Ondansetron for paediatric uraemic pruritus: a case report

Pruritus, secondary to chronic renal failure, can be an extremely distressing symptom. A 15-year-old girl, in end-stage renal disease, presented with pruritus that did not improve on starting peritoneal dialysis. Despite normalising the calcium, phosphate and parathyroid levels, pruritus worsened and showed no response to antihistamines. She was commenced on ondansetron and showed dramatic improvement. Severe uraemic pruritus is rare, but distressing in children and can improve with ondansetron.     

The effect of Ondansetron on memory in schizophrenic patients

It has been well established that patients with schizophrenia have impaired cognitive function on neuropsychological tasks related to memory. Previous studies also suggest serotonin's central role in memory. This double-blind crossover study aimed to explore the effect of Ondansetron, a selective serotonin 3 receptor (5-HT(3)) antagonist, on a variety of memory tasks in schizophrenic patients. Clozapine-treated schizophrenic patients in remission (N=21) were randomly treated with Ondansetron or placebo and then evaluated at three consecutive points. These evaluations included clinical measures (including Positive and Negative Syndrome Scale for Schizophrenia, Clinical Global Impression and Extrapyramidal Symptoms Rating Scale) and neuropsychological measures (including Digit Span, Paired Association, Rey-Osterich Complex Figure Test, Digit Symbol and the Rivermead Behavioral Memory Tests). Ondansetron, when compared with placebo, did not affect the above clinical measures and most of the neuropsychological tests. Short-term administration of Ondansetron, however, was associated with significantly improved visuo-spatial memory as measured by the Rey-Osterich Complex Figure Test. These preliminary results suggest Ondansetron's possible role in enhancement of memory function in schizophrenia.     

盐酸恩丹西酮乳酸羟基乙酸共聚物微球中药物的含量测定

目的:建立测定盐酸恩丹西酮乳酸羟基乙酸共聚物微球含量的方法.方法:采用二氯甲烷溶解微球后,再以水提取主药,用紫外分光光度法测定药物的含量.结果:盐酸恩丹西酮在2～20μg·ml-1的范围内,浓度与吸收度的线性关系良好,平均回收率为98.76%±0.64%,RSD为1.82%.结论:该方法操作简单、可靠,可用于快速测定微球中药物的含量.     

昂丹司琼联合地塞米松预防妇科腹腔镜术后恶心呕吐的疗效观察

目的 评价昂丹司琼联合地塞米松预防妇科腹腔镜术后恶心呕吐的临床疗效。方法 选择90例ASAⅠ～Ⅱ级行妇科腹腔镜手术的病人，随机将病人分为三组，在手术结束时分别静注昂丹司琼8mg和地塞米松10mg（A组，n=30），昂丹司琼8mg（B组，n=30）、生理盐水（对照组，C组，n=30）。结果 在术后8小时内和9-24小时内恶心呕吐发生率A组（16．7％、10．0％）和B组（20．0％、33．3％）明显低于C组（63．3％、60．0％）（P〈0．05），A组在术后8小时内恶心呕吐发生率与B组比较无显著性差异（P〈0.05），但在术后9-24小时内恶心呕吐发生率明显低于B组（10．0％vs33.3％）（P〈0．05）。结论 昂丹司琼联合地塞米松可显著减少妇科腹腔术后恶心呕吐发生率，而且其作用维持时间要长于单纯应用昂丹司琼。     

盐酸恩丹西酮缓释胶囊的制备及质量控制

目的:制备盐酸恩丹西酮缓释胶囊并建立其质量控制方法。方法:制备盐酸恩丹西酮缓释胶囊;测定盐酸恩丹西酮释放度,进行释放机制及影响因素研究;用高效液相色谱法测定主药盐酸恩丹西酮的含量。结果:制得盐酸恩丹西酮胶囊体外释放曲线符合一级动力学方程和Higuchi方程;盐酸恩丹西酮检测浓度在9.93～79.44μg/ml范围内与峰面积积分值线性关系良好,平均回收率为100.15%(RSD=0.44%)。结论:该制剂具有明显的缓释作用,制备工艺简单,值得推广。     

Ondansetron reduces mood disturbance among biologically predisposed, alcohol-dependent individuals

