20%脂肪乳对家兔持续异丙酚输注血药浓度、分布容积及药理效应的影响

目的 探讨20％脂肪乳对家兔持续恒速输注异丙酚血药浓度、分布容积及药理效应的影响.方法 52只家兔随机分为4组(n=13):异丙酚组(P组),低剂量脂肪乳组(L组),高剂量脂肪乳组(H组),生理盐水组(S组).每组家兔以70 mg/(kg·h)持续恒速输注异丙酚120 min.恒速输注异丙酚60 min后,P组维持原速率继续输注异丙酚,L组和H组输注异丙酚同时输注20％脂肪乳,速率分别为0.3 mL/(kg·h)和15 mL/(kg·h);S组输注异丙酚同时输注生理盐水,速率为15 mL/(kg·h),3组输注不同液体时间为60 min.各组取8只家兔于异丙酚输注后30、60、65、70、80、90、105、120 min以及停药后10、20、30、60、120、180 min采血测定异丙酚血药浓度,计算相关药代动力学参数;用平均动脉压(MAP)、心率(HR)、神经反射率评价药理效应;各组另取5只家兔于异丙酚输注120 min时获取家兔脑组织、测量异丙酚脑组织浓度.结果 H组经20％脂肪乳输注后,血药浓度上升,消除相分布容积(V)[各组分别为(34.56±16.11)mL、(33.37±29.87)mL、(7.29±3.20)mL和(35.46±13.58) mL]、稳态分布容积(Vss)[各组分别为(11.13±3.21) mL、(13.87±4.09)mL、(4.82±1.46) mL和(11.61±4.11) mL]降低(P＜0.05);MAP、HR上升(P＜0.05);90、120 min痛觉反射存在率与其余3组比较差异有统计学意义(P＜0.05);120 min时异丙酚脑组织浓度降低[各组分别为(1.92±0.41)μg/g、(1.90±0.53)μg/g、(1.27±0.40)μg/g和(2.02±0.49)μg/g,P＜0.05].结论 当20％脂肪乳以高剂量输注时,可降低异丙酚药物分布容积,升高血药浓度,降低异丙酚脑组织浓度,导致药理效应减弱.以临床营养支持相类似的低速率输注时,并不会对以上指标产生影响.     

Sleep apnea and nocturnal myoclonus in the elderly

—Insomnia, daytime sleepiness, and nocturnal wandering, so common in the elderly, are caused largely by two specific pathophysiologic processes. Sleep apnea is a condition where respiration pauses during sleep, leading to arousal. Sleep apnea is due either to obstruction in the throat or failure of the central respiratory center. Periodic movements in sleep are characterized by frequent ankle and leg flexions, leading to arousal. Sleep apnea and periodic movements in sleep require specific diagnoses and treatments. Each process occurs in 20%–30% of people over 65, and perhaps the majority of older people have one or the other condition or both. Because of possible interactions with these sleep disorders, the widespread prescribing of sleeping pills to elderly patients is irrational and often dangerous. In the future, large-scale clinical trials will be needed to define effective long-term treatments for these conditions and to define when treatment is worthwhile.     

Synthesis and hypnotic activities of <Emphasis Type="Italic">N</Emphasis>-Cbz-α-aminoglutarimidooxy carboxylate derivatives

Typical hypnotic drugs, such as barbitals and glutethimide, have a cyclic imide (-CO-NH-CO-) moiety. The N-Cbz-alpha-aminoglutarimidooxy carboxylate derivatives, which we previously showed exhibit moderate anticonvulsant activities, also have a cyclic imide (-CO-N-CO-) moiety. This structural similarity prompted us to examine the hypnotic activities of the N-Cbz-alpha-aminoglutarimidooxy carboxylate derivatives, and we describe their moderate hypnotic activities here.     

