非诺贝特与阿托伐他汀治疗高脂血症及高尿酸血症的效果比较

目的观察微粒化非诺贝特与阿托伐他汀对高脂血症合并高尿酸血症的治疗效果。方法55例高血脂症合并高尿酸血症患者随机分为两组。治疗组30例给予微粒化非诺贝特200mg／d;对照组25例给予阿托伐他汀10mg／d。两组患者均给治疗8周。比较两组临床疗效、血脂和血尿酸水平及不良反应。结果两组治疗后与治疗前比较,甘油三酯（TG）、总胆固醇（TC）差异均有统计学意义。治疗后治疗组与对照组TG差异有统计学意义。治疗组降低血尿酸效果好于对照组。两组均无严重不良反应。结论非诺贝特与阿托伐他汀均可用于高血酸症及高脂血症治疗,短时间内使血脂达标,减少脑血管病的危险因素。     

阿托伐他汀对老年Ⅱ型糖尿病高脂血症的疗效观察

目的:比较他汀类药物阿托伐他汀与贝特类药物非诺贝特治疗老年Ⅱ型糖尿病血脂紊乱的疗效.方法:122例老年Ⅱ型糖尿病高脂血症患者随机分为两组,治疗组(阿托伐他汀组)62例,男44例,女18例,对照组(非诺贝特组)60例,男43例,女17例.治疗组口服阿托伐他汀10 mg, 每晚一次(qn);对照组口服非诺贝特100 mg,每日3次,疗程8周,观察降脂疗效及不良反应.结果:阿托伐他汀降三酰甘油(TG)、总胆固醇 (TC)和低密度脂蛋白(LDL-C)优于非诺贝特(P<0.05);升高高密度脂蛋白(HDL-C)效果相似(P>0.05).结论:阿托伐他汀对老年Ⅱ型糖尿病血脂紊乱的疗效优于非诺贝特.     

阿托伐他汀与非诺贝特治疗高脂血症的比较

目的:比较阿托伐他汀与非诺贝特治疗高脂血症的疗效及安全性.方法:高脂血症86例,随机分为阿托伐他汀组43例,给阿托伐他汀10 mg,qd,共8周;非诺贝特组43例,给非诺贝特200 mg,qd,共8周.结果:两组治疗4周,胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-ch)均开始显著下降(P<0.01), 治疗8周高密度脂蛋白胆固醇(HDL-ch) 开始显著上升(P<0.05); 阿托伐他汀组治疗8周TC下降较非诺贝特组明显(P<0.05);不良反应发生率阿托伐他汀组9.3%,非诺贝特组4.7%,差异有极显著性(P<0.01).结论:两药均有明显的调脂作用,阿托伐他汀治疗8周TC下降明显优于非诺贝特,非诺贝特的不良反应发生率较低.     

阿托伐他汀联合非诺贝特治疗缺血性脑卒中的疗效及对患者血脂、高敏C反应蛋白水平的影响

目的:探讨阿托伐他汀联合非诺贝特防治缺血性脑卒中的临床效果及对患者治疗前后血脂、高敏C反应蛋白(hs-CRP)的影响。方法:64例缺血性脑卒中患者随机分为观察组与对照组各32例。两组患者均给予常规对症治疗,同时对照组给予阿托伐他汀片20 mg,po qn;观察组在对照组基础上再加用非诺贝特胶囊0.2 g,po qd。两组疗程均为3个月。比较两组患者治疗前后神经功能缺损评分、血脂和血清hs-CRP水平变化,及两组药品不良反应。随访1年,观察两组患者脑卒中复发情况。结果:治疗后两组CNDF评分均较治疗前显著降低(P<0.05),且观察组显著低于对照组(P<0.05)。治疗后观察组血脂、血清hs-CRP水平较治疗前明显改善(P<0.05),且均明显优于对照组(P<0.05);而对照组治疗前后血脂、血清hs-CRP水平差异无统计学意义(P>0.05)。两组不良反应发生率差异无统计学意义(P<0.05)。对照组复发率明显高于观察组(P<0.05)。结论:阿托伐他汀联合非诺贝特治疗缺血性脑卒中效果显著,可有效调节血脂、降低血清hs-CRP水平和不良脑血管事件的复发,值得临床推广使用。     

阿托伐他汀联合非诺贝特治疗急性冠脉综合征的疗效观察

目的探究阿托伐他汀联合非诺贝特治疗急性冠脉综合征的临床效果。方法选取笔者所在医院2009年6月～2011年6月间收治的急性冠脉综合征患者43例,将其随机分为两组,对照组患者21例给予阿托伐他汀治疗,观察组患者22例给予阿托伐他汀联合非诺贝特治疗,分析两组患者的临床用药情况。结果两组患者低密度脂蛋白、胆固醇、三酰甘油、高密度脂蛋白等指标与治疗前相比均有明显改善,而观察组患者用药效果明显优于对照组,差异有统计学意义(P<0.05)。结论阿托伐他汀与非诺贝特联合应用治疗急性冠脉综合征疗效显著,值得临床推广应用。     

辛伐他汀和微粒化非诺贝特对混合型高脂血症的疗效比较 (附56例分析)

