High Resolution Determination of Ondansetron in Human Plasma by HPLC and Pharmacokinetics of Orally Disintegrating Tablets

Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 ran with granisetron as an internal standard. Pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng· mL^-1. The recovery was about 85 % or over for ondan setron and about 90% for internal standard. Linearity was good within the concentration range of 0.5 - 50 ng·mL^-1 with r^2 ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88% -5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7% ±4.4%, 102.2% ± 1.1%, and99.51% ±2.34%, respectively. Pharmacokinetic parameters of AUCo-t, AUCo-∞ , Cmax, Tmax, and T1/2 were 230.2 ± 78.0 ng·h·L^-1 , 265.2± 101.5 ng·h·mL^-1, 35.67 ± 8.94 ng·mL^-l, 1.51 ±0.79 h, and 5.00± 1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.

Ondansetron预防眼科全麻术后恶心、呕吐的临床观察

Ondansetron是一种新型的强效、具有高度选择性的5-HT3受体拮抗剂，已广泛用于癌症病人化疗所致的恶心、呕吐的预防和治疗。最近有研究表明Ondansetron对术后恶心、呕吐有预防和治疗效果。我院于2001年1～4月对眼科全麻手术病人用或不用Ondansetron的术后恶心、呕吐的发病情况进行了双盲法比较观察，以探讨Ondansetron预防和治疗术后恶心、呕吐的效果。……

专属性5—HT_3受体拮抗剂—Ondansetron的药理学与临床应用

Ondansetron(商品名:枢复宁,Zofran)的化学名为1、2、3、9,—四氢—9—甲基—3—〔(2—甲基—1H—眯唑基—1—)甲基〕—4H—咔唑酮,是第一个用于临床的专属性5—HT_3受体拮抗剂,是预防和治疗由化疗药物引起的恶心和呕吐的安全有效药物,该药由英国葛兰素药厂开发,并于1991年上市,我国已批准进口,但价格昂贵,为了减轻癌症患者的痛苦和降低治疗费用,国内齐鲁制药厂与中国医科院药物所共同研制和生产了Ondansetron,现已获得卫生部颁发的新药证书和试生产文号。

Postoperative Nausea and Vomiting Prophylaxis with Ondansetron in Diagnostic Gynecologic Laparoscopy: Preemptive versus Preventive Method

Background and Objective: Post-operative nausea and vomiting (PONV) is a common adverse effect of the anesthesia in laparoscopic surgery. Ondansetron has been used for prevention and treatment of the PONV. The purpose of the present study was to compare the effects of preemptive and preventive intravenous ondansetron on PONV in patients undergoing diagnostic gynecologic laparoscopy. Materials & Methods: In a randomized double-blind clinical trial, 80 women candidate of diagnostic laparoscopy, were enrolled to study in two preemptive or preventive groups (n = 40). Ondansetron 4 mg IV was administered 5 min before anesthesia induction or 5 min before extubation in preemptive or preventive groups, respectively. The frequency and severity of the PONV were compared at post-anesthetic care unit (PACU), 3th, 6th and 24th postoperatively in two groups. Also the first time of need for the antiemetic drug was studied. Results: Demographic data were similar but duration of anesthesia was shorter in preventive group. The PONV rate was similar in two groups [(37.5% and 32.5% in preemptive and preventive groups, respectively (P = 0.815)]. In preemptive group it was more intense at PACU and 24 hours after surgery (P-value <0.05) and rate of vomiting was high (11 vs. 3, P-value 0.037). The first request for antiemetic drug was earlier and the antiemetic consumption dose (P-value <0.05), recovery and hospital stay times were high in preemptive group (P-value = 0.001). Conclusion: Preventive ondansetron is more effective than preemptive form, in reducing the severity of PONV but not rate of the PONV in diagnostic gynecologic laparoscopy.

Ondansetron and Hypothermia Induced Cardiac Arrest in a 97-Year-Old Woman: A Case Report

Background:Ondansetron and hypothermia are both known to induce bradycardia or QT interval prolongation,thus placing affected patients at risk of cardiac arrest.Case Report:Herein,we report the case of a 97-year-old woman who initially presented with confusion and hypothermia,and experienced severe bradycardia and asystolic cardiac arrest after a 4 mg intravenous ondansetron bolus injection.Conclusion:Ondansetron is associated with bradycardia and QTc prolongation,both of which might be further exacerbated by hypothermia.Clinicians should be aware that administering ondansetron in patients with hypothermia might further increase the risk of adverse cardiac events and eventual cardiac arrest.