Differences in enhancing effects of zolpidem and benzodiazepine drugs on recurrent inhibition in rat hippocampal slices

It has been reported that the clinical and electroencephalographic profiles of zolpidem, a non-benzodiazepine drug which binds preferentially to the ω₁ benzodiazepine recognition sites located within the GABA_A receptor complex, are different from those of benzodiazepine drugs, which bind non-selectively to the ω₁ and ω₂ sites. In order to clarify the electrophysiological mechanism underlying the unique profile of zolpidem, the present study compared the enhancing effects of zolpidem and two benzodiazepine drugs, triazolam and diazepam, on recurrent inhibition. This inhibition was expressed as suppression of the orthodromically induced population spikes by the preceding antidromic stimulation of the alveus in the CA1 region of rat hippocampal slices. The rank order of potency for enhancing recurrent inhibition was triazolam > diazepam > zolpidem. From the present results and previously reported findings that zolpidem has a lower affinity for the ω₂ sites than diazepam while both have the same affinity for the ω₁ sites, we concluded that the hippocampal recurrent inhibition appears to be enhanced mainly by activation of the ω₂ sites, but not by that of the ω₁ sites. Furthermore, the lower potency of zolpidem for enhancing recurrent inhibition may underlie its unique profile in terms of its clinical and electroencephalographic effects. Received: 1 November 1996/Final version: 22 January 1997     

深圳地区中毒洗胃现状调查

目的 了解深圳地区医院洗胃的基本情况,为合理应用洗胃术提供依据.方法 选取深圳代表性医院24家,采用调查表对2009年洗胃患者的中毒原因、洗胃机数量及分布影响、洗胃效果的因素、不良反应和并发症发生情况进行调查.结果 安眠镇静类药物中毒是导致洗胃的首要原因,在二级医院中以毒物中毒为首位.洗胃机以全自动洗胃机为主,三级医院基本均为全自动洗胃机.全自动洗胃机的不良反应和并发症少于半自动洗胃机.结论 不同医院洗胃主要原因存在差异,尽量选择全自动洗胃机进行洗胃.     

Utilization of analgesics, sedatives, and pain scores in infants with a prolonged hospitalization: A prospective descriptive cohort study

Aim

Describe the utilization of analgesic and sedative medications and documentation of pain scores in a cohort of critically ill infants in a neonatal intensive care unit.

Method

A prospective, longitudinal, cohort study of infants with a predicted length of stay ≥28 days. Dosages and routes of administration of analgesic and sedative medications and documentation of pain scores were collected on a daily basis.

Results

55 infants were enrolled into the study. Oral sucrose was administered to all 55 infants, 51 infants (93%) were administered enteral acetaminophen and 50 (91%) infants were administered morphine during their hospitalization. Sedatives were administered to 42 infants (76%); 36 (65%) were administered chloral hydrate and 32 (58%) were administered intravenous midazolam. With the exception of the first week of admission, when there was highest utilization of opioids and lower use of sucrose, acetaminophen and sedatives, the pattern of administration of analgesic and sedative agents remained relatively constant throughout the hospitalization. Pain scores were documented for 36 (65%) infants during their hospitalisation, however for these 36 infants, pain scores were infrequently recorded.

Conclusion

There was substantial and varied analgesic and sedative use in this cohort of infants, yet infrequent documentation of pain assessment scores. These practices highlight important clinical implications for sick infants requiring careful consideration of pain and distress management.     