目的比较辛伐他汀和微粒化非诺贝特对混合型高脂血症的疗效.方法56例混合型高脂血症患者随机分为两组,一组接受辛伐他汀(20mg qn,n=28)治疗,一组接受微粒化非诺贝特(200mg qd,n=28)治疗,疗程6周,观察治疗前后血脂成份的变化.结果两组治疗后均能明显降低总胆固醇(TC)、甘油三脂(TG)、低密度脂蛋白胆固醇(LDL-C),升高高密度脂蛋白胆固醇(HDL-C),但辛伐他汀降低TC、LDL-C、LDL-C/HDL-C的幅度比微粒化非诺贝特高(P＜0.05),而微粒化非诺贝特降低TG的幅度比辛伐他汀大(P＜0.05),辛伐他汀治疗后TC、LDL-C恢复至正常水平的百分比显著比微粒化非诺贝特高(P＜0.05),而TG降至正常水平的百分比,微粒化非诺贝特比辛伐他汀高(P＜0.05).结论本研究提示对于甘油三脂轻至中度升高的混合型高脂血症患者,他汀类调脂药为首选药物;而对于严重的高甘油三脂血症者,非诺贝特则是合适的选择.大剂量辛伐他汀(20mg)与微粒化非诺贝特(200mg)均有报告认为能全面调脂[1],但两种药作用机制不同,调脂侧重点不同,如何选择是临床医生面临的困境.本研究旨在比较大剂量辛伐他汀及微粒化非诺贝特对混合型高脂血症的疗效,指导临床用药.     

非诺贝特对高TG的2型糖尿病患者PCI术后的影响

目的通过前瞻性随机对比研究,观察非诺贝特联合阿托伐他汀对高TG的2型糖尿病患者药物洗脱支架置入术后的临床疗效。方法入选符合本研究标准的522例药物洗脱支架置入术后高TG的2型糖尿病患者,随机分为两组,联合治疗组249例,非诺贝特200mg晨日一次口服,阿托伐他汀20mg晚日一次口服;阿托伐他汀组273例,20mg晚日一次口服。疗程12个月。比较两组主要不良心血管事件发生情况、降脂疗效及安全性。结果非诺贝特联合阿托伐他汀组主要不良心血管事件发生率及血清TG明显低于阿托伐他汀组(P<0.05),而HDL-C明显高于阿托伐他汀组(P<0.05)。不良反应发生率相似。结论非诺贝特联合阿托伐他汀明显改善高TG的2型糖尿病患者药物洗脱支架置入术后的预后,两药联合安全有效。     

阿托伐他汀联合依折麦布对冠心病高脂血症患者血脂的影响

目的探讨阿托伐他汀联合依折麦布治疗冠心病高脂血症疗效。方法 136例冠心病高脂血症患者分为阿托伐他汀联合依折麦布治疗组及单用阿托伐他汀对照组,比较两组患者治疗前后的血脂变化、血脂达标率及不良反应。结果治疗后两组患者的总胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-C)均明显降低(P0.05),尤其治疗组明显优于对照组,TC、LDL-C、TG达标率明显高于对照组(P0.01),HDL-C虽有上升但差异无统计学意义(P0.05)。不良反应少。结论阿托伐他汀联合依折麦布对冠心病高脂血症患者有较好的降脂作用,能提高降脂达标率。     

阿托伐他汀联合非诺贝特治疗混合型高脂血症52例

目的探讨阿托伐他汀联合非诺贝特治疗混合型高脂血症的临床疗效及其安全性。方法将104例混合型高脂血症患者随机分为观察组和对照组各52例,观察组采用阿托伐他汀联合非诺贝特治疗,对照组采用阿托伐他汀治疗,比较两组的临床效果及不良反应。结果观察组总有效率86.54%(45/52),对照组总有效率69.23%(36/52),两组比较有显著性差异(P<0.05);两组患者的TC、TG、LDL-C及HDL-C的水平与治疗前比较均有显著性差异(P<0.05),组间比较均有显著性差异(P<0.05)。结论阿托伐他汀联合非诺贝特治疗混合型高脂血症具有协同作用,能有效提高调脂效果,且安全性高,值得临床推广。     

阿托伐他汀联合非诺贝特治疗混合型高脂血症的Meta分析

目的系统评价阿托伐他汀联合非诺贝特治疗混合型高脂血症的疗效与安全性。方法计算机检索Cochrane、Pub Med、CBM、万方、CNKI及维普全文电子期刊数据库中随机对照试验。结果共纳入15项随机对照试验,1980例患者。联合治疗组对总胆固醇(TC)、三酰甘油(TG)和高密度脂蛋白胆固醇(HDL-C)的疗效优于单药治疗组;与单药治疗组相比,未增加药物不良反应(ADR);剂量分组分析结果显示,联合治疗组用常规剂量与低剂量的阿托伐他汀联合非诺贝特治疗,安全性均良好[SMD=1.13,95%CI(0.57,2.24),P>0.05;SMD=1.50,95%CI(0.94,2.39),P>0.05]。阿托伐他汀与非诺贝特联合治疗组对TC、TG和HDL-C的疗效优于单药治疗[SMD=-11.10,95%CI(-18.44,3.77),P<0.05;SMD=-1.20,95%CI(-1.28,1.12),P<0.05;SMD=0.694,95%CI(0.587,0.801),P<0.05]。结论低剂量与常规剂量阿托伐他汀联合非诺贝特治疗混合型高脂血症安全性和有效性均良好。     

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.

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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.     

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.