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ondansetron (Zuplenz / ondansetron OFDS)

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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
来源： ClinicalTrials.gov, Galena Biopharma, Inc.

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

PubMedJournal of pharmaceutical and biomedical analysis2026-08-04

Rapid screening of physicochemical compatibility between co-administered injectable drugs using thermal and spectroscopic approaches.

Granados Pedro A PA, Santana Ingrid A IA, Lima Ana Luiza AL, Gross Idejan P IP et al.

The concomitant administration of injectable drugs in hospital settings frequently involves extemporaneous combinations within the same infusion line, often without compatibility evaluation. This practice may compromise drug stability and patient safety, particularly in intensive care units characterized by complex polypharmacy regimens. In this study, a rapid screening protocol based on complementary thermal, spectroscopic, and morphological techniques was applied to investigate potential physicochemical interactions between injectable drugs under accelerated stress conditions. Dopamine, ondansetron, rocuronium, and fluconazole were combined pairwise as binary physical mixtures and subjected to controlled thermal and photonic stress. Differential scanning calorimetry, thermogravimetric analysis, FTIR spectroscopy, and stereomicroscopy were employed to detect early physicochemical interactions and stress-induced instability. Thermal analysis revealed melting point shifts, enthalpy reduction, amorphization, and premature degradation events for several combinations, indicating different levels of intermolecular interaction. FTIR and morphological analyses demonstrated that some changes in thermal profile were accompanied by chemically relevant alterations and progressive discoloration, particularly after combined thermal and light exposure. Dopamine/fluconazole and dopamine/ondansetron mixtures showed evidence of moderate solid-state interaction, while ondansetron/fluconazole exhibited increased susceptibility to stress-induced instability. Mixtures containing rocuronium exhibited greater sensitivity to combined thermal and photonic stress, especially ondansetron/rocuronium, which showed marked light-dependent instability. Overall, the proposed approach proved useful as a rapid preliminary risk-ranking strategy to identify injectable drug combinations requiring further compatibility investigation under clinically relevant conditions.

PMID 42546540
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PubMedNigerian medical journal : journal of the Nigeria Medical Association2026-08-03

Prophylactic Efficacy of Intravenous Nefopam Versus Ondansetron in Preventing Post-Spinal Shivering in Parturients Undergoing Elective Caesarean Section: A Double-Blind Randomised Controlled Trial.

Malau Kefas Thomas KT, Usman Yohanna Musa YM, Kpalap Precious Barisi PB, Shaki Rimamkanati Christopher RC et al.

Post-spinal shivering (PSS) is a frequent complication of spinal anaesthesia during caesarean section, causing patient discomfort and potential physiological disturbances. Both nefopam and ondansetron possess anti-shivering properties; however, comparative evidence in obstetric patients is limited. The objective of this study is to compare the efficacy and safety of intravenous nefopam and ondansetron in preventing post-spinal shivering in women undergoing elective caesarean section under spinal anaesthesia. This randomised controlled study included 96 ASA II parturients scheduled for elective caesarean section under spinal anaesthesia. Participants were randomly allocated into three groups (n = 32 each). Group N received intravenous nefopam (0.15 mg/kg), Group O received intravenous ondansetron (0.1 mg/kg), and Group P received 10 mL of normal saline as a placebo. The medications were administered 15 minutes before spinal anaesthesia. Patients were monitored for the incidence and severity of shivering using the Crossley and Mahajan scale. Side effects and the need for rescue medication (intravenous pethidine 0.5 mg/kg) were also recorded. Statistical significance was set at p < 0.05. The incidence of PSS was significantly lower in Group N (18.8%) and Group O (18.8%) compared with Group P (59.4%) (p < 0.001). Severe shivering (grades 3-4) occurred only in the placebo group (40.5%). Consequently, the need for rescue pethidine was significantly higher in Group P (37.5%), while none of the patients in Groups N or O required it (p < 0.001). Postoperative nausea was less frequent in Group O (3.1%) and Group N (12.5%) compared with Group P (25%) (p < 0.05). Mild injection-site pain occurred only in Group N (9.4%). Intravenous nefopam and ondansetron are similarly effective in preventing post-spinal shivering and reducing rescue analgesia requirements during caesarean section under spinal anaesthesia. Ondansetron showed better antiemetic effect, while nefopam was associated with mild injection-site discomfort.

