右美托咪定用于心脏瓣膜置换手术后重症监护患者镇静效果观察

目的探讨右美托咪定对心脏瓣膜置换手术后重症监护患者的镇静效果及安全性。方法选择80例心脏瓣膜置换术后入住ICU患者,分为对照组和实验组,分别采用咪达唑仑和右美托咪定进行镇静。监测两组患者镇静前后HR、RR、MAP、SpO2、VAS评分、Ramsay评分、达到镇静所需时间、停药后苏醒时间、芬太尼用量及不良反应发生率。结果镇静后,实验组的HR、MAP明显低于对照组(P<0.05),SpO2明显高于对照组(P<0.05),但RR比较差异无统计学意义(P>0.05)。镇静后,两组患者VAS评分、Ramsay评分比较差异有统计学意义(P<0.05)。实验组患者达到镇静所需时间、停药后苏醒时间均明显低于对照组(P<0.05),实验组芬太尼用量明显少于对照组(P<0.05)。实验组患者呕吐、谵妄发生率明显低于对照组(P<0.05),实验组患者心动过缓、低血压发生率明显高于对照组(P<0.05)。结论右美托咪定对心脏瓣膜置换手术后重症监护患者有镇静作用,呕吐、谵妄发生率低。     

右美托咪定和咪达唑仑复合芬太尼对ICU术后机械通气患者镇静的影响

目的观察右美托咪定和咪达唑仑复合芬太尼用于ICU术后机械通气患者的镇静效果及安全性。方法选取150例ICU术后机械通气患者,采用信封法随机分为右美托咪定组和咪达唑仑组,每组75例,两组患者均给予芬太尼持续泵入。右美托咪定组采用右美托咪定0.2～0.6μg/(kg·h)持续泵入。咪达唑仑组采用0.08～0.10 mg/(kg·h)咪达唑仑持续泵入。采用Ramsay分级标准对两组患者镇静效果进行分级评分,观察两组患者的镇静效果。详细记录两组患者芬太尼用量、达到理想镇静所需的时间、停药后苏醒时间、镇静期间呼吸及循环系统功能的变化及其他不反应发生情况。结果右美托咪定组镇静满意率为97.33%,咪达唑仑组镇静满意率为96.00%,两组镇静满意率比较差异无统计学意义(P>0.05)。右美托咪定组芬太尼用量明显低于咪达唑仑组(P<0.05),达到理想镇静所需时间及停药后苏醒时间明显短于咪达唑仑组(P<0.05)。两组患者呼吸抑制、平均动脉压下降、SpO2下降及恶心发生率比较差异无统计学意义,但右美托咪定组谵妄发生率明显低于咪达唑仑组,两组比较差异有统计学意义(P<0.05)。结论右美托咪定复合芬太尼用于ICU术后机械通气患者的镇静治疗,镇静效果满意,可以达到理想镇静时间及易唤醒时间短,谵妄发生率低,可减少芬太尼用量,而且对患者呼吸及循环系统影响小,是一种较为理想的ICU镇静剂。     

右美托咪定镇静对ICU机械通气患者谵妄防控中的作用研究

目的探讨右美托咪定(DEX)镇静对重症监护室(ICU)机械通气患者谵妄的预防作用。方法将我院ICU收治的88例接受机械通气治疗的危重患者随机分为两组:A组(n=44)采用DEX镇静治疗,B组(n=44)采用咪达唑仑镇静治疗。比较两组镇静效果及谵妄发生情况。结果 A组的芬太尼用量显著低于B组(P<0.05),停药后苏醒时间、机械通气时间及住ICU时间均较B组明显缩短(P<0.05);镇静180 min内各时间点,两组Ramsay评分明显升高而MAP、HR明显降低(P<0.05),但两组比较差异无统计学意义(P>0.05);A组的谵妄发生率显著低于B组(11.36%vs 36.36%),且谵妄出现时间明显延迟且持续时间较B组明显缩短(P<0.05)。结论 DEX在ICU机械通气患者中具有较好的镇静效果,可降低谵妄发生率、延缓谵妄出现时间并缩短延续时间。     

