左旋布比卡因、舒芬太尼及地塞米松联合在硬膜外术后镇痛中的应用

目的研究左旋布比卡因、舒芬太尼及地塞米松在病人自控硬膜外镇痛（PCEA）中的效应。方法择期行子宫切除术患者（ASAⅠ-Ⅱ）40例,按术后硬膜外用药的不同随机分为两组,每组20例。Ⅰ组（研究组）术后硬膜外药物配方为左旋布比卡因200mg＋舒芬太尼50μg＋地塞米松10mg,用生理盐水稀释成100mL。Ⅱ组（对照组）术后硬膜外配方为左旋布比卡因200mg＋舒芬太尼50μg,用生理盐水稀释成100mL。采用视觉模拟评分（VAS）记录两组患者术后的镇痛效果,同时记录不良反应恶心呕吐及瘙痒等症状的发生率并测定0.2%左旋布比卡因溶液、舒芬太尼溶液、地塞米松溶液和3种药物配伍后混合溶液的粘度。结果Ⅰ组患者术后无痛状态的持续时间显著超过Ⅱ组,镇痛效果显著强于Ⅱ组,所有病例术后均未发生瘙痒,呼吸与循环功能平稳。舒芬太尼溶液和0.2%左旋布比卡因溶液的粘度显著小于地塞米松溶液和此三种药物配伍后混合液的粘度。结论舒芬太尼、左旋布比卡因和地塞米松配伍硬膜外应用可以获得良好和持久的术后镇痛效果。     

舒芬太尼复合罗哌卡因在小儿骶管阻滞中的应用

目的探讨小剂量舒芬太尼复合罗哌卡因在小儿骶管阻滞中的临床疗效及安全性。方法选择60例ASAⅠ级、年龄1～4岁、无心肺疾患、择期行下腹部手术的患儿,随机均分为实验组和对照组。实验组骶管单次注入0.2%罗哌卡因+舒芬太尼0.5μg/mL,对照组骶管单次注入0.2%罗哌卡因,术中用异丙酚和氯胺酮维持镇静。测定骶管阻滞起效的时间和术后镇痛情况,监测并记录两组患儿围术期的呼吸、循环功能状况,评估麻醉效能,观察围术期不良反应。结果与对照组比较,实验组的感觉阻滞起效时间较短,镇痛时间明显延长,围术期循环功能稳定,阻滞效果可靠,两组不良反应差异无统计学意义。结论小儿下腹部手术经骶管单次注入舒芬太尼复合罗哌卡因的麻醉效果优于单纯应用罗哌卡因,术后镇痛时间长,不良反应少。     

舒芬太尼和左旋布比卡因用于下腹部外科术后自控镇痛的效果研究

目的比较舒芬太尼和左旋布比卡因配伍以及哌替啶和异丙嗪配伍术后镇痛的效果。方法100例手术患者分成两组，Ⅰ组（50例）舒芬太尼100μg＋0．125％左旋布比卡因100ml利用微量泵进行术后自控镇痛（PCA）2ml／h，患者疼痛时可自行或由家属控制给药2ml；Ⅱ组（50例）哌替啶50mg和异丙嗪25mg配伍肌内注射进行术后镇痛，疼痛时即肌内注射1次，下次肌内注射用药时间一般不少于6h。结果使用舒芬太尼和左旋布比卡因配伍进行术后自控镇痛以及使用哌替啶和异丙嗪配伍肌内注射术后镇痛，两种方法镇痛效果差异有显著统计学意义。相比之下，前者具有操作简单、见效快、镇痛效果稳定可控、无成瘾性等优点。结论舒芬太尼和左旋布比卡因配伍术后自控镇痛法优于哌替啶和异丙嗪配伍术后肌内注射镇痛。     

