Palonosetron Fresenius Kabi
Serotonin (5-HT3) Receptor Antagonist — Antiemetic for Chemotherapy-Induced Nausea and Vomiting
Quick Facts About Palonosetron Fresenius Kabi
Key Takeaways About Palonosetron Fresenius Kabi
- Longest-acting 5-HT3 antagonist: With a half-life of approximately 40 hours, palonosetron provides sustained protection against both acute and delayed chemotherapy-induced nausea and vomiting
- Single-dose convenience: A single intravenous dose given 30 minutes before chemotherapy covers the entire risk period, eliminating the need for repeated dosing
- Approved for pediatric use: Safe and effective in children from 1 month of age, with weight-based dosing (20 mcg/kg, maximum 1500 mcg)
- Preferred 5-HT3 antagonist: International guidelines (MASCC/ESMO, ASCO) recommend palonosetron as the preferred agent in this class
- Monitor for serotonin syndrome: Use caution when combining with SSRIs or SNRIs due to the risk of serotonin syndrome
What Is Palonosetron Fresenius Kabi and What Is It Used For?
Palonosetron Fresenius Kabi is a highly selective serotonin (5-HT3) receptor antagonist used to prevent nausea and vomiting caused by cancer chemotherapy. It works by blocking the chemical messenger serotonin, which triggers the vomiting reflex during chemotherapy treatment.
Chemotherapy-induced nausea and vomiting (CINV) remains one of the most distressing side effects of cancer treatment, significantly affecting patients' quality of life and, in severe cases, leading to treatment interruptions or dose reductions. Palonosetron was developed specifically to address this challenge and represents a second-generation 5-HT3 receptor antagonist with unique pharmacological properties that distinguish it from earlier agents such as ondansetron and granisetron.
The active ingredient, palonosetron (administered as the hydrochloride salt), works by selectively binding to and blocking serotonin 5-HT3 receptors located in the chemoreceptor trigger zone (CTZ) in the area postrema of the brain and on vagal afferent nerve terminals in the gastrointestinal tract. During chemotherapy, the cytotoxic drugs cause enterochromaffin cells in the small intestine to release large amounts of serotonin. This serotonin binds to 5-HT3 receptors, triggering the vomiting reflex. By blocking these receptors, palonosetron effectively prevents this cascade.
What sets palonosetron apart from other drugs in its class is its remarkably long elimination half-life of approximately 40 hours — compared to approximately 4 hours for ondansetron and 9 hours for granisetron. This extended duration of action allows a single intravenous dose to provide antiemetic protection for up to 5 days, covering both the acute phase (0–24 hours after chemotherapy) and the delayed phase (24–120 hours), which has historically been more difficult to control.
Palonosetron Fresenius Kabi is approved for use in adults, adolescents, and children over one month of age. It is administered exclusively by healthcare professionals in hospital or clinical settings, typically as part of a comprehensive antiemetic regimen that may also include corticosteroids (such as dexamethasone) and NK1 receptor antagonists (such as aprepitant) for patients receiving highly emetogenic chemotherapy.
International antiemetic guidelines from MASCC/ESMO and ASCO recognize palonosetron as the preferred 5-HT3 receptor antagonist when this drug class is indicated. Its unique binding properties — including allosteric interactions with the 5-HT3 receptor and receptor internalization — contribute to its superior efficacy in preventing delayed-phase CINV compared to first-generation agents.
What Should You Know Before Receiving Palonosetron?
Before receiving palonosetron, inform your healthcare provider about any allergies, heart conditions, electrolyte imbalances, bowel obstruction history, or medications you are taking — particularly antidepressants (SSRIs/SNRIs) or drugs that affect heart rhythm.
Contraindications
Palonosetron must not be used if you have a known allergy (hypersensitivity) to palonosetron or any of the other ingredients in the formulation. The inactive ingredients include mannitol (E421), disodium edetate, sodium citrate (E331), citric acid (E330), water for injections, sodium hydroxide (for pH adjustment), and hydrochloric acid (for pH adjustment). If you have previously experienced an allergic reaction to any 5-HT3 receptor antagonist, discuss this with your healthcare provider before treatment.