PMID 42544185
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PubMedSouth Dakota medicine : the journal of the South Dakota State Medical Association2026-07-29

Amniotic Fluid Embolism: A Case Report.

McCann Sean S, Kallemeyn Brenda B

In obstetrics, an amniotic fluid embolism (AFE) is a rare and highly devastating event. This case highlights the presentation of an amniotic fluid embolism and its treatments. A 35-year-old G1P0 became pulseless shortly after her cesarean section and was successfully resuscitated with high-quality CPR, fluid administration, and a regimen of atropine, ondansetron, and ketorolac. She was under general anesthesia for her cesarean due to non-reassuring heart tones and remained intubated when transferred to the intensive care unit. Due to the rapid responsiveness of treatment, she had a favorable outcome unlike a majority of AFEs. This case highlights the presentation of AFE and importance of prompt treatment. While there are specific diagnostic criteria atypical AFEs are not uncommon, and the threshold should be low for the initiation of treatment. The article reviews the most recent standards of care put forth by the Society for Maternal Fetal Medicine. It also adds to the data that supports the use of various experimental treatments to prevent morbidity and mortality.

PMID 42522074
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PubMedChemistryOpen2026-07-27

In Vivo Evaluation of Psoralen in a Copper Sulfate-Induced Chick (Gallus gallus domesticus) Emesis Model and In Silico Analysis of Its Interaction With D2, 5-HT3 A, and Muscarinic Receptors.

Chandra Kishor K, Bahar Sharif Uddin SU, Akter Khadija K, Khatun Mst Muslima MM et al.

Psoralen (PSN), a naturally occurring furocoumarin, was evaluated for its antiemetic potential using integrated in vivo and in silico approaches, considering the limitations of currently available antiemetic agents. The antiemetic activity of PSN was investigated in a copper sulfate-induced emesis model using 2-day-old chicks (Gallus gallus domesticus). A dose-dependent experimental design was employed with PSN (5, 10, and 20 mg/kg), alongside standard antiemetics (domperidone 6 mg/kg, ondansetron (OND) 5 mg/kg, and hyoscine 21 mg/kg) and combination treatments. Latency to first retch and total retching episodes were recorded, and percentage inhibition was calculated. Molecular docking was performed against D2, D3, 5-HT3A, and muscarinic (M1-M5) receptors. ADMET and toxicity profiles were predicted using SwissADME and ProTox-3.0. PSN produced a significant, dose-dependent reduction in retching. The 20 mg/kg dose showed 65.60% inhibition of retches compared to control. Combination treatment with OND further enhanced inhibition (65.60%). Docking analysis revealed that PSN exhibited the strongest binding affinity toward the D2 receptor (-8.8 kcal/mol), followed by M5 (-8.1 kcal/mol) and 5-HT3A (-7.7 kcal/mol). Pharmacokinetic prediction indicated high gastrointestinal absorption and favorable drug-likeness properties. PSN demonstrates significant antiemetic activity in a validated chick emesis model, supported by moderate binding affinity toward key emesis-related receptors. While docking findings suggest possible receptor interactions, further mechanistic and translational studies are required to confirm the molecular basis of its activity.

PMID 42503454
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PubMedArthroscopy, sports medicine, and rehabilitation2026-07-25

Perioperative Intravenous Dexamethasone Improves Pain and Functional Outcomes After Arthroscopic Rotator Cuff Repair.

Wolterink Trevor D TD, Craddock Germain G, Castle Joshua P JP, Gaudiani Michael A MA et al.

