昂丹司琼对腰-硬联合麻醉剖宫产术中麻醉效果的影响

目的:观察昂丹司琼对腰-硬联合麻醉剖宫产术中麻醉效果的影响。方法:60例单胎足月产妇随机均分为试验组和对照组。试验组产妇于麻醉前30 min静脉输注6%羟乙基淀粉(130/0.4)电解质注射液500 ml,麻醉前5 min给予盐酸昂丹司琼注射液4 ml,缓慢静脉推注;对照组产妇于麻醉前30 min静脉输注6%羟乙基淀粉(130/0.4)电解质注射液500 ml,麻醉前5 min给予0.9%氯化钠注射液4 ml缓慢静脉推注。记录两组产妇开始实施麻醉穿刺前(T1)、麻醉后产妇取左侧卧位后(T2)、胎儿娩出后(T3)、手术结束时(T4)的平均动脉压(MAP)、心率(HR),新生儿Apgar评分及不良反应发生情况。结果:对照组产妇T2、T3时点MAP显著低于同组T1时点及试验组,HR显著高于同组T1时点及试验组,差异均有统计学意义(P<0.05);试验组产妇各时点MAP、HR比较,差异均无统计学意义(P>0.05)。试验组新生儿出生后1 min Apgar评分显著高于对照组,差异有统计学意义(P<0.05),两组新生儿出生后5 min Apgar评分比较,差异无统计学意义(P>0.05)。试验组产妇不良反应发生率显著低于对照组,差异有统计学意义(P<0.05)。结论:腰-硬联合麻醉剖宫产手术中应用昂丹司琼后,可有效降低恶心呕吐、低血压的发生,安全性较好。     

昂丹司琼对切口痛模型大鼠自发痛行为及脊髓背角c-Fos表达的影响

目的:研究昂丹司琼局部应用对切口痛模型大鼠自发痛行为及脊髓背角c-Fos表达的影响.方法:大鼠随机分为生理盐水对照组(n=8),利多卡因20 mg/mL组(n=8),昂丹司琼32 mg/mL组(n=8)和假手术组(单纯乙醚麻醉组)(n=8).通过三点阻滞法分别给予实验药物,15 min后建立切口痛模型,计数其后1 h内大鼠的累积痛评分,并于2 h后取大鼠相应节段脊髓标本,通过免疫组化方法检测脊髓c-Fos的表达情况.结果:与盐水对照组相比,利多卡因组和昂丹司琼组大鼠的累积痛评分均明显下降,其脊髓c-Fos表达也被明显抑制.结论:局部应用昂丹司琼对切口痛模型大鼠自发痛行为及脊髓背角c-Fos表达均有明显的抑制作用.     

昂丹司琼引起胃痉挛1例

昂丹司琼(枢复宁)是一种高选择性的5-羟色胺受体(5-HT3)拮抗剂,临床用于化疗、放疗所引起的恶心、呕吐,镇吐效果好。最近观察到用枢复宁引起胃痉挛1例。 患者女,40岁,患右乳癌伴同侧腋窝淋巴结转移,于2000年4月20日住院。入院后用盐酸多柔     

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。     

昂丹司琼对腹腔镜胆囊切除术后恶心呕吐的预防作用

目的观察静脉应用昂丹司琼对腹腔镜胆囊切除术后恶心呕吐的预防作用。方法 100例全身麻醉下行腹腔镜胆囊切除术的患者,随机分成昂丹司琼组及对照组,每组50例。昂丹司琼组给予昂丹司琼,对照组给予生理盐水。观察两组治疗效果。结果术后0~12 h恶心、呕吐发生率昂丹司琼组与对照组比较,差异有统计学意义(P<0.05);昂丹司琼组术后0~24 h恶心呕吐发生率及挽救药物用量显著低于对照组,差异有统计学意义(P<0.05)。结论麻醉诱导前静脉推注昂丹司琼显著降低了腹腔镜胆囊切除术患者术后恶心呕吐的发生率,值得推广应用。     

昂丹司琼引起过敏性休克

1例50岁肺腺癌男性患者化疗前为预防呕吐给予奥美拉唑40 mg静脉滴注,以及昂丹司琼8 mg静脉滴注.昂丹司琼滴注约15 min时,患者前胸和双臂出现皮疹.停用昂丹司琼,给予地塞米松和异丙嗪治疗.40 min后皮疹遍及全身,继之出现视物模糊、出冷汗、胸闷、乏力、脉搏弱及心音低.查体:HR 75次/min,BP 50/40 mm Hg.给予吸氧、皮下注射肾上腺素、静脉推注地塞米松及静脉滴注多巴胺治疗.患者症状缓解,5 h后生命体征平稳.     