短期重复使用几种精神药物对小鼠自主活动和脑单胺递质的影响

目的 观察短期重复使用几种精神药物对小鼠自主活动和脑单胺递质的影响,以评价药物作用的耐受性和副作用。方法 雄性小鼠作为实验对象。中枢兴奋药实验分3组（每组n＝6）：①对照组;②咖啡因（Caf）组30mg/kg;③右旋苯丙胺（Dex）组10mg/kg。催眠药实验分4组（每组n＝6）：①对照组;②三只仑（TZ）组0．04mg/kg;③速可眠（Sec）组60mg/kg;④裉黑素（Mel）组120mg/kg。小鼠灌胃给药,1次／d。于第1天和第7天称重和测定自主活动。Dex和TZ连续用药7d后,用高效液相色谱法测定小鼠大脑皮层单胺递质及其代谢产物的变化。结果 ①对照组和用药组的体重差异无显著性意义;②连续用药7d,Caf和Dex对自主活动的兴奋作用较第1天明显增强（P＜0．05）;③连续用药7d,虽然催眠药对小鼠自主活动仍有显著的抑制作用,但作用强度较之第1天明显降低（P＜0．05）;④Dex和TZ连续用药7d,小鼠在脑皮层单胺递质水平明显改变,但Dex组的双羟基苯乙酸（DOPAC）和5－羟基吲哚乙酸（5－HIAA）及TZ组的5－HIAA明显降低（P＜0．05）。结论 ①连续应用催眠药1周,其作用有一定的耐受性;②重复使用Dex和TZ1周对鼠脑单胺递质的代谢可能产生不良影响。     

Effect of valerian on human sleep

The effect of an aqueous extract of valerian root on sleep was studied in two groups of healthy, young subjects. One group (N=10) slept at home, the other (N=8) in the sleep laboratory. Sleep was evaluated on the basis of questionnaires, self-rating scales and night-time motor activity. In addition, polygraphic sleep recordings and spectral analysis of the sleep EEG was performed in the laboratory group. Under home conditions, both doses of valerian extract (450 and 900 mg) reduced perceived sleep latency and wake time after sleep onset. Night-time motor activity was enhanced in the middle third of the night and reduced in the last third. The data suggest a dose-dependent effect. In the sleep laboratory, where only the higher dose of valerian was tested, no significant differences from placebo were obtained. However, the direction of the changes in the subjective and objective measures of sleep latency and wake time after sleep onset, as well as in night-time motor activity, corresponded to that observed under home conditions. There was no evidence for a change in sleep stages and EEG spectra. The results indicate that the aqueous valerian extract exerts a mild hypnotic action.     

Effect of zolpidem on sleep and sleep EEG spectra in healthy young men

A single 10 mg dose of zolpidem, an imidazopyridine hypnotic, was administered to young, healthy male volunteers prior to bedtime. The drug reduced REM sleep but did not significantly affect other sleep stages and subjective sleep parameters. All-night spectral analysis of the EEG revealed that power density in nonREM sleep was reduced in the low-frequency range (1.25–2.5 Hz; 5.25–10.0 Hz) and increased in the spindle frequency range (12.25–13.0 Hz). Significant changes in the EEG spectrum were present in the first 4 h of sleep. The pattern of the spectral changes was similar to those induced by other hypnotics that bind to the GABA_A/benzodiazepine receptor complex. There were no residual effects of zolpidem on psychomotor performance in the morning, on the self-rated state in the morning and at noon, and on sleep and EEG parameters in the subsequent drug-free night.     

Laser-evoked potentials to noxious stimulation during hypnotic analgesia and distraction of attention suggest different brain mechanisms of pain control

Psychological accounts of hypnosis have hypothesized that hypnosis and attention might share similar mechanisms and that hypnosis simply represents an extensive state of reduced attention. This assumption implies that reports of pain and electrocortical brain responses to painful stimulation should be similarly reduced when subjects are exposed to suggestions of hypnotic analgesia (HA) or requested to distract their attention from painful stimuli (distraction of attention: DA) as compared to a control condition (CC). To test this hypothesis, we recorded event-related electrical brain potentials to noxious laser-heat stimuli and pain reports during HA, DA, and CC from subjects highly susceptible to hypnotic suggestions. Pain reports were significantly reduced during HA and DA as compared to CC. The amplitudes of the late laser-evoked brain potential (LEP) components N200 and P320 were also significantly smaller during DA than during CC. However, no significant difference of these late LEP amplitudes was obtained for HA as compared to CC. Results indicate that hypnotic analgesia and distraction of attention represent different mechanisms of pain control and involve different brain mechanisms.