右美托咪定复合依托咪酯乳剂在内镜逆行胰胆管造影中的麻醉效果

目的 观察右美托咪定复合依托咪酯乳剂在内镜逆行胰胆管造影(ERCP)中的麻醉效果.方法 选择行ERCP的患者60例,随机分为右美托咪定复合依托咪酯乳剂组(观察组)和依托咪酯乳剂组(对照组),每组30例.观察组静脉微量泵注右美托咪定,芬太尼、咪哒唑仑、依托咪酯乳剂诱导后连接微量泵,依托咪酯乳剂持续输注维持麻醉;对照组给予芬太尼、咪哒唑仑、依托咪酯乳剂诱导后连接微量泵,依托咪酯乳剂维持麻醉.两组均根据术中体动、呛咳情况调整输注速度及追加芬太尼.观察记录手术时间、清醒时间、依托咪酯乳剂及芬太尼总用量,不同时段心率(HR)、平均动脉压(MAP)、呼吸频率(RR)、血氧饱和度(SpO2)、镇静效果、不良反应发生率、内镜医师及患者满意度.结果 观察组依托咪酯乳剂及芬太尼总量少于对照组,差异有统计学意义(P<0.05);麻醉诱导完成后观察组不同时段HR均下降、MAP均轻度升高,对照组不同时段HR、MAP均升高,与T0比较差异均有统计学意义(P<0.05);观察组不同时段HR均低于对照组,MAP在T15、T20、T30时段均低于对照组,差异均有统计学意义(P<0.05);观察组镇静效果优于对照组(P<0.01);观察组体动、呛咳及肌阵挛发生率低于对照组,内镜医师满意度高于对照组(P<0.05).结论 右美托咪定复合依托咪酯乳剂用于ERCP麻醉,是一种安全有效、医患双方均满意的麻醉方法.     

两种不同镇静方法在ICU重症患者中的应用效果比较

目的：比较瑞芬太尼+咪达唑仑、异丙酚+咪达唑仑两种镇静方法在ICU重症患者中的应用效果。方法将2014年3~12月本院ICU收治的64例重症患者随机分为治疗组和对照组,治疗组应用瑞芬太尼+咪达唑仑,对照组应用丙泊酚+咪达唑仑。比较两组的Ramsay镇静评分、Ricker镇静-躁动评分,观察两组患者治疗前及治疗后0.5、6、12 h的心率（HR）、平均动脉压（MAP）、呼吸频率（RR）等循环呼吸指标的变化。结果两组患者治疗0.5、6、12 h后的Ramsay镇静评分、Ricker镇静-躁动评分比较,差异无统计学意义（P>0.05）。两组患者治疗前HR、MAP、RR比较,差异无统计学意义（P>0.05）;治疗后各时间点HR、RR比较差异无统计学意义（P>0.05）,MAP比较差异有统计学意义（P<0.05）。结论瑞芬太尼+咪达唑仑和丙泊酚+咪达唑仑的镇静效果相当,但瑞芬太尼+咪达唑仑对患者的MAP影响较小。     

右美托咪定和咪达唑仑复合芬太尼用于ICU术后机械通气患者的镇静效果及安全性

目的：比较右美托咪定和咪达唑仑复合芬太尼用于ICU术后机械通气患者的镇静效果及安全性。方法选取86例ICU术后机械通气患者随机分为右美托咪定组（n=43）和咪达唑仑组（n=43）,两组患者均常规给予芬太尼持续泵入,在此基础上,咪达唑仑组以咪达唑仑0.08~0.10μg／（ kg· h）持续泵入,右美托咪定组以0.2~0.6μg／（ kg· h）右美托咪定持续泵入,观察两组的镇静效果及不良反应发生情况。结果右美托咪定组的芬太尼用量明显低于咪达唑仑组,差异比较具有统计学意义（ P<0.05）;达到镇静效果时间短于咪达唑仑组,差异比较均有统计学意义（P<0.05）;停药后苏醒时间也短于咪达唑仑组,差异比较有统计学意义（P<0.05）;两组的低血压、呼吸抑制、心动过缓及低氧血症的发生率无显著性差异（P>0.05）,但右美托咪定组患者的谵妄发生率为2.3%,明显低于咪达唑仑组的18.6%,差异比较有统计学意义（P<0.05）。结论右美托咪定用于治疗ICU术后机械通气患者的镇静效果好,芬太尼用量低,且安全性高,值得在临床上推广应用。     