舒芬太尼用于剖宫产术后硬膜外自控镇痛的临床观察

目的以芬太尼为对照,比较不同剂量舒芬太尼复合布比卡因用于剖宫产手术后硬膜外自控镇痛的临床效果和安全性。方法 200例择期剖宫产术后患者,随机双盲分为4组,每组50例,术后硬膜外镇痛分别使用舒芬太尼0.25μg/mL(Ⅰ组)、0.5μg/mL(Ⅱ组)、0.75μg/mL(Ⅲ组)及芬太尼5μg/mL(Ⅳ组)。记录术后第4、8、12、24、48h的镇痛效果、镇静程度,各组可能出现的皮肤瘙痒、恶心呕吐等不良反应。结果与Ⅰ组对应值比较,Ⅱ、Ⅲ组VAS、VAFS评分降低,差异有显著性(P<0.05或P<0.01);与Ⅱ组对应值比较,Ⅲ组VAS、VAFS评分降低,差异有显著性(P<0.05)。各时点Ramsay镇静评分:I组术后8~24h评分低于其他各组对应值,差异有显著性(P<0.05)。结论舒芬太尼复合低浓度布比卡因用于剖宫产术后硬膜外自控镇痛临床效果好,副作用小,舒芬太尼推荐浓度以0.75μg/mL为宜。     

不同剂量舒芬太尼复合左旋布比卡因用于股骨骨折患者手术后自控镇痛的比较

目的比较不同剂量舒芬太尼复合左旋布比卡因用于股骨骨折手术后自控镇痛的效应及其安全性。方法选择择期股骨手术患者90例,术后随机分为A、B、C三组,每组30例,均行硬膜外自控镇痛。A组:舒芬太尼0.75μg/m L+0.125%左旋布比卡因;B组:舒芬太尼1.0μg/m L+0.125%左旋布比卡因;C组:舒芬太尼1.25μg/m L+0.125%左旋布比卡因;每组均用0.9%氯化钠注射液稀释至100 m L。分别记录三组患者:术后4、8、12、24、36、48 h疼痛视觉模拟评分(VAS评分);术后8 h改良Bromage分级;术后不良反应发生例数;不良反应发生率及患者满意率。结果 A组术后8、12、24、36、48 h的VAS评分明显高于B组和C组(P<0.05)。术后8 h改良Bromage分级组间比较差异无统计学意义(P>0.05)。C组术后不良反应发生率明显高于A组和B组(P<0.05);B组患者满意率明显高于A组和C组(P<0.05)。结论舒芬太尼1.0μg/m L是0.125%左旋布比卡因最佳配伍剂量,镇痛效果好、不良反应少、患者满意率高,是股骨骨折患者术后硬膜外镇痛的较佳选择。     

剖宫产术后不同浓度的舒芬太尼混合罗哌卡因硬膜外镇痛的效果

目的评价不同浓度舒芬太尼与罗哌卡因混合用于剖宫产术后硬膜外自控镇痛(PCEA)效果。方法选择90例剖宫产术患者进行术后镇痛,随机分为三组,术后镇痛药液的配方分别为甲组舒芬太尼0.6μg/mL、乙组舒芬太尼0.5μg/mL、丙组舒芬太尼0.4μg/mL。各组均加0.15%罗哌卡因及2mg托烷司琼加生理盐水至100mL。观察术后患者不同时点视觉模拟法(VAS)评分、Ramsay镇静评分及不良反应。结果 0.5μg/mL舒芬太尼组与其他两组比较差异有统计学意义,P<0.05。结论 0.5μg/mL舒芬太尼组用于剖宫产术后镇痛效果满意且不良反应发生率低。     