A Randomized Controlled Trial Comparing the Efficacy of P6 Acupuncture Plus Ondansetron versus Ondansetron or P6 Acupuncture in the Prevention of Nausea and Vomiting after Bupivacaine-Morphine Spinal Anesthesia

Objective: To compare P6 acupuncture plus ondansetron with either ondansetron or P6 acupuncture in the prevention of postoperative nausea and vomiting (PONV) in patients submitted to spinal anesthesia. Methods: A randomized controlled trial was performed with 90 patients undergoing orthopedic surgery under spinal anesthesia with bupivacaine, 15 to 17.5 mg, and morphine, 100 μg. They were assigned to one of the three groups: Group Ondansetron (n = 30), patients were given ondansetron, 8 mg intravenously, before spinal block was performed;Group P6 acupuncture (n = 30), patients were subjected to bilateral electrical stimulation of P6 acupoint for 30 minutes before anesthesia;and Group P6 acupuncture plus ondansetron (n = 30), the exact combination of the groups Ondansetron and P6 acupuncture. Results: In the post anesthesia care unit, the incidence of nausea and vomiting ranged from 13.3% to 26.7% and from 6.7% to 13.3%, respectively, with no significant differences among groups (p > 0.05). Ondansetron group had the highest incidence of nausea (73.3%) (p < 0.001) and vomiting (43.3%) (p < 0.001) at the ward from 0 to 24 hours, followed by P6 acupuncture (33.3% and 26.7%) and P6 acupuncture plus ondansetron groups (16.0% and 0%). Conclusion: Preoperative stimulation of P6 acupoint in combination with ondansetron has higher efficacy than either P6 acupoint stimulation or the administration of ondansetron on the prevention of PONV in patients submitted to bupivacaine-morphine spinal anesthesia.

Repeated generalized seizures shortly after single intramuscular dose is an additional reasonable cause to restrict the use of ondansetron: A case report

Background: Ondansetron, a 5-hydroxytryptamine (5-HT) receptor antagonist, is generally regarded as a safe and well tolerated antiemetic. Meanwhile, some reports mentioned that it is a probable cause of single generalized seizures after intravenous administration. Our report may be the first to indicate repeated generalized seizures after intramuscular therapeutic dose of ondansetron. Methods and Results: We report a 24-year-old female with nausea and vomiting related to gastritis that experienced repeated ondansetron-induced seizures shortly after a single intramuscular therapeutic dose. Two minutes after intramuscular injection of 4 mg ondansetron, our patient developed the first generalized seizure. Within the following two hours, seizures occurred two more times. In the emergency department, the patient developed a fourth, but weaker and shorter, generalized seizure. The patient was not hypoglycemic, but her blood hemoglobin and serum electrolytes were below normal. A few hours later, the patient was discharged. The dramatic onset of the seizures, as well as the complete recovery and absence of any neurological sequel in our patient, indicated that it was probably related to ondansetron. Conclusion: Patients should be informed about the potential side effects of ondansetron especially the life-threatening repeated generalized seizures, and clinicians should restrict its use to hospitalized patients.

Palonosetron versus Ondansetron as Prophylaxis against Postoperative Nausea and Vomiting (PONV) after Laparoscopic Sleeve Gastrectomy: A Randomized Controlled Trial

Introduction: Postoperative nausea and vomiting (PONV) are prevalent symptoms after laparoscopic surgeries with an incidence rate of (54% - 79%) in bariatric procedures. Despite its popularity, limited studies assessed the effect of antiemetics for PONV prophylaxis after laparoscopic sleeve gastrectomy (LSG). The aim of this trail is to compare the effectiveness of a single pre-induction intravenous dose of Palonosetron versus Ondansetron for prophylaxis of PONV, 24 hours after LSG. Subjects and Methods: This prospective randomized controlled double-blind parallel-group study was conducted from May till December 2019. Recruited patients were consented and randomized using a closed envelop method into two groups with fifty patients each. The total number of nausea and vomiting attacks in the 24 hours postoperatively was considered as a primary end point. The secondary end points were the frequency of nausea, retching and vomiting attacks in the 24 hours post-surgery. The severity of nausea was evaluated using a 10 cm visual analogue scale (VAS). Results: This RCT included 100 patients divided into 2 groups of 50 patients each. Patients received either 75 mcg Palonosetron (Group I) or Ondansetron 4 mg (group II). Group I had statistically significant fewer episodes of nausea, retching and vomiting in the first 4 hours (P = 0.022) and from 4 to 12 hours (P = 0.024) but not after 12 hours post LSG. Total episodes of nausea, retching and vomiting in 24 hours postoperative were significantly less in group I (P = 0.021). Conclusion: A single dose of intravenous 75 mcg Palonosetron is superior to Ondansetron 4 mg in preventing PONV for patients after LSG.