应用咪达唑仑治疗非心脏大手术患者苏醒期及术后谵妄的疗效分析

目的探讨咪达唑仑治疗非心脏大手术患者苏醒期及术后谵妄的效果。方法选取2014年3月至2015年6月在我院行手术治疗的103例患者,将患者随机分为对照组49例和观察组54例,对照组予以常规手术用药,观察组予以咪达唑仑治疗,比较2组患者苏醒期的躁动镇静、谵妄评分;比较2组患者苏醒期谵妄、术后第1~3天谵妄发生率。结果 2组患者的手术持续时间比较差异无统计学意义(P>0.05);但观察组患者的拔管时间及苏醒时间均明显低于对照组(P<0.05)。观察组患者的苏醒期谵妄发生率为5.56%,明显低于对照组的26.53%(P<0.05);观察组患者的术后谵妄发生率为3.70%,明显低于对照组的16.33%(P<0.05)。结论咪达唑仑能有效降低非心脏大手术患者的苏醒期谵妄、术后谵妄发生率。     

盐酸右美托咪定和咪达唑仑在ICU机械通气患者中的应用效果研究

目的探讨盐酸右美托咪定和咪达唑仑应用于ICU机械通气患者镇静的效果及护理。方法选择60例在ICU行机械通气的患者为观察对象,随机分为试验组和对照组,分别给予盐酸右美托咪定和咪达唑仑镇静,观察镇静后两组的Ramsay评分,心率、呼吸频率、血压、停药后唤醒时间,比较两组呼吸频率下降、心动过缓、低血压、谵妄发生率。结果试验组Ramsay评分在2～4分的多于对照组,停药后唤醒时间明显短于对照组,两组不良反应发生率试验组心动过缓发生率更高,但呼吸频率下降及谵妄发生率明显低于对照组,低血压发生率无统计学意义。结论右美托咪定和咪达唑仑在ICU机械通气中的镇静效果良好,综合护理可有效降低机械通气并发症。     

ICU患者应用右美托咪啶与咪达唑仑镇静后谵妄发生率的比较分析

目的:观察分析ICU(重症监护室)患者应用右美托咪啶与咪达唑仑镇静后谵妄发生率的比较。方法:选取本院(在2017年3月-2018年4月)收治的66例ICU患者,按照不同治疗方法分为右美托咪啶组(33例,应用右美托咪啶治疗方法)和咪达唑仑组(33例,应用咪达唑仑治疗方法)。采用统计学分析两组ICU患者的平均镇静起效时间、镇静后谵妄发生率。结果:两组ICU患者的平均镇静起效时间比较无统计学意义(P0.05),右美托咪啶组镇静后谵妄发生率显著低于咪达唑仑组ICU患者(P0.05)。结论:ICU患者用右美托咪啶的镇静后谵妄发生率相比起咪达唑仑更低。     

观察右美托咪啶在ICU镇静治疗的效果及安全性

目的研讨右美托咪啶在ICU镇静治疗的效果及安全性。方法选取2015年1~12月在我院ICU接受镇静治疗的患者100例,随机分观察组和对照组,每组50例,对照组采用咪达唑仑治疗,观察组采用右美托咪啶治疗,比较两组患者的Ramsay评分、NRS评分、静推芬太尼次数、镇静效率、各项耗时以及不良反应发生情况。结果观察组与对照组的Ramsay评分差异无统计学意义(P>0.05);NRS评分观察组低于对照组(P<0.05);静推芬太尼次数观察组少于对照组(P<0.05);观察组镇静效率高于对照组(P<0.05);观察组与对照组的机械通气时间比较差异无统计学意义(P>0.05);唤醒时间与拔管时间组间比较观察组优于对照组(P<0.05);两组低血压与心动过缓方面比较差异无统计学意义(P>0.05);两组谵妄比较观察组显著低于对照组(P<0.05)。结论右美托咪啶在ICU镇静治疗的效果较好,且安全性较高,值得临床推广。     

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.     

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.