Zofran: Rapid Relief from Nausea and Vomiting
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Synonyms
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Zofran (ondansetron) is a prescription medication classified as a 5-HT3 receptor antagonist, specifically developed for the management and prevention of nausea and vomiting. It is a cornerstone therapeutic agent in both oncology and surgical settings, renowned for its efficacy in blocking the actions of chemicals in the body that can trigger emesis. Its mechanism provides a targeted approach, making it a first-line choice for clinicians managing chemotherapy-induced, radiotherapy-induced, and postoperative nausea and vomiting (PONV). This product card provides a comprehensive, expert-level overview of Zofran for healthcare professionals and informed patients.
Features
- Active Ingredient: Ondansetron hydrochloride.
- Available Formulations: Oral tablets (4mg, 8mg), orally disintegrating tablets (4mg, 8mg), oral solution (4mg/5mL), and injectable solution (2mg/mL for IV/IM administration).
- Drug Class: Selective 5-hydroxytryptamine-3 (5-HT3) receptor antagonist.
- Mechanism of Action: Works by blocking serotonin, a natural substance in the body that causes nausea and vomiting, both centrally in the chemoreceptor trigger zone (CTZ) and peripherally in the vagal nerve terminals.
- Onset of Action: Intravenous administration provides effects within minutes; oral formulations typically work within 1-2 hours.
- Duration of Action: Effects can last from 4 to 24 hours depending on the dosage and formulation.
Benefits
- Highly Effective Prophylaxis: Significantly reduces the incidence and severity of nausea and vomiting associated with highly emetogenic chemotherapy and radiation therapy.
- Rapid Symptomatic Relief: Provides prompt control of active nausea and vomiting episodes, improving patient comfort and quality of life.
- Supports Treatment Adherence: By effectively managing debilitating side effects, it enables patients to complete full courses of critical cancer treatments.
- Versatile Administration: Multiple formulations (tablet, ODT, liquid, injection) allow for tailored administration based on patient need, clinical setting, and ability to swallow.
- Well-Tolerated Profile: Generally associated with a favorable side effect profile compared to older antiemetic agents, with a lower incidence of sedative and extrapyramidal effects.
Common use
Zofran is indicated for the prevention of nausea and vomiting in several key clinical scenarios. Its primary use is in oncology for preventing nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin. It is also approved for the prevention of nausea and vomiting associated with radiotherapy in patients receiving either total body irradiation, single high-dose fraction radiotherapy to the abdomen, or daily fractions to the abdomen. Furthermore, it is a standard prophylactic agent for postoperative nausea and vomiting (PONV) in patients undergoing surgical procedures. It may be used off-label for other causes of severe nausea, such as hyperemesis gravidarum (under specialist supervision), and gastroenteritis, though it is not a first-line treatment for the latter.
Dosage and direction
Dosage varies significantly based on indication, emetogenic potential of the therapy, patient factors, and formulation. The following are general guidelines; always follow a healthcare provider’s specific prescription.
- Chemotherapy-Induced Nausea and Vomiting (Adults): A common regimen is 8mg or 0.15mg/kg administered intravenously 30 minutes before the start of chemotherapy, followed by two additional 8mg doses orally 4 and 8 hours after the first dose. Then, 8mg orally every 12 hours for 1-2 days after chemotherapy.
- Radiotherapy-Induced Nausea and Vomiting (Adults): 8mg orally taken 1-2 hours before radiotherapy, then every 8 hours after the first dose for each day radiotherapy is given.
- Postoperative Nausea and Vomiting (Adults): 16mg orally as a single dose 1 hour before induction of anesthesia. Alternatively, 4mg undiluted may be administered intravenously over at least 30 seconds, preferably before induction.
- Pediatric Use: Dosage is based on body surface area for chemotherapy-induced nausea and vomiting. For patients 4-18 years old, a single 4mg IV dose is used for PONV prevention.
- Administration: Tablets should be swallowed whole with water. Orally disintegrating tablets (ODTs) are placed on the tongue, where they dissolve rapidly and can be swallowed with saliva without water. The oral solution should be measured with the provided dosing cup or syringe.
Precautions
Patients should be advised to inform their physician of their complete medical history, especially of:
- Personal or family history of congenital long QT syndrome.
