布托啡诺对子宫切除术牵拉反应的抑制作用

目的比较咪哒唑仑、芬太尼和布托啡诺不同配伍对子宫切除术内脏牵拉反应的抑制作用。方法选择子宫切除术患者60例,随机分为3组,咪哒唑仑组(M组,n=20)、芬太尼组(F组,n=20)和布托啡诺组(B组,n=20)。术中探查、结扎子宫韧带及切除子宫、关腹各阶段进行疼痛和镇静评分。结果与M组和B组同一阶段比较,F组VAS评分和Ramesay评分居中,差别有统计学意义(P<0.05),与M组和F组同一手术阶段比较,B组VAS评分最低、Ramesay评分最高,差别有统计学意义(P<0.05)。结论本研究条件下,子宫切除术患者椎管内麻醉辅以咪哒唑仑2mg、芬太尼0.05mg和布托啡诺1mg,可以有效的抑制内脏牵拉反应。     

布托啡诺复合咪达唑仑在阑尾切除术麻醉中的效果分析

目的:探讨布托啡诺复合咪达唑仑在阑尾切除术麻醉中的效果。方法:选择阑尾切除术患者100例,随机均分为两组:观察组(A组)及对照组(B组)。A组:布托啡诺复合咪达唑仑。B组:芬太尼和氟哌利多。①两组患者均采用警觉/镇静观察评分法:给药后5分钟、15分钟、30分钟和60分钟的镇静情况;②观察两组患者手术过程内脏牵拉反应的程度;③观察给药后60分钟、120分钟时两组患者对手术过程的记忆情况;④设计麻醉满意程度调查表,调查两组患者对麻醉的满意情况。结果:A组给药后5分钟、15分钟、30分钟和60分钟镇静评分均低于B组(P<0.05)。A组术中牵拉反应优良率高于B组(P<0.05)。A组患者遗忘率高于B组(P<0.05)。A组患者对麻醉满意率高于B组(P<0.05)。结论:布托啡诺复合咪达唑仑在阑尾切除术麻醉中的效果显著,值得借鉴。     

不同剂量布托啡诺复合咪达唑仑用于妇科手术中镇静作用的临床观察

目的评价不同剂量布托啡诺复合咪达唑仑用于妇科手术中的镇静效果及安全性。方法 ASA1-2级择期妇科手术患者60例,随机分为A、B、C 3组。麻醉方法采取腰麻联合硬膜外腔阻滞,于切皮前各组分别给予如下剂量的镇静药物,A组布托啡诺5μg·kg-1＋咪达唑仑30μg·kg-1,B组布托啡诺10μg·kg-1＋咪达唑仑30μg·kg-1,C组布托啡诺15μg·kg-1＋咪达唑仑30μg·kg-1。记录给药前、给药后5min、10min、15min、30min、45min及1h的生命体征数据、患者镇静评分、观察不良反应例数、总体满意度。结果 B、C组的镇静评分明显高于A组;C组呼吸抑制及血压下降发生率明显高于A组、B组。结论妇科手术患者术前静脉注射布托啡诺10μg·kg-1＋咪达唑仑30μg·kg-1,可达到理想的术中镇静效果,且不良反应相对较少。     

咪达唑仑伍用布托啡诺在腹部手术硬膜外麻醉中的临床观察

目的 观察咪达唑仑伍用布托啡诺在腹部手术硬膜外麻醉中的效果.方法 下腹部择期手术患者60例,ASA Ⅰ～Ⅱ级,随机分为2组,Ⅰ组硬膜外麻醉时给予氟哌利多和芬太尼,Ⅱ组给予眯达唑仑和布托啡诺,每组30例,全程观察患者血压、心率、呼吸频率、血氧饱和度、镇静效果及术中的不良反应.结果 Ⅱ组镇静效果、对抗内脏牵拉反应程度及顺性行遗忘明显优于Ⅰ组(P<0.05).结论 眯达唑仑伍用布托啡诺辅用于硬膜外麻醉效果明显,不良反应轻,能够减少对手术的不良记忆和提高麻醉满意率.     

布托啡诺复合咪哒唑仑在区域麻醉中的镇静效果及安全性研究

目的探讨布托啡诺复合咪哒唑仑在区域麻醉中的镇静效果及安全性。方法选择本院需要区域麻醉下行手术的患者50例,随机分为A组（布托啡诺组）25例,B组（芬太尼组）25例。麻醉完成后,A组首量为布托啡诺15μg/kg＋咪哒唑仑40μg/kg,维持量为布托啡诺7.5μg/（kg·h）＋咪哒唑仑20μg/（kg·h）;B组：首量为芬太尼0.75μg/kg＋咪哒唑仑40μg/kg,维持量芬太尼0.375μg/（kg·h）＋咪哒唑仑20μg/（kg·h）。观察各时点MAP、HR、SpO2：、RR,（OAA/S）评分。结果两组在镇静效果和安全性方面无统计学意义。结论布托啡诺复合咪哒唑仑在区域麻醉中能维持术中持续平稳镇静,术后恢复迅速,不会延长术后滞留时间,术中遗忘率。     

