(41.20±4.16)分、卡氏评分(KPS)评分(86.21±3.15)分高于对照组的(38.15±3.50)、(73.58±4.26)分,差异有统计学意义(t=21.067、3.548、15.077,P<0.05)。观察组治疗总有效率为90.00%,高于对照组的70.00%,差异有统计学意义(P<0.05)。结论复方苦参注射液治疗骨转移癌性疼痛,效果显著,可有效减轻癌痛,改善患者生活质量与健康状况。     

西黄胶囊联合盐酸吗啡缓释片治疗中晚期肺癌疼痛临床观察

目的观察西黄胶囊联合盐酸吗啡缓释片治疗中晚期肺癌疼痛的效果。方法 97例中晚期肺癌患者随机分为治疗组和对照组,治疗组给予盐酸吗啡缓释片和西黄胶囊;对照组给予盐酸吗啡缓释片,治疗2周后评价疗效,观察患者疼痛改善及生活质量提高情况。结果治疗组疼痛明显改善,生活质量明显提高。结论西黄胶囊联合盐酸吗啡缓释片治疗癌痛,能显著改善症状,提高生活质量。     

复方苦参注射液辅助治疗恶性肿瘤晚期疼痛的临床效果观察

目的探讨复方苦参注射液辅助治疗恶性肿瘤晚期疼痛的临床效果。方法选择2007年5月～2011年6月在我院治疗的88例恶性肿瘤患者,随机分为观察组和对照组,每组44例,两组患者均进行常规治疗,观察组患者在常规治疗的基础上给予复方苦参注射液辅助治疗,评价两组患者治疗后的疼痛评分及疼痛缓解的有效率、生活质量评分及不良反应情况。结果治疗后,两组患者的疼痛评分均降低,且观察组患者低于对照组,两组间差异具有统计学意义护〈0．05）;观察组和对照组患者疼痛缓解的有效率分别为95．5％（42／44）和81．8％（36／44）,观察组患者疼痛缓解的有效率显著高于对照组,差异具有统计学意义沪〈0．05）;观察组患者的生活质量评分高于对照组（P〈0．05）,而不良反应发生率显著低于对照组,差异具有统计学意义（P〈0．05）。结论复方苦参注射液辅助治疗可有效缓解恶性肿瘤患者的晚期疼痛,值得临床深入研究。     

盐酸吗啡缓释片与硫酸吗啡缓释片对控制癌性疼痛的临床对比研究

目的：探讨盐酸吗啡缓释片与硫酸吗啡缓释片控制癌性疼痛效果。方法癌症患者146例随机分为两组,口服硫酸吗啡缓释片患者73例为对照组,口服盐酸吗啡缓释片患者73例为观察组,比较癌性疼痛缓解情况及不良反应情况。结果观察组治疗后癌性疼痛状况明显好于对照组（P ＜0.05）。观察组癌性疼痛缓解率高于对照组,观察组恶心呕吐、头痛头晕、嗜睡、便秘、排尿困难的发生率均低于对照组（P＞0.05）。结论盐酸吗啡缓释片控制癌性疼痛的效果更好,并发症少且安全性高。     

吗啡缓释片加20%甘露醇注射液与20%甘露醇注射液在晚期癌症疼痛的应用比较

目的观察吗啡缓释片联合20%甘露醇注射液在晚期癌症疼痛中的应用效果。方法选取我院自2012年2月至2012年12月收治的117例晚期癌症疼痛患者作为研究对象,按照随机数字表法随机分为观察组60例与对照组57例,分别给予吗啡缓释片＋20%甘露醇注射液和单纯20%甘露醇注射液治疗,治疗3个周期后比较两组患者的止痛效果和生活质量水平改善情况。结果①观察组CR＋PR率为85.0%,对照组CR＋PR率为70.2%,两组CR＋PR率比较有统计学差异（P〈0.05）。②两组患者生活质量各项指标均较治疗前有改善（P〈0.05）,观察组身体功能、情绪功能、社会功能及总体健康状况较对照组改善明显（P〈0.05）,具有统计学意义。结论吗啡缓释片联合20%甘露醇注射液可显著降低晚期癌症疼痛程度,且对改善患者生活质量水平具有重要价值。     

复方苦参注射液联合硫酸吗啡控释片治疗晚期癌痛的临床观察

目的:观察复方苦参注射液联合硫酸吗啡控释片治疗晚期癌性疼痛的临床疗效。方法:按入院先后顺序将104例患者随机分为治疗组和对照组,治疗组给予复方苦参注射液联合硫酸吗啡控释片治疗,对照组给予单纯硫酸吗啡控释片治疗。结果:治疗组显效率为80.8%,对照组显效率为65.4%,2组比较有显著性差异(P<0.01);治疗组治疗后体力状况提高率为40.4%,对照组为25.0%,2组比较有统计学意义(P<0.05)。结论:复方苦参注射液联合硫酸吗啡控释片治疗晚期癌痛效果明显优于单纯硫酸吗啡控释片,同时可以提高患者的生活质量。     

芬太尼透皮贴剂和盐酸吗啡缓释片治疗中重度癌痛的疗效比较

目的：探讨分析芬太尼透皮贴剂和盐酸吗啡缓释片治疗中重度癌痛的疗效比较。方法选取本院近年来收治的中重度癌痛患者70例,并随机将其分成观察组（35例）和对照组（35例）,给予观察组患者芬太尼贴剂,给予对照组患者盐酸吗啡缓释片,两组均以服药10 d为一个疗程,比较两组疼痛控制情况和疗效。结果观察组患者在不良反应如恶心呕吐、眩晕、便秘等方面发生率低于对照组,然而观察组患者瘙痒发生率要高于对照组,经对比,两组差异具有明显统计学意义（P〈0.05）;两组患者疼痛缓解程度和缓解率比较差异均不明显（P〉0.05）。结论在治疗中重度癌痛中采用芬太尼透皮贴剂能够达到和盐酸吗啡缓释片相似的镇痛效果,且不良反应发生率低于盐酸吗啡缓释片,是较为理想的阿片类药物,值得在临床推广和应用。     

复方苦参注射液治疗晚期肝癌的临床观察

目的：观察复方苦参注射液治疗晚期肝癌的临床疗效。方法：选择48例晚期肝癌患者（均无手术、放疗、化疗指征）分为治疗组（24例，给予一般治疗＋复方苦参注射液静滴治疗）和对照组（24例，给予一般治疗）。结果：治疗组（生活质量改善率为41．6％，疼痛缓解率为71％）的临床疗效明显优于对照组。结论：复方苦参注射液治疗晚期肝癌安全、有效，能有效地改善晚期肝癌患者的症状，提高生活质量。     

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.