Warnings and Precautions
Several conditions require special attention before palonosetron administration. Your healthcare team should be informed if any of the following apply to you:
- Bowel obstruction or chronic constipation: Palonosetron may slow bowel movements. Patients with a history of intestinal obstruction or recurrent severe constipation should be monitored carefully, as 5-HT3 antagonists can reduce colonic transit time.
- Heart rhythm disorders: Palonosetron may cause prolongation of the QT interval on electrocardiogram (ECG). Patients with a personal or family history of QT prolongation, congenital long QT syndrome, or other cardiac conduction abnormalities require careful assessment. QT prolongation can, in rare cases, lead to serious cardiac arrhythmias.
- Electrolyte imbalances: Untreated low potassium (hypokalemia) or low magnesium (hypomagnesemia) increase the risk of cardiac rhythm disturbances. These electrolyte levels should be checked and corrected before palonosetron administration.
When palonosetron is used together with other serotonergic medications (particularly SSRIs and SNRIs), there is a risk of serotonin syndrome — a potentially life-threatening condition characterized by agitation, confusion, rapid heart rate, elevated blood pressure, dilated pupils, muscle twitching, diarrhea, and excessive sweating. Seek immediate medical attention if these symptoms develop.
Pregnancy and Breastfeeding
The safety of palonosetron during pregnancy has not been established in humans. Animal reproductive studies have not provided sufficient data to determine whether palonosetron poses a risk to the developing fetus. As a precautionary measure, palonosetron should not be used during pregnancy unless the clinical benefit clearly outweighs the potential risk. Women of childbearing potential should discuss contraceptive measures with their healthcare provider.
It is not known whether palonosetron or its metabolites are excreted in human breast milk. Because many drugs are excreted in breast milk and because of the potential for adverse reactions in nursing infants, a decision should be made whether to discontinue breastfeeding or to avoid palonosetron treatment, taking into account the importance of the medication to the mother.
Driving and Operating Machinery
Palonosetron may cause dizziness or fatigue. If you experience these effects, do not drive, operate heavy machinery, or perform activities that require alertness until you know how the medication affects you. This is particularly important in the first 24 hours after administration, when central nervous system effects are most likely to occur.
Each vial of Palonosetron Fresenius Kabi contains 4.55 mg of sodium, equivalent to approximately 0.23% of the WHO recommended maximum daily sodium intake of 2 grams for adults. This is considered essentially sodium-free and is not clinically significant for most patients, including those on sodium-restricted diets.
How Does Palonosetron Interact with Other Drugs?
Palonosetron can interact with serotonergic drugs (SSRIs, SNRIs) increasing the risk of serotonin syndrome, and with QT-prolonging medications increasing the risk of cardiac arrhythmias. Always inform your healthcare provider about all medications you are taking.
Drug interactions with palonosetron are an important clinical consideration. While palonosetron is primarily metabolized by CYP2D6 (with minor contributions from CYP3A4 and CYP1A2), formal interaction studies have shown that it does not significantly inhibit or induce these enzymes at therapeutic concentrations. Nevertheless, several categories of medications require careful attention when used concomitantly.
Serotonergic Medications (Major Interaction)
The most clinically important drug interaction involves concurrent use of palonosetron with other serotonergic medications. When palonosetron is combined with drugs that increase serotonin levels, there is a risk of developing serotonin syndrome, a potentially serious condition. The following drug classes are of particular concern:
- SSRIs (selective serotonin reuptake inhibitors): fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram
- SNRIs (serotonin-norepinephrine reuptake inhibitors): venlafaxine, duloxetine, desvenlafaxine, milnacipran
- MAOIs (monoamine oxidase inhibitors): phenelzine, tranylcypromine, selegiline
- Other serotonergic agents: tramadol, fentanyl, lithium, triptans, St. John's Wort
QT-Prolonging Medications (Major Interaction)
Palonosetron can prolong the QT interval, and concurrent use with other QT-prolonging drugs may have additive effects, increasing the risk of serious cardiac arrhythmias including torsades de pointes. Medications of concern include certain antiarrhythmics (amiodarone, sotalol), some antibiotics (moxifloxacin, erythromycin), antipsychotics (haloperidol, ziprasidone), and other antiemetics (droperidol).