ONDANSETRON对防治介入化疗引起恶心呕吐的作用

动脉插管灌注化疗治疗肿瘤中,化疗药物引起的毒副作用,虽比全身化疗轻,但不宜忽视,尤其是消化道反应(恶心、呕吐),可在治疗中或以后出现。一直是医生较大的困扰,而ondansetron(枢复宁)的应用,则对克服呕吐等带来了希望,就此笔者以84例动脉灌注化疗治疗肿瘤应用枢复宁的情况作一报道。

5HT_3受体拮抗剂的止吐作用:ICS205-930和Ondansetron的临床研究

恶心和呕吐是肿瘤化疗中最令人头痛的副作用,三十年前发现的氮芥类是细胞毒药物中一种最严重的致吐剂,顺铂、蒽环类抗生素和其它烷化剂,虽增强了肿瘤化疗效果,但也加剧了呕吐作用,有时化疗所致的恶心和呕吐严重到不得不推迟甚至拒绝治疗的程度。胃复安(Metoclopramide)是现用的有效止吐剂,但仅在大剂量时才能减轻呕吐,此时常导致锥体外副作用,如牙关紧闭、斜颈、面部痉挛、角弓反张、眼球盲动、坐立不安等。5HT_3受体拮抗剂能抑制细胞毒素和X射线所引起的呕吐,又不产生锥体外副作用,是一种很有希望的止吐药物。目前临床上至少有五种5HT_3受体拮抗剂,如ICS205-930、Granisetron(BRL43694)、Ondansetron(GR38032F)、Batanopride(BMY-25801)、Zacopride。

地塞米松、昂丹司琼预处理联合异丙嗪预防和治疗剖宫产术中恶心呕吐的效果

目的观察地塞米松、昂丹司琼预处理联合异丙嗪预防和治疗剖宫产术中恶心呕吐的效果。方法选择2022年5月至9月在北部战区总医院接受子宫下段剖宫产术的100例产妇作为研究对象,按照随机数字表法将其分为观察组和对照组,每组各50例。对照组:胎儿娩出后,给予产妇静注昂丹司琼8 mg;观察组:术前给予地塞米松8 mg+昂丹司琼8 mg,胎儿娩出后,给予产妇静注异丙嗪12.5 mg。比较两组患者术中应用卡前列素甲酯栓后5 min(T_(1))、6~15 min(T_(2))、16~30 min(T_(3))的恶心呕吐的发生率。结果观察组患者T_(1)时的恶心呕吐发生率略低于对照组,但差异无统计学意义(P>0.05)。观察组患者T_(2)和T_(3)时的恶心呕吐发生率较对照组明显降低,且差异有统计学意义(P<0.05)。结论地塞米松、昂丹司琼预处理联合异丙嗪预防和治疗剖宫产术中恶心呕吐的效果确切,值得临床进一步推广应用。

隔物灸辅助昂丹司琼预防淋巴瘤化疗相关恶心、呕吐的效果

目的 探讨隔物灸辅助昂丹司琼对淋巴瘤化疗相关恶心、呕吐的预防效果。方法 选取2019年1月至2022年7月在台州市中心医院(台州学院附属医院)治疗的淋巴瘤化疗患者共计112例,按照随机数字表法将其分成研究组和对照组,每组56例。对照组给予昂丹司琼治疗,研究组给予隔物灸辅助昂丹司琼治疗。比较两组化疗结束后7 d恶心、呕吐发生率、症状积分、生活质量。结果 研究组恶心、呕吐发生率低于对照组,差异有统计学意义(P<0.05)。研究组恶心、呕吐积分低于对照组,差异有统计学意义(P<0.05)。研究组躯体功能、认知功能、社会功能、情绪功能评分高于对照组,差异有统计学意义(P<0.05)。结论 隔物灸辅助昂丹司琼应用于淋巴瘤化疗患者中,可提高恶心、呕吐预防效果,缓解恶心、呕吐症状,提高生活质量。

