制造商：
Strativa制药
药理分类：
选择性5-HT3受体拮抗剂。
“活性成分”（词）：
昂丹司琼（碱）4毫克，8毫克，口服水溶性薄膜，薄荷味。
指示（S）：
预防恶心和呕吐与高致吐性化疗，包括顺铂≥50mg/m2。与初次和重复中度致吐性化疗疗程的恶心和呕吐的预防。在患者接受全身照射，高剂量的分数，腹部，或每日分数到腹部放射治疗与预防恶心和呕吐。预防术后恶心和/或呕吐。
药理作用：
昂丹司琼是一种选择性五羟色胺5-HT3受体拮抗剂。这些受体位于外周迷走神经末梢以及中央化学感受器触发区。昂丹司琼的止吐作用可能是由于血清素抑制外周活动，集中，或在这两个网站。然而，出现细胞毒性化疗与小肠肠嗜铬细胞的5 - 羟色胺的释放。另外，尿中排泄量的5 - 羟吲哚乙酸，羟色胺的主要代谢物，顺铂给药增加平行呕吐发作。拮抗作用释放的5 - 羟色胺在5-HT3受体的迷走神经端子可能会抑制呕吐反射。
临床试验：
昂丹司琼口腔被证明是统计上显着优于安慰剂在预防化疗引起的恶心和呕吐，在两个双盲，单一疗法试验的患者在成人和儿童患者接受高致吐性化疗，以及多个研究接受初次和重复中度致吐性化疗的课程。第一次审判相比，在357名成年患者接受高致吐性化疗方案治疗含顺铂≥50mg/m2口服剂量昂丹司琼。在主要终点，66％的患者接受昂丹司琼了24Mg，每日一次，55％，8毫克，每天两次，55％接受32mg每日一次完成24小时的研究期间，无呕吐和没有止吐药物。所有3个剂量均表现显着优于安慰剂组。
在67例患者接受中度致吐性药物环磷酰胺为基础的化疗含阿霉素进行的一项研究中，61％的患者接受恩丹西酮经历没有呕吐相比，6％，而安慰剂组（P <0.001）。在随后的化疗疗程（396个）148例无对照研究评价昂丹司琼，昂丹司琼预防呕吐重新疗程后，79％的。三个开放标签，不受控制的试验，在182 4-18岁儿童给出了各种非顺铂，顺铂或治疗癌症。其次是管理的口服昂丹司琼3天的起始剂量盐酸昂丹司琼注射液。在这些研究中，58％的170例可评估患者并没有呕吐的第1天。
三双盲研究评估了口服昂丹司琼在辐射引起的恶心和呕吐的预防疗效。第一次随机研究，涉及20例，结果显示，口服昂丹司琼前总辐射体各组分明显比安慰剂有效防止呕吐。第二项研究比较了口服昂丹司琼胃复安在105例患者接受单一高剂量的放射治疗前或后场大小≥80平方厘米腹部。昂丹司琼是更有效的比胃复安达到完全控制的呕吐（呕吐）。在第三个试验，涉及135例，口服恩丹西酮显着更有效地实现完全控制的呕吐相比，丙氯拉嗪的患者接受了1 - 4周的课程分割放疗>100平方厘米腹部的一个字段的大小。
口服昂丹司琼预防术后恶心和呕吐的疗效进行研究在两个双盲试验，涉及865住院患者接受外科手术的女性患者。患者接受昂丹司琼一小时前，麻醉诱导。昂丹司琼被证明是比安慰剂更有效的预防术后恶心和呕吐。
法律分类：
接收
成人：
允许每部影片完全溶解后再下一部电影。舌头上溶解为4-20秒，然后再吞咽。高致吐了24Mg（陆续给为3 8毫克电影）开始前30分钟的单日化疗（多天，单剂量没有研究）。中度致吐：8毫克每8小时2剂量开始30分钟前化疗，然后8毫克每1-2天，化疗完成后的12小时。给予全身照射：8毫克，1 - 2小时前放疗各组分的每一天。单一高剂量的部分放射治疗腹部：8毫克1 - 2小时前放疗，然后8毫克每8小时后，第一次剂量为1-2天，放疗后完成。每日分次放射治疗腹部：8毫克1 - 2小时前放疗，然后8毫克每8小时后，第一次剂量放射治疗的每一天。后运预防：16mg（鉴于先后作为两个8毫克电影）麻醉诱导前1小时。对于一切：严重肝功能障碍：最大8mg/day。
儿童：
高致吐性化疗，放疗，术后预防或<4yrs年龄：不推荐使用。允许每部影片完全溶解后再下一部电影。舌头上溶解为4-20秒，然后再吞咽。 4-11岁：中度致吐：4毫克每4小时3剂量化疗前开始30分钟，然后4毫克每8小时化疗后1-2天完成。
禁忌（S）：
伴随阿朴吗啡：深刻低血压或意识丧失的风险。
警告/注意事项：
可能掩盖渐进性肠梗阻和/或胃扩张（特别是腹部手术后或化疗引起的恶心/呕吐的病人）。不要使用替代胃肠减压。肝功能障碍。怀孕（Cat.B）。哺乳期的母亲。
互动（补）：
强效CYP3A4诱导剂（如苯妥英钠，卡马西平，利福平）可能会增加昂丹司琼的间隙。可减少曲马多的镇痛活性。
不良反应（S）：
头痛，疲倦/乏力，便秘，腹泻;罕见：支气管痉挛，过敏性反应，一过性心电图改变，包括QT间期延长（特别是IV形式）。
如何提供：
水溶性薄膜-10
Available in 4-mg and 8-mg films, the same strength of oral ondansetron, with the same recommended dosing1-5
Can be dosed prior to therapy or surgery1
Pediatric dosing (ages 4 to 11 years), indicated only in moderately emetogenic chemotherapy, is one 4-mg film given 3 times a day1
When dosing more than one film, each ZUPLENZ film should be allowed to dissolve completely before administering the next film1
Appropriate for use in a variety of settings, including in office, at home, traveling, hospitals, infusion centers, hospices, nursing homes, and rehabilitation facilities
For the prevention of postoperative, highly and moderately emetogenic cancer chemotherapy-induced, and radiotherapy-induced nausea and vomiting.
