百花定喘丸中非法掺入西药成分的鉴别与含量测定

目的:检查中成药百花定喘丸中非法掺入的西药成分醋酸泼尼松及地西泮。方法:采用高效液相色谱-二极管阵列检测(HPLC-DAD)分析技术,分离和测定百花定喘丸的甲醇提取液。结果:检查3批样品均含有醋酸泼尼松和地西泮并测定其含量。结论:本法操作简便,结果准确,专属性强,适用于检测百花定喘丸中添加的醋酸泼尼松及地西泮。     

安定溶液舌下给药治疗小儿惊厥疗效观察

目的探讨安定溶液舌下给药治疗小儿惊厥的临床疗效及安全性。方法选择惊厥患儿92例,随机分为治疗组46例,舌下给药0.5mg/kg;对照组46例,直肠给药0.5mg/kg。比较两组控制惊厥显效率和总有效率及控制惊厥平均起效时间。同时观察治疗组的不良反应。结果治疗组显效率高于对照组(χ2=7.38,P=0.012),总有效率与对照组差异无统计学意义(χ2=0.548,P=0.714);治疗组平均起效时间较对照组短(t=5.42,P=0.000);治疗组除止惊后嗜睡、乏力外未见其它不良反应。结论舌下给药临床应用安全方便,止惊快速有效,值得临床推广。     

吗啡依赖大鼠海马CA1区地西泮结合抑制因子基因表达与位置偏爱的观察

目的研究地西泮结合抑制因子(DBI)在大鼠吗啡精神依赖中所起的作用。方法30只雄性Sprague-Dawley(SD)大鼠随机分为研究组20只和生理盐水对照组10只,研究组再分为依赖组及戒断3d组、戒断6d组、戒断10d组。在处死前各个时点进行条件性位置偏爱测评,处死后利用组织原位杂交技术检测DBImRNA在海马CA1区(HIPCA1)的表达,进行组间比较,并用相关分析检测吗啡依赖大鼠海马CA1区DBImRNA的表达与CPP之间的相关性。结果1.吗啡成瘾组海马CA1区DBImRNA的表达OD值为0.28±0.018,显著高于对照组的0.24±0.018(P<0.05),并在戒断的第3天达到峰值,随后出现下调。2.在戒断第1、3、6、10天,研究组海马CA1区DBImRNA的表达与CPP之间呈正相关(P<0.01)。结论1.DBImRNA在慢性吗啡处理大鼠海马CA1区的表达上调,说明DBI参与了慢性吗啡依赖生物学过程。2.海马CA1区DBImRNA的表达和CPP有密切关系,推测DBI可能在精神依赖中起重要作用。     

产程活跃期安定缩短产程临床探讨

目的:探讨产程活跃期应用安定缩短产程的临床疗效.方法:在本院住院分娩的初产妇,其产程活跃期静脉注射安定120例,同时取不用安定者120例与之对照,对两组的宫颈口扩张速度、羊水污染、胎儿宫内窘迫、新生儿窒息及剖宫产率等进行分析讨论.结果:产程活跃期静脉缓注安定可加速宫颈口扩张,缩短产程,效果肯定(P＜0.05),剖宫产率降低(P＜0.05),但同时可增加新生儿窒息(P＜0.01),并由此提出产程中应用安定的注意点.结论:产程活跃期静脉注射安定可加速宫颈口扩张,缩短产程.     

Ketamine anesthesia with or without diazepam premedication for bone marrow punctures in children with acute lymphoblastic leukemia

Ketamine is a drug widely used for analgesia and sedation of children for diagnostic and therapeutic procedures. The authors investigated in a randomized controlled clinical trial if diazepam premedication would have a beneficial effect on side effects related to ketamine anesthesia for bone marrow punctures (BMPs) in children with acute lymphoblastic leukemia (ALL). Sixteen children 4 years or older at the time of BMP were eligible. The first 2 BMPs after complete remission was obtained were studied. BMPs were performed under ketamine anesthesia (1.0-1.5 mg/kg iv), as usual. Patients were randomized to receive 1 h before the first BMP blinded, either diazepam or placebo orally and before the second BMP the other way round. Blood pressure, heart rate, and oxygen saturation were monitored, and patients were observed for signs of anxiety, pain, and other side effects. The patients were interviewed after each BMP and asked for their preference 1 week after the second BMP. Ketamine anesthesia appeared as safe and effective after diazepam premedication as after placebo premedication. From the interviews and questionnaires, it was clear that half of the children preferred diazepam premedication because of less awful dreaming and more gradual falling asleep and waking up. Diazepam premedication may be useful for selected children with ALL receiving ketamine anesthesia for BMPs.     