舒芬太尼用于剖宫产术后硬膜外自控镇痛的临床观察

目的 观察不同浓度舒芬太尼用于剖宫产术后硬膜外自控镇痛的临床效果.方法 ASAⅠ～Ⅱ级腰硬联合麻醉下行剖宫产患者60例,术后给予硬膜外自控镇痛,根据舒芬太尼浓度不同随机分为两组,每组30例.Ⅰ组:舒芬太尼0.5μg/ml+0.125％布比卡因,总量100ml;Ⅱ组:舒芬太尼0.75μg/ml+0.125％布比卡因,总量100ml.预充混合液5ml,背景输注量3ml/h,PCEA量2ml,锁定时间20min.分别记录术后镇痛效果(疼痛视觉模拟评分VAS)、镇静情况(Ramsay镇静评分)、下肢运动情况(改良Bromage分级)及不良反应.结果 Ⅱ组VAS评分明显低于Ⅰ组(P＜0.05),有统计学意义.两组Ramsay镇静评分、下肢运动情况及不良反应无显著差异(P＞0.05).结论 舒芬太尼0.75μg/ml复合0.125％布比卡因适用于产科术后镇痛,镇痛效果满意,副作用少,值得推广.     

小剂量舒芬太尼复合罗哌卡因用于小儿术后镇痛的临床观察

目的：评价小剂量舒芬太尼复合罗哌卡因用于小儿术后镇痛的效果、运动阻滞情况及其不良反应。方法选择ASAI-Ⅱ级择期腹部以下手术的患儿60例，在蛛网膜下腔-硬膜外下进行手术，随机分成两组﹕A组为0.125%罗哌卡因100ml，B组为0.1%罗哌卡因100ml加入舒芬太尼20μg。均用生理盐水配成100ml，以3ml/h的速率硬膜外持续注入，观察术后24h内镇痛效果及术后患儿恶心、呕吐、下肢麻木、头疼、皮肤瘙痒、尿潴留等不良反应。结果术后镇痛效果B组优良率高于A组。恶心、呕吐、下肢麻木、头疼、皮肤瘙痒、尿潴留发生率两组间无明显差异。 B组的运动阻滞较A组恢复快（P〈0.05）。结论小剂量舒芬太尼复合罗哌卡因用于小儿术后镇痛可提供较好的镇痛效果且不良反应少。     

氟比洛芬酯复合不同剂量舒芬太尼在骨科术后静脉镇痛的应用

目的观察氟比洛芬酯复合不同剂量的舒芬太尼在骨科术后静脉镇痛的应用方法 ASAI-Ⅱ择期骨科手术病人100例,随机分为3组:I,舒芬太尼150μg+生理盐水共100 mL(舒芬太尼1.5μg·mL-1);Ⅱ,舒芬太尼100μg+氟比洛芬酯100 mg+生理盐水共100 mL(舒芬太尼1μg·mL-1+氟比洛芬酯1 mg·mL-1);Ⅲ,舒芬太尼150μg+氟比洛芬酯100 mg+生理盐水共100 mL(舒芬太尼1.5μg·mL-1+氟比洛芬酯1 mg·mL-1)。观察并记录术后2、4、12、24 h的镇痛、镇静和不良反应。结果Ⅱ和Ⅲ组在术后4、12、24 h疼痛评分和24 h内的PCA按压次数明显低于I组(P<0.05)。Ⅰ和Ⅲ组恶心的发生率明显高于Ⅱ组(P<0.05)。Ⅰ和Ⅲ组在2、4、12 h镇静评分明显高于II组(P<0.05)。结论舒芬太尼1μg·mL-1+氟比洛芬酯1 mg·mL-1可为骨科术后提供良好的镇痛效果,不良反应少,提高镇痛质量。     

舒芬太尼与左旋布比卡因在断指再植术后镇痛中的应用

目的观察舒芬太尼、左旋布比卡因复合连续臂丛神经阻滞再植的血运情况与术后镇痛的效果及不良反应。方法上肢前臂手术患者60例,采用20G号D-Y套管针行肌间沟或腋路法连续臂丛神经阻滞,术中3h后或术毕接自控镇痛泵,将患者随机平均分成S、R两组。S组为舒芬太尼0.05μg/kg+0.225%左旋布比卡因+0.9%生理盐水,配100mL镇痛泵。R组为0.225%左旋布比卡因+0.9%生理盐水配100mL镇痛泵,两组背景剂量4mL/h,自控药量每次4mL,锁定时间40min,观察术后血运及镇痛效果。记录镇痛泵情况及患者有无不良反应。结果 S组在术后6、12、24、36、48h的患肢(指)的血运及镇痛效果明显优于R组(P<0.05)。结论 S组明显优于R组,是一种安全、有效、确切的方法。     

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.     