The concomitant use of apomorphine with ondansetron is contraindicated based upon reports of profound hypotension and loss of consciousness.
Patients known to have hypersensitivity to ondansetron and to other selective 5-HT3 receptor antagonists should not take ZUPLENZ. Hypersensitivity reactions, including anaphylaxis and bronchospasm, have been reported. Rarely and predominantly with intravenous ondansetron, transient electrocardiographic changes, including QT interval prolongation, have occurred.
The use of ZUPLENZ in patients following abdominal surgery or in patients with chemotherapy-induced nausea and vomiting may mask a progressive ileus and/or gastric distension. ZUPLENZ does not stimulate gastric or intestinal peristalsis and should not be used instead of nasogastric suction.
The most common adverse drug reactions (≥5%) reported in clinical trials of patients receiving ondansetron for prevention of nausea and vomiting associated with cancer chemotherapy or radiotherapy were headache, malaise/fatigue, constipation, and diarrhea. For postoperative nausea and vomiting, headache occurred at a rate significantly different from placebo.
Manufacturer:
Strativa Pharmaceuticals
Pharmacological Class:
Selective 5-HT3 receptor antagonist.
Active Ingredient(s):
Ondansetron (as base) 4mg, 8mg; oral soluble film; peppermint flavor.
Indication(s):
Prevention of nausea and vomiting associated with highly emetogenic chemotherapy, including cisplatin ≥50mg/m2. Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy. Prevention of nausea and vomiting associated with radiotherapy in patients receiving total body irradiation, single high-dose fraction to the abdomen, or daily fractions to the abdomen. Prevention of post-op nausea and/or vomiting.
Pharmacology:
Ondansetron is a selective antagonist of serotonin 5-HT3 receptors. These receptors are located peripherally on vagal nerve terminals as well as centrally at the chemoreceptor trigger zone. The antiemetic effects of ondansetron may be due to the inhibition of serotonergic activity peripherally, centrally, or in both sites. However, cytotoxic chemotherapy appears to be associated with serotonin release from the enterochromaffin cells of the small intestine. Additionally, urinary excretion of 5-hydroxyindoleacetic acid, the main metabolite of serotonin, increases after cisplatin administration in parallel with the onset of emesis. Antagonism of the released serotonin at the 5-HT3 receptors of the vagal nerve terminals may inhibit the vomiting reflex.
