The Pharmacological and Toxicological Studies of Tou Tong Shen Xiao Dan

Tou Tong Shen Xiao Dan(TTSXD)consisted of traditional Chinese Medicines including:Chuanxion(Ligustici Chuanxiong),Hounghua(Salt lower),Taoren(Peach seed),Gouteng(Hooked Uncaria),Xixin(Herb Asari)and Baizhi(Dahurian angelica root)etc.The results of thepresent study showed that TTSXD had strong sedative and analgesic effects and could dilate thblood ves-sels,lower blood presure,increase cerebral blood flow(CBF),raise the ability to tolerate hypoxia.Improve the microcirculation,prevent platelet aggregation and reduce the visicosity of the wholeblood. Acute and subacute toxicological studies didn't demonstrate toxic and side effects on livingbodies.     

酸枣仁中黄酮类镇静催眠有效成分的研究

本文对辽宁产的酸枣仁中的黄酮类成分进行了初步研究,从中分离出一种淡黄色无定形粉末,经鉴定为黄酮碳甙(spinosin)。动物实验证明,酸枣仁中镇静催眠作用的成分不仅是皂甙成分,黄酮也是主要成分之一。     

老年机械通气镇静治疗时不良反应的原因分析和护理

目的 探讨ICU老年机械通气患者镇静治疗时发生不良反应的原因及护理对策.方法 对2005年1月至2006年8月期间行镇静治疗的68例老年气管插管患者出现的各类不良反应进行分类统计及原因分析.结果 老年患者镇静治疗过程中出现血压下降、肺部感染、镇静过深等各类不良反应,经及时治疗和护理干预后均得到有效控制.结论 老年机械通气患者镇静治疗时,易发生各类不良反应,须及时评估患者的镇静等级和意识变化,密切监测患者的生命体征,加强呼吸道管理.     

缬草西番莲镇静催眠作用的研究

目的：研究不同剂量缬草西番莲水提物的镇静催眠作用并确定其活性部位及分析其有效剂量。方法：观察不同剂量缬草西番莲水提物对小鼠自主活动的影响以及直接镇静催眠作用、及与戊巴比妥钠的协同作用。结果：缬草西番莲水提物能显著增加小鼠睡眠率,减少小鼠的自主活动次数;延长阈上剂量戊巴比妥钠睡眠时间,缩短入睡潜伏期,显著增加阈下剂量戊巴比妥钠小鼠睡眠率。结论：缬草西番莲水提物具有良好的镇静催眠作用,是其镇静催眠活性的有效组分。     

Comparison of effects of propofol and midazolam at sedative concentrations on sympathetic tone generation in the isolated spinal cord of neonatal rats

BACKGROUND: Propofol and midazolam are common sedatives for critically ill patients. Little is known about the effects of propofol and midazolam on central sympathetic activity when drug concentrations in extracellular milieu are under precise control. Previous work using an in vitro neonatal rat splanchnic nerve-spinal cord preparation has demonstrated that tonic sympathetic activity is generated spontaneously in the thoracic spinal cord. The aim of this study was to investigate the concentration effects of propofol and midazolam on spinally generated sympathetic activity. METHODS: Using an in vitro neonatal rat splanchnic nerve-spinal cord preparation that allows the precise control of drug concentrations, the central sympathetic effects elicited by the application of propofol (10-640 microM) and midazolam (10-640 microM) were compared. RESULTS: There was a prompt decrease in sympathetic activity on application of propofol or midazolam in a concentration-dependent manner. A significant decrease in sympathetic activity was observed on application of propofol at 80-640 microM; however, the application of propofol at 10-40 microM caused only a slight alteration in activity. The sympathetic activity was not altered significantly by 10 microM of midazolam, but the application of midazolam at 20-640 microM caused a significant decrease in activity. Thus, in these experimental conditions, the minimum concentration of propofol causing a significant decrease in sympathetic activity was 80 microM and that of midazolam was 20 microM. CONCLUSIONS: The current findings suggest that the administration of 9-19 microM of propofol or 0.7-0.9 microM of midazolam, the clinically relevant concentrations for sedation, does not alter central sympathetic outflow at the spinal cord level. However, propofol at a concentration of 86 microM, which could be achieved by a single-bolus loading dose to induce sedation, depresses central sympathetic activity.     