- Electrolyte imbalances (e.g., hypokalemia, hypomagnesemia).
- Congestive heart failure, bradyarrhythmias, or use of other medications that prolong the QT interval.
- Phenylketonuria (PKU), as the orally disintegrating tablets contain aspartame.
- Abdominal surgery or ileus, as ondansetron may mask a progressive gastric dilation or ileus.
- Liver impairment, as metabolism may be reduced, requiring dosage adjustment.
- Allergies, including to other 5-HT3 receptor antagonists.
Contraindications
Zofran is contraindicated in patients with:
- Known hypersensitivity to ondansetron or any component of the formulation.
- Concomitant use of apomorphine, due to the risk of profound hypotension and loss of consciousness.
Possible side effect
While generally well-tolerated, the following side effects have been reported:
- Very Common (>10%): Headache, constipation.
- Common (1-10%): Dizziness, fatigue, drowsiness, diarrhea, fever, sensation of warmth or flushing, injection site reactions.
- Uncommon (0.1-1%): Hiccups, hypotension, chest pain, arrhythmias (including QT prolongation), seizures, blurred vision, transient elevation in liver enzymes.
- Rare (<0.1%): Anaphylaxis, extrapyramidal reactions (although less common than with older antiemetics), severe constipation leading to bowel obstruction.
Drug interaction
Ondansetron is primarily metabolized by CYP enzymes and has the potential for several interactions:
- QT-Prolonging Agents: Concomitant use with drugs known to prolong the QT interval (e.g., certain antiarrhythmics like amiodarone, antipsychotics like haloperidol, antibiotics like erythromycin, antidepressants) may result in additive effects and increased risk of serious cardiac arrhythmias like Torsades de Pointes. This combination requires careful consideration and monitoring.
- CYP 3A4 Inducers: Drugs that induce the CYP3A4 enzyme system (e.g., rifampin, carbamazepine, phenytoin) may increase ondansetron clearance and decrease its plasma concentration, potentially reducing efficacy.
- CYP 3A4 Inhibitors: Drugs that inhibit CYP3A4 (e.g., ketoconazole, erythromycin) may decrease ondansetron clearance and increase plasma concentrations, potentially increasing the risk of side effects.
- Apomorphine: Contraindicated due to risk of profound hypotension and loss of consciousness.
- Serotonergic Drugs: Theoretical risk of serotonin syndrome when used with other serotonergic drugs (e.g., SSRIs, SNRIs, tramadol), though this is rare.
Missed dose
For scheduled prophylactic dosing (e.g., around chemotherapy), if a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The regular dosing schedule should be resumed, and the dose should not be doubled to make up for the missed one. For as-needed use, this is not applicable.
Overdose
Symptoms of overdose may be an exaggeration of known side effects, including severe hypotension, visual disturbances, syncope, and dizziness. There is also an increased risk of QT prolongation. There is no specific antidote for ondansetron overdose. Management involves providing supportive care, including continuous ECG monitoring for a minimum of 24 hours to monitor for QT prolongation and potential arrhythmias. Treatment of any clinically significant effects should be symptomatic and supportive.
Storage
- Store all formulations at controlled room temperature, 20°C to 25°C (68°F to 77°F).
- Protect from light.
- Keep the oral solution in the original bottle; do not freeze.
- Keep all medications out of the reach of children and pets.
Disclaimer
This information is for educational and informational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided may not cover all possible uses, directions, precautions, drug interactions, or adverse effects.
Reviews
- Clinical Oncology Perspective: “Zofran remains a foundational agent in our antiemetic regimens for moderately to highly emetogenic chemotherapy. Its predictable efficacy and multiple formulations allow us to tailor care effectively. The introduction of the ODT was a significant advancement for patients with difficulty swallowing.”
- Anesthesiology Perspective: “For high-risk PONV patients, a prophylactic dose of IV Zofran is a standard part of our protocol. It has a rapid onset and significantly reduces the need for rescue antiemetics in the PACU, improving patient satisfaction and potentially allowing for earlier discharge in outpatient settings.”
- Patient Perspective (Chemotherapy): “This medication was a game-changer during my chemo treatments. The nausea was debilitating after my first session. Once we added Zofran beforehand, I was able to manage it much better and actually maintain my nutrition and hydration.”