Clinical Trials:
Oral ondansetron was demonstrated to be statistically significantly superior to placebo in the prevention of chemotherapy-induced nausea and vomiting in two double-blind, monotherapy trials in patients receiving highly emetogenic chemotherapy, as well as multiple studies in adult and pediatric patients receiving initial and repeat courses of moderately emetogenic chemotherapy. The first trial compared oral doses of ondansetron in 357 adult patients receiving highly emetogenic chemotherapy regimens containing cisplatin ≥50mg/m2. At primary endpoint, 66% of patients receiving ondansetron 24mg once daily, 55% receiving 8mg twice daily, and 55% receiving 32mg once daily completed the 24-hour study period with no emetic episodes and no rescue antiemetic medications. All 3 doses were shown to be significantly superior to placebo.
In a study conducted in 67 patients receiving moderately emetogenic cyclophosphamide-based chemotherapy containing doxorubicin, 61% of patients receiving ondansetron experienced no emetic episodes compared to 6% in the placebo group (p<0.001). Uncontrolled studies evaluating ondansetron given during subsequent chemotherapy courses (396 total) in 148 patients showed that ondansetron prevented emesis following 79% of re-treatment courses. Three open-label, uncontrolled trials were performed in 182 children 4–18 years old with cancer who were given a variety of cisplatin or non-cisplatin regimens. An initial dose of ondansetron HCl injection was followed by administration of oral ondansetron for 3 days. In these studies, 58% of the 170 evaluable patients had no emetic episodes on day 1.
Three double-blind studies evaluated the efficacy of oral ondansetron in the prevention of radiation-induced nausea and vomiting. The first randomized study, involving 20 patients, showed that oral ondansetron given before each fraction of total body radiation was significantly more effective than placebo in preventing emesis. The second study compared oral ondansetron to metoclopramide in 105 patients receiving single high-dose radiotherapy over an anterior or posterior field size of ≥80cm2 to the abdomen. Ondansetron was significantly more effective than metoclopramide in achieving complete control of emesis (0 emetic episodes). In a third trial, involving 135 patients, oral ondansetron was significantly more effective in achieving complete control of emesis compared to prochlorperazine in patients receiving a 1- to 4-week course of fractionated radiotherapy over a field size of >100cm2 to the abdomen.
The efficacy of oral ondansetron in preventing post-op nausea and vomiting was studied in two double-blind trials involving 865 female patients undergoing inpatient surgical procedures. Patients received ondansetron one hour prior to induction of anesthesia. Ondansetron was shown to be significantly more effective than placebo in preventing post-op nausea and vomiting.
Legal Classification:
Rx
Adults:
Allow each film to dissolve completely before taking the next film. Dissolve on tongue for 4–20 secs before swallowing. Highly emetogenic: 24mg (given successively as three 8mg films) 30mins before start of single-day chemotherapy (multi-day, single-dose not studied). Moderately emetogenic: 8mg every 8hrs for 2 doses beginning 30mins before chemotherapy, then 8mg every 12hrs for 1–2 days after chemotherapy completed. Total body irradiation: 8mg 1–2hrs before each fraction of radiotherapy administered each day. Single high-dose fraction radiotherapy to abdomen: 8mg 1–2hrs before radiotherapy, then 8mg every 8hrs after 1st dose for 1–2 days after radiation completed. Daily fractionated radiotherapy to abdomen: 8mg 1–2hrs before radiotherapy, then 8mg every 8hrs after 1st dose for each day of radiotherapy. Post-op prophylaxis: 16mg (given successively as two 8mg films) 1hr before induction of anesthesia. For all: severe hepatic dysfunction: max 8mg/day.
Children:
Highly emetogenic chemotherapy, radiotherapy, post-op prophylaxis or <4yrs of age: not recommended. Allow each film to dissolve completely before taking the next film. Dissolve on tongue for 4–20 secs before swallowing. 4–11yrs: moderately emetogenic: 4mg every 4hrs for 3 doses beginning 30mins before chemotherapy, then 4mg every 8hrs for 1–2 days after chemotherapy completed.
Contraindication(s):
Concomitant apomorphine: risk of profound hypotension or loss of consciousness.
Warnings/Precautions:
May mask progressive ileus and/or gastric distention (esp. after abdominal surgery or patients with chemotherapy-induced nausea/vomiting). Do not use as alternative to nasogastric suction. Hepatic dysfunction. Pregnancy (Cat.B). Nursing mothers.
Interaction(s):
Potent CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampicin) may increase clearance of ondansetron. May reduce analgesic activity of tramadol.
Adverse Reaction(s):
Headache, malaise/fatigue, constipation, diarrhea; rare: bronchospasm, anaphylaxis, transient ECG changes, including QT prolongation (esp. IV form).
How Supplied:
Soluble film—10