BACKGROUND: Early-onset alcoholics (EOA) differ from late-onset alcoholics (LOA) by developing problem drinking during youth, experiencing severe behavioral problems, having a familial disease history, and possessing a tendency toward subsyndromal mood disturbance, including symptoms of depression, anxiety, and hostility. Subsyndromal mood disturbance is, therefore, an important component of the early-onset syndrome and may be mediated by serotonin dysfunction. Therefore, the serotonin-3 antagonist ondansetron, which has been shown to be effective at improving drinking outcomes and promoting abstinence among EOA, presumably by ameliorating serotonin dysfunction, also may exert its beneficial effects by alleviating mood disturbance among EOA. METHODS: After one lead-in week of single-blind placebo administration, subjects underwent 11 weeks of double-blind outpatient treatment using a 2 x 4 factorial design that examined age of onset (EOA versus LOA) and medication dose (placebo, or ondansetron 1, 4, or 16 microg/kg twice daily) combined with weekly standardized group cognitive-behavioral therapy. The placebo lead-in week was used to adjust for study entrance effects but not for excluding subjects. Assessments of mood were performed by using the overall score and subscales of the Profile of Mood States both at screening and at weekly intervals during the study. RESULTS: Subsyndromal mood disturbance was shown to be an important component of early-onset alcoholism. Ondansetron (16 microg/kg twice daily) showed greater therapeutic efficacy at alleviating symptoms of overall mood disturbance, fatigue, vigor, confusion/bewilderment, and depression among EOA compared with LOA. EOA-associated improvements in mood disturbance seemed to be independent of drinking behavior. CONCLUSIONS: Ondansetron has been shown to be an effective treatment for early-onset alcoholism. Ondansetron's ability to improve symptoms of depression, anxiety, and hostility among EOA may make an additional contribution to its therapeutic effect. Mechanistic studies are needed to delineate more clearly the relationship between serotonin dysfunction and pathophysiology among various subtypes of alcohol-dependent individuals.     

Behavioural and pharmacological characterisation of the elevated “zero-maze” as an animal model of anxiety

The elevated zero-maze is a modification of the elevated plus-maze model of anxiety in rats which incorporates both traditional and novel ethological measures in the analysis of drug effects. The novel design comprises an elevated annular platform with two opposite enclosed quadrants and two open, removing any ambiguity in interpretation of time spent on the central square of the traditional design and allowing uninterrupted exploration. Using this model, the reference benzodiazepine anxiolytics, diazepam (0.125–0.5 mg/kg) and chlordiazepoxide (0.5–2.0 mg/kg) significantly increased the percentage of time spent in the open quadrants (% TO) and the frequency of head dips over the edge of the platform (HDIPS), and reduced the frequency of stretched attend postures (SAP) from the closed to open quadrants. In contrast, the anxiogenic drugm-chlorophenyl-piperazine (mCPP; 0.25–1.0 mg/kg) induced the opposite effects, decreasing %TO and HDIPS, and increasing SAP. The 5-HT_1A receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT; 0.001–0.1 mg/kg) had no effects on either %TO or HDIPS, but did decrease SAP at 0.01 mg/kg although not at higher or lower doses. Similarly, the 5-HT₃ receptor antagonist, ondansetron (0.0001–1.0 mg/kg) decreased SAP and increased %TO at 0.01 mg/kg, but not at other doses. The present data suggest that a combination of the novel zero-maze design and a detailed ethological analysis provides a sensitive model for the detection of anxiolytic/anxiogenic drug action.     

昂丹司琼的合成工艺改进

目的改进昂丹司琼的合成工艺。方法以1，2，3，9-四氢-4H-咔唑-4-酮经N-甲基化、Mannich反应和缩合得止吐药昂丹司琼。结果取得较佳的工艺条件，总收率为43．9％。结论该方法易于工业化生产。     

Treatment of acute gouty arthritis with the 5-hydroxytryptamine antagonist ondansetron

We report on a 28-year-old man with hematemesis, renal dysfunction, and arterial hypertension who suffered from an acute gouty attack presenting as podagra. Because of the accompanying symptoms conventional treatment of the gouty attack with colchicine or nonsteroidal anti-inflammatory drugs was contraindicated. We treated the pain of acute arthritis with the specific 5-hydroxytryptamine subtype 3 receptor antagonist ondansetron. Within 30 min after intravenous injection of this drug a substantial degree of pain relief had occurred. Unwanted side effects due to treatment were not observed. It is suggested that the 5-hydroxytryptamine released during a gouty attack induces pain via activation of 5-hydroxytryptamine subtype 3 receptors on nociceptive afferent nerve fibers. 5-Hydroxytryptamine subtype 3 receptor antagonists may therefore be a novel class of drugs for the effective treatment of acute gouty attacks when conventional treatment is contraindicated.Abbreviation 5-HT 5-hydroxytryptamine Correspondence to: H. Schworer     

恩丹西酮预防全麻上腹部手术后恶心呕吐的临床研究

目的：探讨静脉注射恩丹西酮的时机和剂量对吸静复合全麻上腹部手术患者术后心呕吐的预防效果。方法：150例ASAⅠ-Ⅲ级成人患者随机分成五组。A组：麻醉诱导前静脉注射恩丹西酮4mg,B组：麻醉诱导前静脉注射恩丹酮8mg,C组：术毕静脉注射恩丹西酮4mg,D组：术后静脉注射恩丹西酮8mg,E组不用恩丹西酮。结果：A、B、C、D、E组患者术后恶心 呕吐发生率分别为50．0％,40．0％,53．3％,16．7％,56．7％（P＜0．01）。结论：术毕静脉注射恩丹西酮8mg更能有效预防全麻上腹术后恶心呕吐。