布托啡诺复合咪达唑仑应用于阑尾切除术麻醉中的临床观察

目的 观察布托啡诺复合咪达唑仑应用于阑尾切除术麻醉的临床效果.方法 选取连续硬膜外阻滞麻醉下行阑尾切除术患者80例,随机分为观察组和对照组,每组40例.观察组给予布托啡诺复合咪达唑仑,对照组给予氟芬合剂进行辅助麻醉;比较2组术中镇静程度、牵拉反应、遗忘程度、不良反应及术后满意度.结果 给药后5 min、15 min、30 min和60 min时,观察组镇静评分明显低于对照组(P<0.05);观察组抑制内脏牵拉反应有效率明显高于对照组(P<0.05);给药后60 min、120 min,观察组所有患者对手术过程均无记忆,而对照组18例患者(占45%)能回忆手术时情景(P<0.05);2组术中血压、心率、脉搏血氧饱和度总体处于平稳状态,无严重不良反应出现;观察组满意度明显高于对照组(P<0.05).结论 布托啡诺复合咪达唑仑作为辅助用药应用于阑尾切除术麻醉,具有良好的镇静、镇痛和遗忘作用,并能有效抑制内脏牵拉反应,从而提高麻醉质量,增加患者的满意度,有利于手术的顺利进行,值得临床推广.     

布托啡诺抑制子宫切除术牵拉反应的作用观察

目的观察布托啡诺抑制子宫牵拉反应的疗效,评价临床效果及安全性。方法选择60例ASAⅠ级择期患者,随机分为两组,每组30例:布托啡诺组(R组),杜氟合剂组(F组)。R组静脉滴注布托啡诺2mg(生理盐水稀释至50mL);F组静注氟哌利多2.5mg和杜冷丁50mg。观察术中镇静状态、血流动力学变化、牵拉反应和不良反应。结果两组患者镇静评分均在2~4级。血流动力学变化布托啡诺组相对平稳,杜氟合剂组用药后MAP、HR、RR均有下降;两组抑制牵拉反应效果和不良反应相似。结论在子宫切除术中腰-硬联合麻醉的基础上辅助应用布托啡诺2mg,术中血流动力学平稳,能有效地抑制子宫牵拉反应。     

咪达唑仑复合芬太尼在阑尾切除术硬膜外麻醉中的临床应用

目的观察咪达唑仑复合芬太尼在硬膜外麻醉阑尾切除术的临床应用效果。方法行阑尾切除手术患者50例,ASAⅠ ~Ⅱ级,随机分成两组,咪达唑仑复合芬太尼（MF组,n =25）和氟哌利多复合芬太尼（DF组,n=25）。两组均为T12~L1硬膜外穿刺,麻醉平面T6-L3,观察两组患者术中牵拉反应、镇静程度及不良反应等发生情况。结果观察术中两组中MF组更好地抑制术中的牵拉反应;手术开始后5、15、30 min三个不同时间点两组的警觉/镇静（OAA/S）评分,MF组明显低于DF组;MF组患者术中遗忘率高于DF组,差异有统计学意义（P〈0.05）。结论咪达唑仑复合芬太尼用于硬膜外麻醉下阑尾切除术的临床效果优于氟哌利多联合芬太尼,有良好的术中遗忘、镇静及抗牵拉反应的作用。     

布托啡诺联合用药防治剖宫产术中胃牵拉痛和寒战的临床观察

目的比较布托啡诺复合咪哒唑仑与单独使用布托啡诺或布托啡诺复合曲马多防治腰-硬联合麻醉下剖宫产术中胃牵拉痛和寒战的临床效果。方法选择在腰-硬联合麻醉下行剖宫产术患者120例,随机分成3组,每组40例。胎儿取出后即刻,B组静滴布托啡诺15ug/kg,BM组静滴布托啡诺10μg/kg＋咪哒唑仑0.03mg/kg,BQ组静滴布托啡诺10μg/kg＋曲马多1mg/kg。观察术中产妇的MAP、HR、RR、SPO2的变化,及给药前（T0）、注药后5min（T1）、给药后30min（T2）、给药后60min（T3）产妇的RSS评分和胃牵拉痛的VAS评分及出现寒战的情况。结果 3组产妇MAP、HR、RR、SPO2的变化的差异无统计学意义。给药前（T0）3组产妇RSS评分、VAS评分、Wrench寒战分级,P〉0.05差异无统计学意义。T1、T2、T3时3组产妇的RSS评分差异无统计学意义。T1、T2、T3时VAS,B组明显高于BM组、BQ组,P〈0.01。T1、T2、T3时Wrench寒战分级,B组明显高于BM组、BQ组,P〈0.01。不良反应：3组均未出现呼吸抑制和呕吐者,恶心B组出现2例,BM、BQ组分别出现3例和2例（P〉0.05）。结论布托啡诺复合咪哒唑仑和布托啡诺复合曲马多防治剖宫产术中胃牵拉痛和寒战,优于单独用药。     