To evaluate the effect of perioperative dexamethasone on patient-reported pain, functional outcomes, and minimal clinically important difference (MCID) achievement following arthroscopic rotator cuff repair. Patients who underwent rotator cuff repair between 2013 and 2023 were identified and divided into groups. Those who received peri operative dexamethasone were compared with controls. Outcomes included visual analog scale (VAS) pain, patient-reported outcomes measurement information system (PROMIS) upper extremity, PROMIS pain interference, and MCID. Multivariate logistic and linear regression models adjusted for age, sex, body mass index, diabetes, race/ethnicity, smoking, and preoperative opioid use. Subgroup analyses were performed by tear size. A total of 309 patients was included (187 dexamethasone and 122 control). Dexamethasone administration was associated with improved functional recovery and sustained pain reduction. PROMIS upper extremity and PROMIS pain interference scores favored Dexamethasone at 6 weeks, 3 months, and 6 months (all P < .01). VAS pain was significantly lower at 12 months (1.9 ± 2.9 vs 3.1 ± 3.5, P = .003) and 24 months (1.0 ± 2.5 vs 1.8 ± 3.1, P = .035). Only 37% of patients completed a 2-year follow-up, limiting the strength of these long-term comparisons. In small/medium tears, MCID achievement for VAS was greater at 6 weeks (31% vs 21%, P = .041) and 3 months (34% vs 21%, P = .012). Logistic regression confirmed dexamethasone as an independent predictor of early MCID (OR 1.67, 95% CI 1.02-2.73, P = .041). Large/massive tears showed transient VAS improvement without MCID benefit. Opioid consumption did not differ between groups (all P > .12). Dexamethasone reduced ondansetron use in large/massive tears at 0-4 hour (β = -0.34, P = .04) and in small/medium tears at 4-8 hour (β = -0.19, P = .04), with no differences for other antiemetics. Complication rates were similar (11.2% vs 4.9%, P = .055). Perioperative intravenous dexamethasone is a safe adjunct to arthroscopic rotator cuff repair, supporting early antiemetic benefits, durable pain relief, and selective improvements in patient-reported outcomes. Benefits appear most pronounced in small/medium tears at early follow-up and large/massive tears at later stages, suggesting tear size-specific response. Level III, retrospective comparative study.

PMID 42500163
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PubMedClinical medicine insights. Case reports2026-07-23

Successful Management of Refractory Cannabinoid Hyperemesis Syndrome With Topical Capsaicin: A Case Report With Proposed Mechanism of Action and Literature Review.

Ilyas Muhammad M, Fernando Anushka A, Choriyev Abubakir A, Adi Mohammad M et al.

Cannabinoid hyperemesis syndrome (CHS) is a debilitating disorder of chronic, heavy cannabis users characterized by cyclic severe nausea, vomiting, and abdominal pain that is classically relieved by hot baths. Standard antiemetics often fail, and dysregulation of endocannabinoid signaling with involvement of heat-sensitive TRPV1 channels has been proposed. Topical capsaicin - a TRPV1 agonist - has been reported in small series and case reports to reproduce the hot-water effect and rapidly relieve symptoms. A 28-year-old man with daily high-potency cannabis use (∼2 g/day for 7 years) presented to the emergency department with 48 hours of intractable non-bilious vomiting (∼20 episodes/day), severe periumbilical cramping (8/10), and a history of similar episodic flares relieved by prolonged hot showers. Initial ED therapy (IV fluids, ondansetron, metoclopramide, pantoprazole) produced minimal benefit; labs showed hypokalemic, hypochloremic metabolic alkalosis and pre-renal azotemia, with otherwise unremarkable imaging and enzymes. After informed consent, ∼2 g of 0.1% topical capsaicin cream was applied across the abdomen. The patient experienced an acute burning sensation for ∼15-30 minutes; retching ceased within 10 minutes, pain fell to 2/10 by 30 minutes and resolved by 90 minutes, and he tolerated oral intake. Vital signs normalized and electrolytes/renal function returned to baseline at 48-hour follow-up. He was discharged with counseling on cannabis cessation and a capsaicin tube for prodromal use. Topical capsaicin produced rapid, durable symptom resolution in this case of refractory CHS with only transient local discomfort. The effect is plausibly mediated by TRPV1 activation followed by peripheral desensitization, recapitulating the therapeutic hot-water response. Given consistent positive signals from case reports, series, and small pilot data, topical capsaicin is a low-risk, accessible adjunct for refractory CHS, but larger controlled studies are needed to define optimal dosing, duration, and long-term outcomes.

PMID 42491286
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