| Drug / Class | Interaction Type | Risk | Clinical Action |
|---|---|---|---|
| SSRIs (e.g., fluoxetine, sertraline) | Serotonergic | Serotonin syndrome | Monitor closely; use with caution |
| SNRIs (e.g., venlafaxine, duloxetine) | Serotonergic | Serotonin syndrome | Monitor closely; use with caution |
| QT-prolonging drugs (e.g., amiodarone) | Cardiac | QT prolongation, arrhythmias | ECG monitoring recommended |
| Tramadol, fentanyl | Serotonergic | Serotonin syndrome | Monitor for serotonin symptoms |
| Lithium | Serotonergic | Serotonin syndrome | Monitor lithium levels and symptoms |
| Aprepitant / fosaprepitant | Pharmacodynamic | Minimal — complementary action | Safe to combine; guideline-recommended |
| Dexamethasone | Pharmacodynamic | Minimal — synergistic benefit | Routine combination; enhances efficacy |
It is important to note that palonosetron is routinely combined with corticosteroids (particularly dexamethasone) and NK1 receptor antagonists (such as aprepitant or fosaprepitant) as part of guideline-recommended antiemetic regimens. These combinations are considered safe and synergistic, providing superior CINV prevention compared to any single agent alone.
What Is the Correct Dosage of Palonosetron Fresenius Kabi?
Adults receive a single 250 microgram intravenous bolus dose approximately 30 minutes before chemotherapy. Children receive 20 micrograms per kilogram body weight (maximum 1500 micrograms) as a 15-minute intravenous infusion before chemotherapy.
Palonosetron is administered exclusively by healthcare professionals in a clinical setting. The dosing schedule is straightforward due to the drug's long half-life, which allows single-dose administration per chemotherapy cycle. It is critical that palonosetron is not administered on consecutive days unless a new chemotherapy cycle is being initiated.
Adults
Adult Dosing
The recommended dose for adults is 250 micrograms of palonosetron, administered as a single intravenous bolus injection over 30 seconds, approximately 30 minutes before the start of chemotherapy. No dose adjustment is required based on age, gender, or race. Patients with mild to moderate hepatic or renal impairment do not require dose adjustments. There are limited data for patients with severe hepatic or renal impairment.
Children and Adolescents (1 Month to 17 Years)
Pediatric Dosing
The recommended dose for pediatric patients is 20 micrograms per kilogram of body weight (maximum total dose: 1500 micrograms), administered as a single intravenous infusion over 15 minutes, starting approximately 30 minutes before chemotherapy. The dose is calculated by the treating physician based on the child's current body weight.
Elderly Patients
Elderly Dosing
No dose adjustment is necessary for elderly patients. Clinical studies have included patients over 65 years of age and have not identified age-related differences in safety or efficacy. Standard adult dosing of 250 micrograms applies.
| Patient Group | Dose | Route | Administration |
|---|---|---|---|
| Adults | 250 micrograms | IV bolus | Over 30 seconds, 30 min before chemo |
| Children (1 month–17 years) | 20 mcg/kg (max 1500 mcg) | IV infusion | Over 15 minutes, 30 min before chemo |
| Elderly (≥65 years) | 250 micrograms | IV bolus | No dose adjustment required |
| Renal impairment (mild–moderate) | 250 micrograms | IV bolus | No dose adjustment required |
| Hepatic impairment (mild–moderate) | 250 micrograms | IV bolus | No dose adjustment required |
Missed Dose
Since palonosetron is administered by healthcare professionals in a clinical setting prior to each chemotherapy cycle, missed doses are uncommon. If the dose is not administered before chemotherapy begins, it should be given as soon as possible. The antiemetic benefit may be reduced if administration is significantly delayed. Palonosetron should not be given after chemotherapy has been completed, as its primary mechanism of action is preventive rather than therapeutic for established nausea and vomiting.