昂丹司琼对肺癌化疗所致恶心呕吐的预防

目的：评价单剂昂丹司琼对肺癌化疗所致恶心、呕吐的预防作用。方法：选择35例肺癌化疗患者,采用自身交替对照的方法,观察单次静脉注射昂丹司琼8mg对化疗所致恶心、呕吐的预防作用。结果：单剂昂丹司琼对肺癌化疗所致恶心、呕吐的控制率分别为91．4％、94．3％;甲氧氯普胺的控制率分别为65．7％,74．3％,两者比较差异显著。结论：单剂昂丹司琼对肺癌化疗所致恶心、呕吐有明显的预防作用。     

昂丹司琼对剖宫产术中使用安列克所致恶心呕吐的预防作用

目的:研究昂丹司琼对剖宫产术中使用安列克所致恶心呕吐的预防作用.方法:选取于我院2015年10月~2016年10月期间进行剖宫产手术的产妇80例,随机分为观察组与对照组,每组40例,对照组于胎儿娩出后手术医生发现子宫收缩不佳决定使用安列克即时(在安列克使用前1min)静脉注射浓度为0.9%的生理盐水2mL,观察组静脉注射昂丹司琼4mg.比较两组使用安列克后不同时间段(5min,10min,30min)恶心呕吐发生情况.结果:对照组产妇用药后5min、10min、30min恶心呕吐发生率分别为7.5%、35.0%、60.0%,较观察组5.0%、12.5%、2.5%显著较高(P<0.05);对照组恶心呕吐程度明显高于观察组,观察组5.0%的患者恶心呕吐程度为3级较对照组的75.0%显著较低(P<0.05).结论:昂丹司琼对剖宫产术中使用安列克所致的恶心呕吐预防效果显著,有利于肠道功能的恢复,安全可靠,值得临床推广.     

不同时间点应用昂丹司琼对食管癌全麻术后恶心呕吐的影响

目的探讨不同时间点应用昂丹司琼对预防食管癌全麻术后恶心呕吐（PONV）的影响。方法选择气管插管加静脉复合全麻下行食管癌根治手术患者150例,按不同给药时间分为A组、B组、c组各50例。以双盲方式按下述方法给药：A组于麻醉诱导前予以昂丹司琼8mg静脉注射,B组于关闭胸腔前予以昂丹司琼8mg静脉注射,C组于术毕拔出气管导管后予以昂丹司琼8mg静脉注射。比较3组PONV发生情况。结果B组PONV总发生率为20．0％,低于A组的50．0％及B组的44．0％,差异均有统计学意义（P〈0．05）;但A组与B组总发生率比较差异无统计学意义（P〉0．05）。结论食管癌手术在关闭胸腔前应用昂丹司琼,可以预防PONV的发生。     

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。     

牛磺酸对东莨菪碱所致记忆获得性障碍模型小鼠的改善作用

目的观察牛磺酸对东莨菪碱所致模型小鼠学习记忆及对其脑组织M胆碱受体结合力的影响。方法将昆明小鼠随机分组,设立正常对照组,东莨菪碱模型组及阳性对照药(吡拉西坦)组,牛磺酸小剂量组(0.3g·kg-1),中剂量组(0.75g·kg-1),大剂量(1.875g·kg-1)组,分别灌胃给药,于d5,除正常对照组腹腔注射生理盐水外,其它各组注射东莨菪碱1mg·kg-1,20min后进行Morris水迷宫测试,测试5d后处死,取其脑组织进行M受体结合力测定。结果在行为学实验中,牛磺酸各剂量组游出时间与模型组相比有明显缩短(P<0.05),并可以提高模型小鼠M胆碱受体的结合力。结论牛磺酸对东莨菪碱所致模型小鼠学习记忆障碍及M受体有一定的改善作用。     

Effect of metoclopramide,ondansetron and granisetron on aldosterone secretion in man

