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ondansetron (Zuplenz / ondansetron OFDS)

✓ Approved

Galena Biopharma, Inc. · HTR3A · 小分子

什么是 ondansetron?

ondansetron 是一种小分子,由Galena Biopharma, Inc.研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名Zuplenz, ondansetron OFDS
公司Galena Biopharma, Inc.
药物类别小分子
分子靶点HTR3A
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

ondansetron 作用于 1 个分子靶点:

HTR3A5-hydroxytryptamine receptor 3A (5-HT3R, 5-HT-3)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

相关研究文献

PubMedInternational journal of molecular sciences2026-10-27

Modulation of the Liver-Brain Axis by Ondansetron in Thio-Acetamide-Induced Acute Hepatic Encephalopathy.

Sari Fatih Mehmet FM, Bilgin Yasin Y, Cicek Betul B, Kurt Engin E et al.

Hepatic encephalopathy (HE) is a severe neurological complication of liver failure characterized by hyperammonemia, oxidative stress, neuroinflammation, and progressive neuronal dysfunction. Ondansetron (OND), a selective 5-hydroxytryptamine-3 (5-HT3) receptor antagonist, has reported anti-inflammatory and neuroactive properties, but its effects in HE remain poorly defined. This study evaluated OND in a thioacetamide (TAA)-induced acute HE model in female Sprague-Dawley rats. Animals were assigned to Control, TAA, OND, TAA+OND (0.5 mg/kg), and TAA+OND (1 mg/kg) groups. Serum and cerebral glutamine, oxidative and antioxidant parameters, histopathological alterations, and TLR2, NF-κB, IL-1β, GFAP, NLRP3, and caspase-1 immunoreactivity were assessed in liver and brain tissues. TAA increased glutamine accumulation, produced tissue injury, altered redox parameters, and increased several inflammation-related markers. OND significantly reduced cerebral glutamine and attenuated selected biochemical, histopathological, and immunohistochemical alterations, with generally more pronounced effects at 0.5 mg/kg. These findings indicate that OND administration is associated with partial modulation of metabolic, oxidative, inflammatory, and structural alterations in TAA-treated rats, warranting further receptor-specific and functional studies to clarify its mechanisms and therapeutic relevance.

PMID 42942034
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PubMedAmerican journal of therapeutics2026-10-23

Does Repeated-Dose Ondansetron Provide Additional Benefit in Children with Acute Gastroenteritis? A Systematic Review and Meta-Analysis.

Fonseca Caio Henrique Prado CHP, Sobral Milene Vitória Sampaio MVS, Cordeiro E Silva José Henrique JH

PMID 42912510
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PubMedPharmaceutical science advances2026-10-20

Corrigendum to "D-pinitol modulates the anti-emetic effects of aprepitant, domperidone, and ondansetron in chicks" [Pharmaceut. Sci. Adv. 3, (2025), 100073].

Rahman Elit E, Rahman Anisur A, Sheikh Salehin S, Polash Jannatul Islam JI et al.

[This corrects the article DOI: 10.1016/j.pscia.2025.100073.].

PMID 42898476
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PubMedInnovations in clinical neuroscience2026-10-20

Concurrent Management of Adolescent Cannabinoid Hyperemesis Syndrome and Delirium With Haloperidol.

Hsu Jeremiah J, Kotdawala Mahaksh M, Priolo Thomas T

Cannabinoid hyperemesis syndrome (CHS) manifests in adults as severe nausea accompanied by episodic vomiting and intense abdominal pain, typically associated with prolonged, high-dose cannabis use. The clinical course of CHS is divided into 3 distinct phases: prodromal, hyperemetic, and recovery. Traditional antiemetic and antinausea medications, such as ondansetron and metoclopramide, are often used in the acute clinical setting to address these isolated symptoms. Discussions and occasional use of haloperidol have demonstrated a level of symptom relief in patients with CHS. In several instances, patients report complete resolution of symptoms previously refractory to, or only partially relieved by, traditional antiemetics and antinausea medications. This case report explores the hospital course of a 15-year-old female adolescent who presented to the emergency department with a recurrent episode of CHS. The patient reported symptoms of nausea, intense abdominal pain, compulsive bathing behavior, physical agitation, and delirium. In the setting of CHS symptoms refractory to traditional antiemetics and concurrent behavioral disturbances, the patient was started on a standing low dose of haloperidol. Within 6 days of starting haloperidol treatment, the patient reported complete resolution of her presenting symptoms and was subsequently discharged from the hospital. We conclude that patients presenting with CHS and concurrent delirium, as is often the clinical presentation, would further benefit from the off-label use of haloperidol. Although minimal literature exists on the management of CHS, there is almost no evidence examining CHS comorbid with delirium and/or agitation. This report seeks to demonstrate the underlying causality and explore the scientific mechanisms to show the clear benefits of haloperidol as an antiemetic and antinausea medication, in addition to any sequelae of delirium, and highlighting the need for a revision of pre-existing CHS treatment protocols, specifically in the emergency department setting.