昂丹司琼制剂安全性风险分析

目的 分析昂丹司琼制剂的安全性风险,为临床合理用药提供参考。方法 对我国药品不良反应监测数据库(2004年1月1日至2022年9月30日)、世界卫生组织(WHO)药品不良反应监测数据库(建库至2022年10月31日)以及其他国内外数据库(建库至2023年12月31日)的不良反应报告以及国内外风险控制措施等相关资料进行整理与分析。结果 昂丹司琼严重不良反应报告中,过敏性休克、呼吸困难、肝功能损害不良反应突出;在孕期使用昂丹司琼有导致胎儿唇腭裂的风险,产妇若在分娩前后使用本品,应暂停哺乳。结论 医疗机构需关注昂丹司琼制剂的致畸风险,在孕妇中使用应权衡利弊。同时,药品上市许可持有人应及时完善产品说明书,加强和医疗机构的风险沟通,促进药品的合理使用。

昂丹司琼联合地塞米松治疗恶性肿瘤化疗后恶心呕吐的临床效果分析

目的比较恶性肿瘤化疗后恶心呕吐患者应用昂丹司琼联合地塞米松与昂丹司琼单药治疗的临床效果。方法方便选取2020年1月—2023年9月黔西南布依族苗族自治州人民医院收治的88例行化疗后恶心呕吐患者作为研究对象,根据治疗方案的不同分为研究组(44例)及对照组(44例)。对照组予以昂丹司琼单药治疗,研究组在对照组治疗基础上联合地塞米松。对比两组临床疗效、急性及延迟性恶心和呕吐控制率、不良反应发生情况。结果对照组治疗总有效率为63.64%(28/44),低于研究组的84.09%(37/44),差异有统计学意义(χ^(2)=4.768,P<0.05)。研究组急性恶心和呕吐控制率均高于对照组,差异有统计学意义(P均<0.05);两组延迟性恶心和呕吐控制率、不良反应总发生率对比,差异无统计学意义(P均>0.05)。结论昂斯丹琼联合地塞米松在恶性肿瘤化疗后恶心呕吐患者中应用效果显著,可有效防治化疗后的急性与延迟性恶心及呕吐症状,安全可靠,具有一定的临床价值意义。

昂丹司琼对降低剖宫产术后镇痛恶心呕吐及提升生活质量的研究

目的探究使用昂丹司琼降低剖宫产术后镇痛恶心呕吐及提升生活质量的效果。方法回顾性选取2022年1月—2023年6月广西壮族自治区桂东人民医院收治的100例剖宫产产妇的临床资料,根据预防性使用止吐药物的不同分成两组,其中A组65例(昂丹司琼4 mg+地塞米松5 mg),B组35例(地塞米松5 mg),对比两组术后恶心呕吐发生率、舒适度评分和生活质量评分。结果A组术后恶心呕吐发生率为6.15%,显著低于B组的22.86%,差异有统计学意义(χ^(2)=11.398,P<0.05);A组舒适度评分和生活质量评分显著高于B组,差异有统计学意义(P均<0.05)。结论预防性使用昂丹司琼能有效预防剖宫产术后镇痛恶心呕吐的发生,有助于提高患者舒适度和生活质量。

艾盐包中脘穴热熨联合盐酸昂丹司琼片预防血液病化疗相关性恶心呕吐临床研究

目的:探究艾盐包中脘穴热熨联合盐酸昂丹司琼片预防血液病化疗相关性恶心呕吐(CINV)的临床效果。方法:选取接受化疗的108例血液病CINV患者为研究对象,按随机数字表法分为对照组和研究组各54例。对照组给予盐酸昂丹司琼片治疗,研究组给予艾盐包中脘穴热熨联合盐酸昂丹司琼片治疗。比较2组治疗后临床疗效、中医证候评分、恶心呕吐程度分级、生活功能指数量表(FLIE)评分及不良反应发生率。结果:治疗后,研究组总有效率为96.30%,对照组为83.33%,2组比较,差异有统计学意义(P<0.05)。研究组恶心呕吐程度分级改善优于对照组,差异有统计学意义(P<0.05)。治疗后,研究组嗳气反酸、食欲不振、疲乏无力等中医证候评分均低于对照组,差异有统计学意义(P<0.05)。治疗后第5天、第21天,研究组FLIE评分均高于对照组(P<0.05)。治疗期间,研究组不良反应发生率为1.85%,对照组为12.96%,2组比较,差异有统计学意义(P<0.05)。结论:艾盐包中脘穴热熨联合止吐药治疗血液病患者CINV疗效显著,可有效改善中医证候,减轻恶心呕吐反应,提高生活质量,且安全性较高。