Summary The plasma aldosterone response following the administration of drugs with antagonist and agonist activity at Serotonin _{3 and 4} (5-HT_3&4) receptors has been examined in 9 healthy male volunteers receiving the following four treatments i.v. in a randomised, cross-over sequence: ondansetron 8 mg, granisetron 3 mg, metoclopramide 20 mg, and saline 20 ml.Metoclopramide significantly increased the mean plasma aldosterone level to 196% of basal level at 5 min. It rose to 234% at 15 min and remained at more than 185% of basal level for the duration of the experiment. The response to ondansetron and granisetron did not differ significantly from placebo.If dopamine antagonism is discounted, the results suggest that metoclopramide-induced aldosterone secretion results from its agonist activity at 5-HT₄ receptors, although slow neuronal depolarization via an unidentified receptor remains a possibility. Antagonism at the 5-HT₃ receptor plays no role, as the selective antagonist, granisetron, did not elicit a significant response. It seems unlikely that the 5-HT₄ receptor is the second, low affinity binding site of ondansetron, unless it had no agonist activity at this receptor.     

Randomised controlled trial of ondansetron in smoking cessation

A double-blind, placebo controlled trial was undertaken to examine the effect of the 5-HT₃ antagonist, ondansetron .25 mg bd on cigarette withdrawal symptoms and on proportion of individuals maintaining continuous abstinence for 4 weeks in a smoking treatment programme. A total of 111 smokers were allocated to active or placebo conditions and began taking their study medication 2 weeks before the quit date. They attended the smokers clinic for weekly group treatment sessions. The results showed no evidence for less severe withdrawal symptoms or improved abstinence rates in the active medication group. They suggest that inhibiting 5-HT₃ activity is not an effective method of controlling nicotine withdrawal or helping smokers to stop.     

盐酸昂丹司琼片在健康人体的生物等效性研究

目的:研究两种盐酸昂丹司琼片在中国健康人体的生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服(8 mg)盐酸昂丹司琼试验制剂与参比制剂,采用液-质联用法测定血浆中昂丹司琼的血药浓度,应用SPSS 13.0统计软件进行统计分析。结果:试验制剂与参比制剂中昂丹司琼的主要药动学参数,Cmax分别为(33±8)和(32±8)μg/L,tmax分别为(1.5±0.3)和(1.5±0.4)h,AUC0~24分别为(176±67)和(168±58)μg.h.L-1,AUC0~∞分别为(188±70)和(182±63)μg.h.L-1。试验制剂对参比制剂的相对生物利用度为(103.2±10.0)%。结论:两种盐酸昂丹司琼片剂具有生物等效性。     

Efficacy of dronabinol alone and in combination with ondansetron versus ondansetron alone for delayed chemotherapy-induced nausea and vomiting*

ABSTRACT

Objective: To compare the efficacy and tolerability of dronabinol, ondansetron, or the combination for delayed chemotherapy-induced nausea and vomiting (CINV) in a 5-day, double-blind, placebo-controlled study.

Research design and methods: Patients receiving moderately to highly emetogenic chemotherapy received dexamethasone (20?mg PO), ondansetron (16?mg IV) and either placebo or dronabinol (2.5?mg) prechemotherapy on day 1. Patients randomized to active treatment (dronabinol and/or ondansetron) also received dronabinol (2.5?mg) after chemotherapy on day 1. On day 2, fixed doses of placebo, dronabinol (10?mg), ondansetron (16?mg), or combination therapy were administered. On days 3–5, patients received placebo, flexible doses of dronabinol (10–20?mg), ondansetron (8–16?mg), or dronabinol and ondansetron (10–20?mg dronabinol, 8–16?mg ondansetron).

Main outcome measures: Total response (TR = nausea intensity <?5?mm on visual analog scale, no vomiting/retching, no rescue antiemetic), nausea (occurrence and intensity) and vomiting/retching episodes.

Results: Sixty-four patients were randomized; 61 analyzed for efficacy. TR was similar with dronabinol (54%), ondansetron (58%), and combination therapy (47%) versus placebo (20%). Nausea absence was significantly greater in active treatment groups (dronabinol, 71%; ondansetron, 64%; combination therapy, 53%) versus placebo (15%; p < 0.05 vs. placebo for all). Nausea intensity and vomiting/retching were lowest in patients treated with dronabinol. Active treatments were well tolerated. The low number of patients due to slow enrollment limits the interpretation of these data.

Conclusions: Dronabinol or ondansetron was similarly effective for the treatment of CINV. Combination therapy with dronabinol and ondansetron was not more effective than either agent alone. Active treatments were well tolerated.     

