曲马多与氯胺酮的超前镇痛作用在剖宫产中的比较

目的：比较剖宫产手术切皮前硬膜外小剂量使用曲马多与氯胺酮的超前镇痛效应。方法：选择72例择期或急诊剖宫产手术病人随机分为3组,每组24例,分别在手术切皮前经硬膜外导管注入曲马多25mg（Ⅰ组）,氯胺酮30mg（Ⅱ组）,生理盐水0.5ml（Ⅲ组）。术后均采用硬膜外病人自控镇痛（PCEA）。观察项目：（1）3组剖宫产手术病人中的手术时间。（2）2%利多卡因麻醉用药总量。（3）术后疼痛开始时间。（4）术后PCEA用药量。（5）PCEA镇痛的不良反应（恶心、呕吐）。（6）PCEA镇痛后VAS评分。结果：3组病人,在手术时间上无统计学意义。术中麻醉药用量,Ⅰ组、Ⅱ组与Ⅲ组相比明显减少,差异有显著性（P〈0.05）。但Ⅰ组与Ⅱ组之间差异无显著性（P〉0.05）。术后疼痛开始时间,与Ⅲ组相比较,Ⅰ组与Ⅱ组均明显延长（P〈0.05）,PCEA术后用量依次为Ⅲ组〉Ⅰ组〉Ⅱ组,3组差异均有显著性（P〈0.05）。PCEA的VAS评分,3组间无差异。结论：手术切皮前经硬膜外小剂量曲马多或氯胺酮均降低术后病人对PCEA镇痛药的需要量,但氯胺酮的硬膜外超前镇痛效果较曲马多更有效。     

越鞠丸石油醚部位潜在的快速抗抑郁作用与BDNF、TrkB蛋白表达的上调相关

目的研究越鞠丸石油醚部位是否具有快速抗抑郁潜力,并对其有效剂量及潜在的生物学机制进行了探讨。方法将44只昆明种♂小鼠随机分成空白组(生理盐水组)、越鞠丸石油醚部位(YJ-PE)高、中、低剂量组及氯胺酮组。单次给药后30 min对昆明小鼠进行小鼠悬尾行为绝望测试。再将24只昆明种♂小鼠分成空白组、筛选出有效的越鞠丸石油醚部位低剂量组和氯胺酮组,单次给药24 h后进行小鼠悬尾行为绝望测试。利用Western blot实验分别检测给药后30 min及24 h小鼠海马区BDNF和TrkB蛋白的表达变化。结果单次给药越鞠丸石油醚部位从30 min到24 h均能对其小鼠悬尾的行为绝望行为产生抗抑郁作用。给予越鞠丸石油醚部位30 min后小鼠海马中的BDNF及其受体TrkB的表达明显上调,且这种抗抑郁的作用机制可持续到24 h。结论越鞠丸石油醚部位(低剂量)具有快速抗抑郁的药物潜力,且这种潜在的快速抗抑郁作用与BDNF及其受体TrkB的激活相关。     

基于突触可塑性机制探讨氯胺酮抗抑郁作用的研究现状

氯胺酮是一种离子型谷氨酸N-甲基-D-天冬氨酸(NMDA)受体拮抗药,常用于麻醉诱导和维持.近年来,突触可塑性机制成为氯胺酮抗抑郁作用的研究热点,其机制涉及多种兴奋性神经递质、α-氨基-3-羟基-5-甲基-4-异恶唑-丙酸受体(AMPAR)、脑源性神经营养因子(BDNF)、西罗莫司靶蛋白(mTOR)、真核延伸因子2激酶...     

氯胺酮快速抗抑郁机制研究进展

<正>抑郁症(Major Depressive Disorder,MDD)是一种以显著而持久的心境低落、思维迟缓、认知功能损害、意志活动减退和躯体症状为主要临床特征的一类心境障碍疾病。MDD具有高致残率和高自杀率,全球约有17%的人在经受着这种疾病,长期的药物治疗造成了患者及其家庭的严重生活经济负担~([1])。抑郁症是一种异质性的综合征,使其难以确定潜在的病理生理机制,从而使抑郁症和相关的情绪障碍     