基于均匀设计法对酸枣仁镇静催眠有效组分的配伍研究

目的 优选酸枣仁中3种具有镇静催眠作用的主要有效组分(总皂苷、总黄酮、总生物碱)最佳配伍.方法 采用均匀设计法将70只小鼠随机分为7组,分别为对照组及给药A～F组,观察各组小鼠自主活动情况;采用阈上剂量戊巴比妥钠(45 mg/kg)协同睡眠试验,以小鼠的睡眠潜伏期和睡眠时间为评价指标,筛选酸枣仁镇静催眠有效组分的最佳配伍.对所得有效组分最佳配伍的药效进行比较和验证实验.结果 与对照组比较,给药A、C、E组小鼠自主活动减少(P＜0.05、0.01),C、D组小鼠站立次数略有减少(P＜0.05).在阈上剂量戊巴比妥钠协同试验中,给药组C～F睡眠潜伏期显著缩短(P＜0.01),B～F组睡眠时间显著延长(P＜0.01).经多元统计分析,酸枣仁镇静催眠有效组分的最佳配伍组合为总皂苷200mg/kg、总黄酮0 mg/kg、总生物碱20 mg/kg.结论 应用均匀设计与药效学相结合确定中药有效组分配伍的方法是可行的.验证实验表明,酸枣仁有效组分的最佳配伍组合可以达到与原药材相同的疗效.     

异丙酚-瑞芬太尼在胃镜检查的应用观察

目的研究异丙酚-瑞芬太尼在胃镜检查中应用的镇静效果及安全性。方法胃镜检查患者镇静组106例给予异丙酚-瑞芬太尼镇静,对照组162例常规胃镜检查。比较两组患者胃镜检查中的反应和感受、检查时间,记录镇静组清醒时间。结果与对照组相比,镇静组患者胃镜检查时间短(P<0.05),患者98.1%舒适无痛苦(P<0.05);镇静组清醒时间为(7.9±2.9)min。结论胃镜检查中适量应用异丙酚-瑞芬太尼镇静、镇痛是安全、有效的。     

In silico and in vivo investigation of ferrocene‐incorporated acyl ureas and homoleptic cadmium carboxylate derivatives for anticonvulsant,anxiolytic, and sedative potential

In this study different derivatives of ferrocene‐incorporated acyl ureas and homoleptic cadmium carboxylates were investigated for potential anticonvulsant, anxiolytic and sedative properties, using in‐silico and in‐vivo techniques. The molecular docking studies reveled that ferrocene compounds derivative 1‐(4‐bromobenzoyl)‐3‐(4‐ferrocenylphenyl) urea (PB1) and cadmium compounds derivative bis (diphenylacetato) cadmium (II) (DPAA) exhibit binding affinities against various neurotherapeutic molecular targets involved in epilepsy, anxiety, and sedation. Both PB1 and DPAA showed high binding affinities against protein targets like mammalian shaker voltage dependent potassium channel beta subunit complex, calcium release‐activated calcium channel, sodium channel 2A inactivation gate, human sodium/hydrogen exchanger regulatory factor, and gamma amino butyric acid A receptor associated protein. PB1 (2–10 mg/kg) and DPAA (1–5 mg/kg) delayed onset time of pentylenetetrazole‐induced myoclonic jerks and tonic‐clonic seizures in mice while decreased duration of tonic‐clonic seizures, determining the anticonvulsant effect of these compounds. PB1 and DPAA (0.5–1 mg/kg) exhibited anxiolytic effect by increasing time spent and number of animals entries into open arms, while decreasing time spent in dark compartment. Furthermore, PB1 (0.5–1 mg/kg) and DPAA (0.1–1 mg/kg) reduced onset time of sleep and increased duration time of sleep in mice, showing sedative effect. Taken together, our results indicate that aforementioned derivatives of ferrocene and cadmium are potent neurotherapeutic agents possessing anticonvulsant, anxiolytic and sedative properties.     

黄芩汤及其组成药物药理作用的初步研究

黄芩汤及其组成药物甘草、乌枣、黄芩和芍药有明显抗炎作用,除芍药外,其它药物有明显解痉作用。黄芩,甘草和黄芩汤有明显解热作用。黄芩汤和芍药加甘草有非常明显的镇痛作用,黄芩汤和单味黄芩有一定的镇静作用。