一种新型呕吐动物模型——水貂

目的 用水貂建立一种新型呕吐动物模型。方法 将水貂随机分组 ,给予 3种经典致呕剂顺铂、阿朴吗啡、硫酸铜及X射线全身照射 ,测定致吐反应和抗呕吐药的抗呕吐反应 ,最后取水貂肠管进行 5 HT免疫组化检测。结果 顺铂 ( 7 5mg·kg- 1 ,ip)、阿朴吗啡 ( 1 6mg·kg- 1 ,sc)和硫酸铜 ( 40mg·kg- 1 ,ig) 3种致呕剂均使水貂发生恶心、干呕和呕吐 ,顺铂引起水貂呕吐的阈值剂量为 5mg·kg- 1 。昂丹司琼和甲氧氯普胺可抑制顺铂和阿朴吗啡所致的干呕、呕吐。 5 HT免疫组化结果提示 ,肠道EC细胞 5 HT释放参与呕吐的发生机制。结论 水貂可作为一种新型呕吐模型 。

托烷司琼治疗腹部手术后恶心、呕吐的多中心随机对照研究

目的:评价iv单剂量(2 mg)托烷司琼对全身麻醉下的腹部手术后病人出现的恶心和(或)呕吐症状的疗效。方法:采用前瞻、随机、对照、平行和多中心的实验设计,患者共64例,全麻术后神智清醒、出现中度以上的恶心症状和(或)呕吐,立即通过iv托烷司琼2 mg(试验组)或昂但司琼4 mg(对照组)观察用药后24 h内,呕吐和恶心程度的变化,比较两组之间的差别。结果:完成研究61例,淘汰3例,淘汰率为4.7％;托烷司琼和昂但司琼均能显著缓解全麻术后发生的呕吐和恶心症状,其呕吐和恶心平均停止时间、用药后24 h发生呕吐病例数和呕吐病人平均呕吐次数,两组比较结果相似,研究者和病人自身评价,两种药物的疗效相似(P>0.05)。结论:托烷司琼单剂量(2 mg)对全身麻醉外科腹部手术后病人发生的呕吐和(或)恶心症状有较好的疗效。

国产恩丹西酮预防化疗引起恶心呕吐80例临床观察

采用随机对照法观察了恩丹西酮对８０例顺铂及非顺铂类化疗药的止吐作用，化疗第１周期用思丹西酮或胃复安，第２周期交换。结果显示，恩丹西酮对控制急性呕吐的有效率为９１．３％，而胃复安仅为５８．８％（ｐ＜０．０１）；其对非顺铂类的止吐作用，前２天优于顺铂（Ｐ＜０．０５）；它对迟发性呕吐的疗效也优于胃复安。本研究认为，恩丹西酮控制顺铂及非顺铂类化疗引起的恶心呕吐均有良好的疗效，副作用少。

氟哌啶与枢复宁减少术后PCA恶心呕吐的临床观察

８０例全麻下择期手术的病人，随机、双盲分为四组，ＰＣＡ用药均为吗啡（２ｍｇ／ｍｌ）。Ⅰ组为对照组；Ⅱ组为吗啡药液中加入小剂量氟哌啶（０．０５ｍｇ／ｍｌ）；Ⅲ组为吗啡药液中加入大剂量氟哌啶（０．１２５ｍｇ／ｍｌ）；Ⅳ组在麻醉诱导时静注枢复宁４ｍｇ。记录术后４、８、１２、２４、４８ｈ吗啡用量、疼痛评分、恶心、呕吐、镇静评分。枢复宁组（Ⅳ组）病人恶心和呕吐发生率由７７．７％和５０％（对照组）分别降低至４０％和２０％，差别有显著性（Ｐ＜０．０５）；氟哌啶组（Ⅱ组及Ⅲ组）病人恶心和呕吐发生率虽然分别降低至５５％和３５％、４２．１％和２１．１％，但无统计学意义（Ｐ＞０．０５）。氟哌啶组病人术后１２小时的镇静评分明显高于对照组（Ｐ＜０．０１）。各组间疼痛、ＶＡＳ评分及吗啡用量无差别（Ｐ＞０．０５）。结果提示静脉注射枢复宁能有效地减少术后ＰＣＡ治疗中的恶心呕吐，效果优于氟哌啶。