越鞠丸石油醚部位潜在的快速抗抑郁作用与BDNF、TrkB蛋白表达的上调相关北大核心CSCD

目的研究越鞠丸石油醚部位是否具有快速抗抑郁潜力,并对其有效剂量及潜在的生物学机制进行了探讨。方法将44只昆明种♂小鼠随机分成空白组(生理盐水组)、越鞠丸石油醚部位(YJ-PE)高、中、低剂量组及氯胺酮组。单次给药后30 min对昆明小鼠进行小鼠悬尾行为绝望测试。再将24只昆明种♂小鼠分成空白组、筛选出有效的越鞠丸石油醚部位低剂量组和氯胺酮组,单次给药24 h后进行小鼠悬尾行为绝望测试。利用Western blot实验分别检测给药后30 min及24 h小鼠海马区BDNF和TrkB蛋白的表达变化。结果单次给药越鞠丸石油醚部位从30 min到24 h均能对其小鼠悬尾的行为绝望行为产生抗抑郁作用。给予越鞠丸石油醚部位30 min后小鼠海马中的BDNF及其受体TrkB的表达明显上调,且这种抗抑郁的作用机制可持续到24 h。结论越鞠丸石油醚部位(低剂量)具有快速抗抑郁的药物潜力,且这种潜在的快速抗抑郁作用与BDNF及其受体TrkB的激活相关。     

曲马多辅助氯胺酮静脉复合麻醉40例

目的：观察曲马多辅助儿童氯胺酮静脉复合麻醉的效果。方法：９０例患儿,分成曲马多组４０例,氟哌啶组５０例,其中曲马多组用曲马多２ｍｇ／ｋｇ,氟哌啶０．１ｍｇ／ｋｇ辅助氯胺静脉麻醉,氟哌啶组不用曲马多,余法同上组。结果：曲马多组患儿ＨＲ,ＳｐＯ２,ＭＡＰ均保持稳定,且在镇痛及抑制牵拉反应方面与氟哌啶组比较差异显著（Ｐ〈０．０５）,结论：曲马多加氟哌啶辅助小儿氯胺酮静脉复合麻醉无明显呼吸,循环抑制,安全     

氯胺酮的抗抑郁作用及其机制

<正>氯胺酮(ketamine)俗称K粉,为苯环利啶(PCP)的衍生物,是一种高亲和、非竞争性的N-甲基-D-天门冬氨酸(N-methyl-D-aspartate,NMDA)受体拮抗剂。氯胺酮最初作为一种分离麻醉剂而应用于临床,其后发现,氯胺酮还可以产生愉悦的幻觉、浮漂感和分离感等而被作为一种娱乐性新     

小剂量氯胺酮对静脉曲马多术后镇痛效果的影响

<正>曲马多在临床可用于患者自控镇痛(PCA),近来有某些辅助药物被用来提高术后镇痛的效果,并取得了一定成效,本文拟就小剂量氯胺酮辅助曲马多用于患者自控镇痛做一研究,探讨小剂量氯胺酮对曲马多自控镇痛的影响,并评价其安全性。     

耶鲁发现堪比氯胺酮的抗抑郁新药

耶鲁大学近期发表于英国《分子精神病学》（MolecularPsychiatry）杂志的一项研究显示,一种正在开发中的天冬氨酸（NMDA）通路新药Lanicemine（AZD6765）具有与氯胺酮相仿的抗抑郁作用,但没有被作为毒品滥用时的危险副作用。     

氯胺酮抗抑郁作用快速起效机制及发展前景

<正>抑郁症是一种常见的慢性复发性疾病。抑郁症的主要表现有快感缺失、无望感、无助感、自我评价下降等症状。全球有17%的人口饱受抑郁症困扰[1]。抑郁症严重性的另外一些表现是自杀危险性增加,以及对共病抑郁障碍的慢性躯体疾病病人愈后和转归产生消极影响。与其他严重疾病相比,抑郁症给社会造成的经济负担是惊人的。     

Effectiveness of memantine on depression-like behavior,memory deficits and brain mRNA levels of BDNF and TrkB in rats subjected to repeated unpredictable stress

Background

Previous clinical and preclinical studies have indicated that the N-methyl-d-aspartate (NMDA) receptor antagonist, memantine, has neuroprotective properties as well as antidepressant effects. The present study was designed to examine behavioral and molecular effects of memantine administration in rats subjected to the repeated unpredictable stress (RUS) paradigm.