Overdose
There is no specific antidote for palonosetron overdose. In clinical trials, doses up to 90 micrograms per kilogram (approximately 6 mg) have been administered without dose-limiting adverse effects. In the event of overdose, treatment should be symptomatic and supportive. Dialysis is unlikely to be effective due to palonosetron's large volume of distribution.
Palonosetron Fresenius Kabi must not be mixed with other medicinal products. Each vial is intended for single use only; any unused solution should be discarded according to local pharmaceutical waste guidelines.
What Are the Side Effects of Palonosetron Fresenius Kabi?
The most common side effects of palonosetron are headache, dizziness, constipation, and diarrhea. Serious side effects are rare but can include QT prolongation on ECG. Most side effects are mild and transient.
Like all medicines, palonosetron can cause side effects, although not everybody experiences them. Clinical trials and post-marketing surveillance have identified the following adverse reactions, categorized by frequency. Most reported side effects are mild to moderate in severity and resolve without specific treatment.
Common Side Effects
May affect up to 1 in 10 patients
- Headache
- Dizziness
- Constipation
- Diarrhea
Uncommon Side Effects
May affect up to 1 in 100 patients
- High or low blood pressure (hypertension/hypotension)
- Abnormal heart rate or insufficient blood supply to the heart
- Abnormally high or low levels of potassium in the blood
- High blood sugar levels or sugar in urine
- Low calcium levels in the blood
- High levels of the pigment bilirubin in the blood
- Elevated liver enzymes
- Abnormal ECG (QT prolongation)
Very Rare Side Effects
May affect up to 1 in 10,000 patients
- Burning, pain, or redness at the injection site
Additional Side Effects in Children and Adolescents
The safety profile of palonosetron in pediatric patients is generally consistent with that observed in adults, though some additional side effects have been reported:
Common in Children
May affect up to 1 in 10 patients
- Headache
Uncommon in Children
May affect up to 1 in 100 patients
- Dizziness
- Involuntary jerky body movements (dyskinesia)
- Abnormal heart rate
- Cough or shortness of breath
- Nosebleed (epistaxis)
- Itchy skin rash or hives (urticaria)
- Fever
- Pain at the infusion site
Contact your healthcare provider or seek emergency care immediately if you experience signs of a severe allergic reaction (difficulty breathing, swelling of the face, lips, tongue, or throat, severe skin rash), signs of serotonin syndrome (agitation, confusion, rapid heartbeat, fever, muscle stiffness, twitching), or irregular heartbeat with lightheadedness or fainting.
The overall safety profile of palonosetron is considered favorable. In pivotal clinical trials comparing palonosetron with first-generation 5-HT3 antagonists (ondansetron, dolasetron), the incidence of adverse events was comparable across treatment groups. Importantly, the rate of headache — the most common side effect — was similar to or lower than that observed with older agents in the same class.
If you experience any side effects not listed above, or if any of the described side effects become severe or persistent, inform your healthcare provider. You can also report suspected adverse reactions through your national pharmacovigilance reporting system to help monitor the safety of medicines.
How Should Palonosetron Fresenius Kabi Be Stored?
Palonosetron Fresenius Kabi does not require special storage conditions. Keep out of sight and reach of children. Do not use after the expiry date or if the solution is not clear or contains visible particles.
Palonosetron Fresenius Kabi solution for injection does not require any special storage conditions regarding temperature or light protection. However, the following general storage guidelines should be observed:
- Keep out of sight and reach of children: As with all medications, store securely and inaccessibly to prevent accidental exposure in children.
- Check the expiry date: Do not use this medicine after the expiry date stated on the vial label and outer carton. The expiry date refers to the last day of the indicated month.
- Inspect before use: Do not use the solution if it is not clear and colorless or if it contains visible particles. A qualified healthcare professional should inspect the solution before administration.
- Single use only: Each vial is intended for one-time use. Any unused solution remaining in the vial after withdrawal of the required dose must be discarded. Do not save or re-use leftover medication.