Anxiolytic-Like Effects of Perospirone, a Novel Serotonin-2 and Dopamine-2 Antagonist (SDA)-Type Antipsychotic Agent

We examined the anxiolytic potential of perospirone, a novel serotonin-2 and dopamine-2 antagonist (SDA)-type antipsychotic agent, and compared its effects with those of the standard anxiolytic diazepam and the conventional antipsychotic haloperidol by using conditioned defensive burying (CDB) and social interaction (SI) tests in rats. The tests were conducted 1 h after oral administration of the drug. Diazepam inhibited CDB specifically directed toward a probe previously associated with brief electric shock and increased the time spent in SI by pairs of naive rats in a brightly illuminated novel environment. Perospirone mimicked the effects of diazepam by dose dependently suppressing CDB and facilitating SI. In contrast, haloperidol failed to inhibit CDB or increase SI. Thses results suggested that, unlike the conventional antipsychotic haloperidol, perospirone exerts anxiolytic-like effects in animal models with different motivational and emotional states. A braoder efficacy of perospirone for the treatment of anxiety and related symptoms in schizophrenia is discussed.     

Maturation-related changes in tolerance development to hexobarbital after short term treatment with diazepam in the rat

Male rats at six different ages received diazepam on a 4-day treatment schedule. Cross-tolerance to hexobarbital was tested several times during withdrawal period with an anaesthesia threshold technique. Pattern of cross-tolerance was different at different ages. Thus, age and maturation of the rat is a variable which must be considered in studies of tolerance to diazepam.     

Influence of prior maze experience on behaviour and response to diazepam in the elevated plus-maze and light/dark tests of anxiety in mice

A single prior undrugged exposure to the elevated plus-maze has been reported to reduce open arm activity on retest and to attenuate/abolish the anxiolytic response to benzodiazepines at retest intervals ranging from 48 h to 14 days. The present study was designed to examine the generality of these findings by comparing the effects of prior maze experience on baseline behaviour and response to diazepam in two murine models of anxiety. Parallel experiments were conducted in which DBA/2 mice were exposed/not exposed to the plus-maze, treated daily with saline or diazepam (2–4 mg/kg daily for 8 days) and then tested on either the elevated plus-maze or in the light/dark test of exploration. Results show that, in both tests, diazepam reduced behavioural indices of anxiety in maze-naive mice only. However, interpretation of this apparent loss of diazepam efficacy is at least partially confounded by the observation that maze experience per se altered baseline behaviour in both procedures,reducing open arm activity in the plus-maze andincreasing light compartment activity in the light/dark test. The apparent elimination of an anxiolytic response to diazepam in two animal models of anxiety by prior plus-maze experience is discussed in relation to experience-related baseline shifts in behaviour.     

Comparison of Gas Chromatography and Receptor Bioassay in the Determination of Diazepam in Plasma after Conventional Tablets and Controlled Release Capsules

Abstract: Plasma levels of diazepam and its metabolites were compared after a controlled release formulation and a regular tablet. Both gas chromatographic analysis of plasma diazepam and desmethyldiazepam and radioreceptor assay of total benzodiazepine activity were used. Also the concentrations of benzodiazepine in saliva samples were analyzed by radioreceptor assay. A typical initial plasma peak was seen after the regular tablet but not after the controlled release capsule. Hence the excessive initial sedation can be avoided and the risk of abuse reduced. Desmethyldiazepam increased for about two days after a single dose of diazepam. The receptor assay correlated in general with the sum of diazepam and its desmethyl derivative. The saliva assay gave about 2.5% of the plasma total benzodiazepine which correlates well with the expected free benzodiazepine. It seems that both the plasma radioreceptor assay and the saliva assay can be used to monitor the total benzodiazepine concentration.     

The influence of haloperidol and aminooxyacetic acid on etonitazene, alcohol, diazepam and barbital consumption

Four groups of rats were given free choice between water and solutions of either 3 micrograms/ml etonitazene, 5% ethanol (v/v), 0.1 mg/ml diazepam or 3 mg/ml barbital for 10-14 days. With the exception of barbital, some rats spontaneously preferred the drug solutions to water. This preference was reduced by addition of 7 micrograms/ml haolperidol. In a forced drug fluid consumption procedure, the daily administration of 15 mg/kg i.p. of the gamma-aminobutyric acid (GABA)-transaminase blocker aminooxyacetic acid (AOAA) led to a reduction of ethanol and diazepam intake, but not of etonitazene and barbital. It is suggested that the diminished consumption of ethanol and diazepam as caused by GABA-T-inhibition may also be mediated by dopamine which seems to act indirectly, via benzodiazepine receptors and GABA neurons.