The Effects of Tramadol on Electroencephalographic Spectral Parameters and Analgesia in Rats

The effects of different doses of tramadol on analgesia and electroencephalographic (EEG) spectral parameters were compared in rats. Saline or tramadol 5, 10, 20 or 40 mg/kg was administered. The degree of analgesia was evaluated by tail-flick latency, and the degree of seizure was measured using numerical seizure score (NSS). Additionally, band powers, median power frequency and spectral edge frequency 95 were measured to quantify the EEG response. All doses of tramadol produced spike-wave discharge. Tramadol significantly and dose-dependently increased the analgesia, but these effects did not correspond with the changes in the EEG spectral parameters. NSS significantly increased in the Tramadol 20 and 40 mg/kg treatment groups compared to the Control and TRA5 groups, and two rats given 40 mg/kg had convulsions. In conclusion, tramadol dose-dependently increased the analgesic effect, and the 10 mg/kg dose appears to be a reliable clinical dose for analgesia in rats, but dose-dependent increases in analgesia and seizure severity did not correlate with EEG spectral parameters.     

Antidepressant and anxiolytic effects of the proprietary Chinese medicine Shexiang Baoxin pill in mice with chronic unpredictable mild stress

Depression and anxiety often co-occur with cardiac diseases. The Shexiang Baoxin pill (SBP) is a proprietary Chinese medicine initially used to treat cardiac conditions. This study explored whether SBP has antidepressant and anxiolytic effects in addition to hormonal and psychotropic mechanisms. Mice underwent 6 weeks of chronic unpredictable mild stress (CUMS) to induce depression- and anxiety-like behavior. During the 6-week experiment, mice received SBP at intragastric doses of 20.25 mg/kg or 40.5 mg/kg daily. Animals were then tested for depression in sucrose preference, forced-swimming, and tail suspension paradigms, and for anxiety in open field and elevated plus maze tests. Both SBP doses significantly reduced anhedonic behavior in the sucrose preference test; the high SBP dose also increased the number of entries into the central zone of the open field. SBP-treated mice had markedly lower blood levels of corticotrophin-releasing hormone (CRH) and adrenocorticotropic hormone (ACTH) than stressed mice treated with vehicle. Either low- or high-dose SBP reversed stress-induced reductions of norepinephrine (NE) and dopamine (DA) metabolites and the expression levels of brain-derived neurotrophic factor (BDNF), nerve growth factor (NGF), and glial cell-derived neurotrophic factor (GDNF) in related brain regions. These results suggest that SBP could prevent and alleviate prolonged stress-induced anhedonia and anxiety in association with its suppression of the hypothalamic-pituitary-adrenal (HPA) axis hyperactivity, modulation of brain monoamine neurotransmitter metabolism and neurotrophins. SBP may be particularly suitable for the management of depressive and anxiety disorders in patients with cardiac conditions.     

右美托咪定与曲马多对椎管内麻醉后寒战治疗效果的比较

目的研究右美托咪定与曲马多在治疗椎管内麻醉后寒战的临床疗效比较。方法将90例2012年1月至2013年1月期间在我院行腹式妇科手术中出现椎管内麻醉后寒战的患者,随机分为D、T、C三组,每组30例,分别采取不同的措施,D组患者注射右美托咪定,T组患者注射曲马多和C组患者注射生理盐水。观察患者在用药后的寒战改善程度以及恶心,呕吐,强化镇静方面的比较。结果 D、T组寒战级别较C组降低(P<0.05),T组恶心呕吐发生率高于D、C两组(P<0.05),D组的镇静评分高于T、C组。结论右美托咪定与曲马多对于椎管内麻醉后寒战的治疗均有一定的作用,但是相对来说右美托咪定的效果更好,且用药后的不良反应更少,值得在临床上推广使用。     

不同剂量曲马多用于术后静脉镇痛的效果观察

目的探讨曲马多术后镇痛合适的剂量。方法ASAⅠ-Ⅱ级的中下腹手术患者200例,均在气管插管静脉复合麻醉下完成手术,随机分为4组,每组50例。曲马多推荐剂量:T1组负荷剂量3.0mg.kg-1,单次给药量20mg,持续背景输注10mg.h-1,锁定时间5min;T2组负荷剂量1.5mg.kg-1,单次给药量40mg,持续背景输注10mg.h-1,锁定时间10min;自选剂量:T3组负荷剂量1.5mg.kg-1,单次给药量10mg,持续背景输注10mg.h-1,锁定时间5min;T4组负荷剂量0.75mg.kg-1,单次给药量10mg,持续背景输注10mg.h-1,锁定时间5min;观测患者24h内心率、血压、呼吸率、脉氧饱和度、视觉疼痛模拟评分(VAS)、镇静评分、PrinceHenry评分以及不良反应的发生率,并记录患者24h内用药量。结果VAS评分:T4组>T1、T2、T3组(P<0.05),PHS评分:T4组>T1、T2、T3组(P<0.05),恶心发生率T1、T2、T3组>T4组(P<0.05),T1、T2、T3组差异无显著性。排气时间延长发生率4组患者差异无显著性。曲马多24h用药量:T4组>T1组、T2组>T3组(P<0.05)。结论自选剂量T3组能取得同推荐剂量T1和T2组相同的镇痛效果,不良反应的发生率不增加,建议作为曲马多用于本地区术后静脉患者自控镇痛的设置参数。     