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.     

Nachweis einiger Heilmittel in der Kniegelenksynovialflüssigkeit

Zusammenfassung Mittels Gaschromatographie und Dünschichtchromatographie wiesen die Autoren 11 Substanzen nach, welche durch Injektion oder nach Verabreichung per os in die Kniegelenksynovialflüssigkeit eindrangen. In ihrer Aufstellung konnten sie eine direkte Beziehung zwischen Struktur sowie chemischphysikalischen Eigenschaften der Substanz und ihrer Fähigkeit, aus dem Blut in die Kniegelenksynovialflüssigkeit einzudringen, nicht nachweisen, außer der Tatsache, daß Substanzen mit starker Affinität zu Eiweißstoffen erst in höheren Dosen nachweisbar waren.     

Biochemical and molecular characterisation of cubozoan protein toxins

Class Cubozoa includes several species of box jellyfish that are harmful to humans. The venoms of box jellyfish are stored and discharged by nematocysts and contain a variety of bioactive proteins that are cytolytic, cytotoxic, inflammatory or lethal. Although cubozoan venoms generally share similar biological activities, the diverse range and severity of effects caused by different species indicate that their venoms vary in protein composition, activity and potency. To date, few individual venom proteins have been thoroughly characterised, however, accumulating evidence suggests that cubozoan jellyfish produce at least one group of homologous bioactive proteins that are labile, basic, haemolytic and similar in molecular mass (42-46 kDa). The novel box jellyfish toxins are also potentially lethal and the cause of cutaneous pain, inflammation and necrosis, similar to that observed in envenomed humans. Secondary structure analysis and remote protein homology predictions suggest that the box jellyfish toxins may act as α-pore-forming toxins. However, more research is required to elucidate their structures and investigate their mechanism(s) of action. The biological, biochemical and molecular characteristics of cubozoan venoms and their bioactive protein components are reviewed, with particular focus on cubozoan cytolysins and the newly emerging family of box jellyfish toxins.     

Dose tolerability of chronically inhaled voriconazole solution in rodents

Invasive pulmonary aspergillosis (IPA) is a fungal disease of the lung associated with high mortality rates in immunosuppressed patients despite treatment. Targeted drug delivery of aqueous voriconazole solutions has been shown in previous studies to produce high tissue and plasma drug concentrations as well as improved survival in a murine model of IPA. In the present study, rats were exposed to 20 min nebulizations of normal saline (control group) or aerosolized aqueous solutions of voriconazole at 15.625 mg (low dose group) or 31.25 mg (high dose group). Peak voriconazole concentrations in rat lung tissue and plasma after 3 days of twice daily dosing in the high dose group were 0.85 ± 0.63 μg/g wet lung weight and 0.58 ± 0.30 μg/mL, with low dose group lung and plasma concentrations of 0.38 ± 0.01 μg/g wet lung weight and 0.09 ± 0.06 μg/mL, respectively. Trough plasma concentrations were low but demonstrated some drug accumulation over 21 days of inhaled voriconazole administered twice daily. Following multiple inhaled doses, statistically significant but clinically irrelevant abnormalities in laboratory values were observed. Histopathology also revealed an increase in the number of alveolar macrophages but without inflammation or ulceration of the airway, interstitial changes, or edema. Inhaled voriconazole was well tolerated in a rat model of drug inhalation.