PMID 42899270
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PubMedAsia-Pacific journal of clinical oncology2026-10-15

Selective Serotonin Receptor (5-HT3) Antagonist Prescribing in Cancer Inpatients: A Retrospective Clinical Audit.

Corey Henshaw H, Gray Matthew M, Bui Kim Tam KT, Linton Anthony A

Selective serotonin receptor (5-HT3) antagonists are first-line antiemetics for chemotherapy-induced, radiotherapy-induced, and post-operative nausea and vomiting; other causes of nausea in advanced cancer warrant alternative agents. We aimed to determine patterns of inpatient 5-HT3 antagonist prescribing and its guideline concordance. We retrospectively reviewed electronic medical records of all patients admitted under Medical Oncology at a single metropolitan hospital over 6 months who were prescribed a 5-HT3 antagonist. Data on demographics, cancer, and the prescription (agent, indication, prescriber, duration, administration) were extracted and reviewed for guideline concordance. Analyses were descriptive. Of 210 patients admitted between January and June 2025, 81 (38.6%) were prescribed a 5-HT3 antagonist. Mean age was 64.2 years (range 24-87); 41 (50.6%) were female, and 62 (76.5%) had metastatic cancer. Of 137 prescriptions written, 134 (97.8%) were for ondansetron. Nausea was documented in 104 (75.9%), but a specific cause in only 55/104 (52.9%). The most common prescribers were Emergency (62, 45.3%) and After-Hours (32, 23.4%) doctors. Prescriptions were brief (median 1 day); 82 (59.9%) were administered at least once, and 62/82 (75.6%) were single-dose. Overall, 93 (67.9%) were non-concordant. Concordance was 10/14 (71.4%) in Medical Oncology, 20/21 (95.2%) in anesthetics and intensive care, 4/4 (100%) in Radiation Oncology, and 4/4 (100%) in Palliative Care, but 2/62 (3.2%) in Emergency and 4/32 (12.5%) in After-Hours prescribers. 5-HT3 antagonists were frequently prescribed outside guideline recommendations, particularly by clinicians less familiar with cancer. Targeted education, electronic order-set redesign, and structured documentation of the suspected mechanism of nausea may improve guideline-concordant antiemetic prescribing.

PMID 42878036
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PubMedJournal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners2026-10-11

Add-on oral amisulpride for prevention of chemotherapy-induced nausea and vomiting during highly emetogenic chemotherapy: A randomized double-blind placebo-controlled group sequential trial.

Gr Gayathri G, Ramasubbu Mathan Kumar MK, Mishra Archana A, Hota Debasish D et al.

IntroductionGuideline-based prophylaxis prevents most vomiting during highly emetogenic chemotherapy (HEC), but nausea remains incompletely controlled, especially where NK1 receptor antagonists and olanzapine are inaccessible or ineffective. Amisulpride, a dopamine D2/D3 antagonist, may add benefit with less sedation than olanzapine.MethodsAdults receiving cisplatin-based or anthracycline-cyclophosphamide HEC were studied during a single cycle in this randomized, double-blind, placebo-controlled group sequential trial. All received intravenous ondansetron and dexamethasone on day 1 plus oral dexamethasone 8 mg twice daily on days 2-4, with oral amisulpride (25 mg before chemotherapy, then 12.5 mg nightly for 3 days) or placebo. The primary endpoint was the 4-day (0-96 h) no-nausea responder rate; the planned sample size of 94 targeted an 18 percentage-point improvement. Two interim and one final analysis used O'Brien-Fleming efficacy and futility boundaries.ResultsThe trial stopped for futility at the second interim analysis (70 participants; 35 per arm). No-nausea response was 65.7% with amisulpride versus 57.1% with placebo (risk difference 8.6 percentage points; 95% CI -14.2 to 31.3; p = 0.461). Complete response (no emesis or rescue medication) was 80.0% versus 68.6% (p = 0.274). VAS, FLIE, rescue medication use, and adverse-event frequency were similar, apart from more frequent constipation with amisulpride.ConclusionsThe 8.6 percentage-point difference favored amisulpride but fell short of the 18-point practice-changing MCID, in a well-controlled placebo arm. Without an olanzapine- or NK1-containing comparator, the trial cannot position amisulpride against those regimens, nor exclude a smaller benefit worth having where they are inaccessible.

PMID 42858047
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