The differential regulation of BDNF and TrkB levels in juvenile rats after four days of escitalopram and desipramine treatment

Major depressive disorder is a major health problem in adults and is now recognized as a substantial problem in children as well. Tricyclic antidepressants, including desipramine (DMI), are no better than placebo in treating childhood and adolescent depression, but are effective in treating adult depression. Several studies have suggested that normal BDNF (brain-derived neurotrophic factor) signaling is necessary for antidepressant drug action. Antidepressant drugs induce several plastic changes in the rodent brain which may be associated with changes in BDNF levels and/or with BDNF function. In the present study we report parallel measurements of BDNF mRNA and protein in the frontal cortex and hippocampus after four days of twice daily treatments with escitalopram, a selective serotonin reuptake inhibitor, and desipramine, a tricyclic antidepressant. Post-natal day 13, 21, 28 and adult rats were used in this study. TrkB (the primary receptor for BDNF) mRNA levels were also examined under the same treatment conditions. BDNF mRNA and protein levels, as well as TrkB mRNA levels, were increased significantly in post-natal day 13 pups after escitalopram treatment as compared to control, but desipramine failed to increase either BDNF or TrkB. The failure of desipramine to increase BDNF and TrkB levels in juvenile rats is consistent with the lack of efficacy of desipramine in children and adolescents. The serotonergic nervous system matures earlier than the noradrenergic system, which may explain why escitalopram, but not desipramine, increases BDNF and TrkB levels.     

盐酸曲马多片溶出度测定

目的建立盐酸曲马多片溶出度测定方法。方法以0.01 mol/L盐酸为溶出介质,采用高效液相色谱法测定其溶出度。结果本高效液相色谱法测定盐酸曲马多的质量浓度10.173-1017.3μg/ml内呈良好的线性相关性,相关系数r=0.999 9,平均回收率为99.89%（RSD=1.12%,n=6）,溶出度符合规定。结论该方法准确、可靠、简便、易行,可作为制剂的溶出度测定方法。     

氨酚曲马多片溶出度测定

目的:建立氨酚曲马多片溶出度测定方法。方法:以0．01 mol·L-1盐酸为溶出介质,采用高效液相色谱法测定氨酚曲马多片的溶出度。结果:对乙酰氨基酚和盐酸曲马多线性范围分别为61．6-215．6μg·ml-1和8．0-28．0 μg·ml-1;平均回收率分别为99．9％,100．1％;RSD分别为0．4％,0．6％。结论:本法使两主药测定不互相干扰,可以用于氨酚曲马多片的溶出度测定。     

曲马多的药物基因组学相关研究进展

曲马多是一种中枢性非麻醉镇痛药,广泛应用于各种原因引起的急慢性中重度疼痛。曲马多的药效个体间差异大,临床常见相同剂量的曲马多在不同患者间出现镇痛不足或胃肠道不良反应的现象。近年研究表明,曲马多个体反应的差异与其药代学和药效学相关的多个基因多态性有关。本文综述了曲马多的药物基因组学研究进展,为临床开辟曲马多个体化治疗提供参考。     

盐酸曲马多含量测定方法的改进

目的：建立革除汞盐的高氯酸电位滴定法测定盐酸曲马多的含量。方法：采用Mettler DG113-SC复合电极,以冰醋酸、醋酐为溶剂,用高氯酸滴定液（0．1mol·L^-1）滴定。结果：盐酸曲马多在0．1081～0．2880g范围内线性关系良好（r=1．0000）,最低检测限为1．83mg,平均回收率为99．96％。结论：本方法操作简便快速、灵敏度高、结果准确,可用于盐酸曲马多的含量测定。