布托啡诺用于肺叶切除术后自控静脉镇痛的疗效观察

目的 探讨布托啡诺用于开胸肺叶切除术后患者自控静脉镇痛（PCIA）的效果和安全性.方法 选择40例择期开胸肺叶切除术后患者随机分为布托啡诺组（B组）和芬太尼组（F组）,分别使用布托啡诺和芬太尼进行自控静脉镇痛（（PCIA）.记录术后2、4、8、12、24、48h各时间点的视觉模拟评分（VAS）、镇静评分、不良反应、胸腔引流量和患者满意度等.结果 B组术后12h镇痛VAS评分好于F组,其它各时间点VAS评分及胸腔引流量无统计学差异;镇静评分、患者满意度B组高于F组,而不良反应恶心、呕吐的发生牟B组少于F组.结论 布托啡诺用于开胸肺叶切除术后PCIA,效果确切、安全可靠,不良反应低于芬太尼PCIA.     

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.

     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

2-(Acetoxyphenyl)-(Z)-styryl sulfides as cyclooxygenase inhibitors

2-(Acetoxyphenyl)-(Z)-styryl sulfides are described as selective cyclooxygenase-2 (COX-2) inhibitors, useful for treating inflammation and COX-2-mediated disorders including neoplasia. 2-(Acetoxyphenyl)-(Z)-styryl sulfide is claimed to be the most potent COX inhibitor in the series with a COX-2 selectivity ratio of 33. This compound is also claimed to be superior to celecoxib (Celebrex^®, Pfizer) in inhibiting cell growth of colorectal carcinoma cells. In this evaluation, the COX inhibitory activity of this compound is compared to that previously disclosed for diarylheterocycles and 2-(acetoxyphenyl)alkyl sulfides. The validity of the DLD-1 cell line in the growth inhibition studies is questioned based on recent literature reports indicating the lack of COX-2 expression in this cell line.     

Sleep-disordered breathing with chronic opioid use

Chronic opioid use for pain relief or as substitution therapy for illicit drug abuse is prevalent in our societies. In the US, retail distribution of methadone and oxycodone has increased by 824 and 660%, respectively, between 1997 and 2003. μ-Opioids depress respiration and deaths related to illicit and non illicit chronic opioid use are not uncommon. Since 2001 there has been an emerging literature that suggests that chronic opioid use is related to central sleep apnoea of both periodic and non-periodic breathing types, and occurs in ～ 30% of these subjects. The clinical significance of these sleep-related abnormalities are unknown. This review addresses the present knowledge of control of ventilation mechanisms during wakefulness and sleep, the effects of opioids on ventilatory control mechanisms, the sleep-disordered breathing found with chronic opioid use and a discussion regarding the future research directions in this area.     

Drug targets for cognitive enhancement in neuropsychiatric disorders

The investigation of novel drug targets for treating cognitive impairments associated with neurological and psychiatric disorders remains a primary focus of study in central nervous system (CNS) research. Many promising new therapies are progressing through preclinical and clinical development, and offer the potential of improved treatment options for neurodegenerative diseases such as Alzheimer's disease (AD) as well as other disorders that have not been particularly well treated to date like the cognitive impairments associated with schizophrenia (CIAS). Among targets under investigation, cholinergic receptors have received much attention with several nicotinic agonists (α7 and α4β2) actively in clinical trials for the treatment of AD, CIAS and attention deficit hyperactivity disorder (ADHD). Both glutamatergic and serotonergic (5-HT) agonists and antagonists have profound effects on neurotransmission and improve cognitive function in preclinical experiments with animals; some of these compounds are now in proof-of-concept studies in humans. Several histamine H3 receptor antagonists are in clinical development not only for cognitive enhancement, but also for the treatment of narcolepsy and cognitive deficits due to sleep deprivation because of their expression in brain sleep centers. Compounds that dampen inhibitory tone (e.g., GABA_A α5 inverse agonists) or elevate excitatory tone (e.g., glycine transporter inhibitors) offer novel approaches for treating diseases such as schizophrenia, AD and Down syndrome. In addition to cell surface receptors, intracellular drug targets such as the phosphodiesterases (PDEs) are known to impact signaling pathways that affect long-term memory formation and working memory. Overall, there is a genuine need to treat cognitive deficits associated with many neuropsychiatric conditions as well as an increasingly aging population.