一种中药提取物的制备及对东莨菪碱模型小鼠学习记忆能力的影响

目的 优选自制中药的最佳提取工艺,并考察采用最佳提取工艺得到的提取物对东莨菪碱致记忆障碍模型小鼠学习记忆的影响.方法 以出膏率为评价指标,采用L9(34) 正交试验,对提取溶剂、溶剂倍数、浸泡时间及提取时间4个因素进行考察;将昆明种小鼠随机分为正常对照组、东莨菪碱模型组、脑复康组(阳性对照药,400 mg·kg-1)、中药提取物高剂量组(2.0 g·kg-1)、中剂量组(1.0 g·kg-1)、低剂量组(0.5 g·kg-1)共6组,灌胃给药4周后,除正常对照组腹腔注射生理盐水外,其他各组腹腔注射东莨菪碱3 mg·kg-1,20 min后进行Morris水迷宫测试.结果 自制中药最佳提取工艺为加入12倍量的50% 乙醇溶液,浸泡90 min后,加热回流提取3次,每次提取2 h;最佳提取工艺得到的提取物灌胃给药能够提高东莨菪碱模型小鼠学习记忆能力,缩短Morris水迷宫游泳时间(P<0.05).结论 优选出的提取工艺设计合理、结果可靠,该工艺得到的自制中药提取物可以改善东莨菪碱模型小鼠的记忆障碍.     

不同厂家盐酸昂丹司琼片的溶出度考察

目的对3个不同厂家所生产的盐酸昂丹司琼片体外溶出度进行了考察,为临床用药提供参考。方法根据《中华人民共和国药典》(2010版)中盐酸昂丹司琼片的溶出度实验项下要求,采用浆法测定溶出度,紫外-可见分光光度法测定吸光度,对照品法计算溶液中盐酸昂丹司琼浓度。利用Excel软件计算累积溶出百分率及溶出参数,并进行比较分析。结果 3个厂家盐酸昂丹司琼片的体外溶出度均符合药典规定,但各自间存在一定差异。结论不同厂家盐酸昂丹司琼片的溶出情况存在一定差异。     

奥丹西酮在原发性肝癌患者的药物动力学

目的观察奥丹西酮在原发性肝癌患者体内的药物动力学特性。方法8名接受顺铂 5 -氟尿嘧啶化疗的原发性肝癌患者单次和多次口服16mg 奥丹西酮后 ,应用反相高效液相色谱法测定血浆药物浓度 ,并用PKBP -N1程序在计算机上拟合。结果奥丹西酮表现为二房室模型,其单剂量和多剂量口服主要药动学参数分别为 :T1/2β 为4.3±0.5h和5.7±0.7h(P<0.01),Cmax 为42.6±3.8μg/L和49.2±2.3μg/L(P<0.05),Tmax 为1.8±0.2h和1.8±0.1h,AUC0～∞为643.2±84.7μg/h·L和833.4±96.7μg/L·h(P<0.01)。结论原发性肝癌患者多次口服奥丹西酮后与单次口服相比 ,体内有蓄积现象 ,消除能力下降 ,生物利用度升高     

Effects of ondansetron administration on opioid withdrawal syndrome observed in rats

This study tested whether a 5-HT₃ receptor antagonist could reverse the signs of precipitated opioid withdrawal. Rats were treated with either saline or morphine for 4 days. After the four days, half of the rats in each group received naloxone and half received saline. Each animal also received one of four doses of ondansetron (0, 1, 2 and 4 mg/kg i.p.). Administration of ondansetron to rats receiving naloxone after chronic morphine decreased the intensity of withdrawal signs such as increased defecation, jumping and wet-dog shakes, elevated the nociceptive threshold values which were decreased by precipitated withdrawal, but produced no change in urination, rectal temperature or salivation. The effects exhibited by ondansetron administration may be explained through interference of its 5-HT₃ receptor antagonist activity with serotoninergic mechanisms involved in the regulation of these withdrawal symptoms. The use of this drug is thus suggested as a possible treatment of opioid withdrawal signs in heroin addicts.     

Concentration of ondansetron in cerebrospinal fluid following oral dosing in volunteers

This study measured the concentrations of ondansetron in plasma and cerebrospinal fluid (CSF) in six volunteers after oral dosing to steady state. Ondansetron concentrations ranged from 39.5–147 ng ml^–1 in plasma and from 2.6–15.4 ng ml^–1 in CSF. There was good correlation between plasma and CSF concentrations (r=0.89,p=0.017). CSF concentrations were less than 15% of plasma concentrations in all cases, indicating that the rate of penetration of the blood brain barrier by ondansetron is low.