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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

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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PubMedPediatric allergy and immunology : official publication of the European Society of Pediatric Allergy and Immunology2026-07-20

Oral food challenges in FPIES: A narrative review and proposals for emergency and home-based management of acute FPIES reaction.

Jubin Virginie V, Dumond Pascale P, Benoist Grégoire G, Amat Flore F et al.

Food Protein-Induced Enterocolitis Syndrome (FPIES) is a non-IgE-mediated food allergy marked by delayed vomiting and potential hypovolemic shock. This review by the French FPIES working group (SFA, GFRUP, Sp2A, SFP) analyzes recent literature on oral food challenges (OFC) adverse reactions and proposes a standardized protocol for OFC and emergency management. Early consensus OFC protocols from 2017 showed limitations-mainly short intervals between doses during OFC and high hospitalization burdens-leading to inconsistent practices. This narrative review of 2017-2025 studies shows that a single 25% age-appropriate portion generally suffices to trigger symptoms, typically within 1-4 h. This approach balances safety and feasibility while reducing hospital time. As part of the French FPIES monitoring register, and to easily apply this portion, the serving size for each food has been established with specialized dieticians. According to severity, acute reactions require prompt rehydration and ondansetron. Oral or sublingual ondansetron, effective for mild to moderate reactions, can limit dehydration and hospital transfers. In a hospital setting, oral rehydration is indicated in mild reactions, whereas vascular hydration (10 mL/kg over 5-20 min) is required for moderate to severe reactions. Corticosteroids may be added in severe cases. Adrenaline is unnecessary unless associated IgE-mediated symptoms are observed. The working group also proposes including oral rehydration solution and ondansetron in every home emergency kit. These proposals provide a national consensus on the management of FPIES by standardizing French practice from the OFC to the acute management of allergic reaction both in hospitals and at home.

PMID 42473072
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PubMedFrontiers in pharmacology2026-07-17

Dexmedetomidine-flurbiprofen axetil-based opioid-free analgesia attenuates postoperative melatonin suppression and improves sleep quality after thyroidectomy: a randomized controlled trial.

Guo Rui R, Luo Xin X, Chen Li L, Rao Pan-Guo PG et al.

To determine whether an opioid-free patient-controlled intravenous analgesia (PCIA) regimen based on dexmedetomidine and flurbiprofen axetil improves postoperative sleep quality and affects nocturnal melatonin secretion compared to a sufentanil-based regimen in patients undergoing thyroidectomy. In this prospective, randomized, double-blind controlled trial, 96 patients undergoing thyroidectomy were randomly assigned to receive either opioid-free PCIA (dexmedetomidine, flurbiprofen axetil, and ondansetron) or opioid PCIA (sufentanil and ondansetron). PCIA was initiated 5 min before the end of surgery. The primary outcome was postoperative sleep quality, assessed using the Richards-Campbell Sleep Questionnaire (RCSQ). Secondary outcomes included urinary 6-sulfatoxymelatonin (6-SMT) excretion normalized to creatinine, detailed sleep parameters, anxiety levels, pain intensity, sedation levels, and postoperative adverse events. Assessments of sleep quality, urinary 6-SMT excretion, and anxiety levels were performed preoperatively (T0) and on postoperative days 1 (T1) and 2 (T2). Pain intensity (assessed by the Visual Analog Scale, VAS) and sedation levels (assessed using the Ramsay Sedation Scale) were measured at postoperative hours 1, 6, 24, and 48. Patients in the opioid-free group exhibited significantly higher RCSQ scores at T1 and T2, indicating improved postoperative sleep quality (all P < 0.001). Correspondingly, urinary 6-SMT excretion was significantly higher in the opioid-free group at both postoperative time points (P < 0.001), suggesting better preservation of nocturnal melatonin secretion. Detailed sleep parameters showed shorter sleep latency, fewer nocturnal awakenings, and longer total sleep time in the opioid-free group (all P < 0.01). Anxiety levels were significantly lower in the opioid-free group (P < 0.001). Postoperative pain intensity and sedation levels were comparable between groups at all time points (all P > 0.05). The incidences of nausea, vomiting, and pruritus were significantly reduced in the opioid-free group (P < 0.05). An opioid-free PCIA regimen based on dexmedetomidine and flurbiprofen axetil provides non-inferior postoperative analgesia while attenuating postoperative melatonin suppression, improving sleep quality, reducing anxiety, and decreasing opioid-related adverse events. This opioid-sparing strategy may represent an effective approach to enhance postoperative recovery after thyroidectomy. https://www.chictr.org.cn, identifier ChiCTR2400079949. 01/17/2024.

PMID 42465992
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PubMedBMC anesthesiology2026-07-17

Comparison of ultrasound-guided erector spinae plane block to intrathecal morphine for postoperative analgesia in patients undergoing elective lumbar fusion operations under general anesthesia: a randomized controlled trial.

Ashoor Tarek Mohamed TM, Abdelaal Hany Abdelnaby Shehata HAS, Elewa Gamal Eldin Mohammad GEM, Esmat Ibrahim Mamdouh IM et al.

Postoperative (PO) pain management after spine surgery is challenging. For such surgeries, erector spinae plane block (ESPB) and intrathecal morphine (ITM) may offer effective PO analgesia. However, the lack of availability of US machines in low-resource settings and proper dose of ITM that confine the side effects may limit the use of either. Nalbuphine presents an effective approach for managing opioid-induced pruritus without diminishing PO pain relief. In first 24 h after lumbar fusion operations under general anesthesia, the researchers examined effectiveness of bilateral ultrasound (US)-guided ESPB on PO pain and analgesic intake in comparison with ITM. One hundred twenty patients premedicated with 4 mg intravenous ondansetron were randomized into group E; bilateral US-guided ESPB, group M; ITM (0.2 mg) or group C; control group. Time to first rescue analgesic (ketorolac) was the primary outcome while parameters of PO analgesic regimen and side effects were considered as secondary outcomes. Compared to C group, E & M groups had longer duration to first rescue analgesic and reduced analgesic consumption within 24 h postoperatively (P < 0.001). Twenty-four hours after surgery, the M group had lower pain scores (P < 0.001) and higher rates of nausea and pruritus (P < 0.001) than the other two groups without any cases of respiratory depression. The analgesic effect of 0.2 mg intrathecal morphine after lumbar fusion operation under general anesthesia provided lower pain scores and lower analgesic demands than erector spinae plane block at the expense of a higher incidence of manageable side effects of intrathecal morphine within the first 24 h postoperatively. IRB: FMASU MD 102/2022. ClinicalTrials.gov Identifier: NCT05338320. The date that the clinical trial was registered in the ClinicalTrials.gov. : April 14, 2022.

PMID 42464120
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