- Disposal: Unused medicine and pharmaceutical waste should be disposed of in accordance with local regulations for cytotoxic and pharmaceutical waste handling.
In clinical settings, storage and handling of palonosetron are managed by pharmacy staff in accordance with institutional protocols. Patients do not typically handle or store this medication at home, as it is administered exclusively in healthcare facilities.
What Does Palonosetron Fresenius Kabi Contain?
Each 5 mL vial contains 250 micrograms of palonosetron (as hydrochloride), equivalent to 50 micrograms per mL. It is a clear, colorless solution supplied in single-use glass vials.
Active Ingredient
The active substance is palonosetron, present as palonosetron hydrochloride. Each milliliter of solution contains 50 micrograms of palonosetron. Each 5 mL vial therefore contains a total of 250 micrograms of palonosetron, which is the standard single adult dose.
Inactive Ingredients (Excipients)
The formulation contains the following excipients, each serving a specific pharmaceutical function:
- Mannitol (E421): Acts as a tonicity agent to ensure the solution is isotonic with blood, preventing discomfort or hemolysis during intravenous administration.
- Disodium edetate: Functions as a chelating agent to enhance the chemical stability of the formulation by binding trace metal ions.
- Sodium citrate (E331): Serves as a buffering agent to maintain the pH of the solution within the optimal range for stability and tolerability.
- Citric acid (E330): Works in conjunction with sodium citrate as part of the buffer system.
- Water for injections: The solvent, meeting pharmacopoeial standards for parenteral preparations.
- Sodium hydroxide and hydrochloric acid: Used for pH adjustment during manufacturing to achieve the target pH range.
Packaging
Palonosetron Fresenius Kabi is supplied as a clear, colorless solution for injection in Type I glass vials sealed with a halobutyl rubber stopper and an aluminum-plastic flip-off cap. The product is available in pack sizes of 1 or 10 vials. Not all pack sizes may be marketed in every country.
Frequently Asked Questions About Palonosetron Fresenius Kabi
Palonosetron is used to prevent nausea and vomiting caused by cancer chemotherapy (chemotherapy-induced nausea and vomiting, or CINV). It belongs to a class of medications called serotonin 5-HT3 receptor antagonists that block the chemical messenger serotonin, which triggers the vomiting reflex during chemotherapy. It is approved for use in adults, adolescents, and children over one month of age.
Palonosetron has an exceptionally long half-life of approximately 40 hours, making it the longest-acting 5-HT3 receptor antagonist available. This means a single intravenous dose can provide antiemetic protection for up to 5 days, covering both the acute phase (first 24 hours) and the delayed phase (days 2–5) of chemotherapy-induced nausea and vomiting. By comparison, ondansetron has a half-life of only about 4 hours.
The most common side effects of palonosetron are headache, dizziness, constipation, and diarrhea. These affect up to 1 in 10 patients and are generally mild and temporary. Less common side effects include blood pressure changes, abnormal heart rate, and altered blood chemistry. Serious side effects such as QT prolongation are uncommon. The overall side effect profile is comparable to other 5-HT3 antagonists.
Yes, palonosetron is approved for use in children and adolescents from 1 month to 17 years of age. The pediatric dose is weight-based at 20 micrograms per kilogram of body weight, with a maximum total dose of 1500 micrograms. Unlike in adults where it is given as a bolus injection, in children it is administered as an intravenous infusion over 15 minutes. Clinical trials have demonstrated its safety and efficacy in the pediatric population.
Palonosetron is a second-generation 5-HT3 receptor antagonist with several advantages over first-generation agents like ondansetron. Its half-life is approximately 40 hours versus 4 hours for ondansetron, allowing single-dose administration per chemotherapy cycle. It has a 30-fold higher binding affinity for the 5-HT3 receptor and demonstrates unique allosteric binding and receptor internalization properties. Clinical trials have shown superior efficacy particularly in preventing delayed-phase CINV (24–120 hours after chemotherapy).
The safety of palonosetron during pregnancy has not been established, and it should only be used if the potential benefit justifies the potential risk to the fetus. It is unknown whether palonosetron passes into breast milk. Women who are pregnant, planning to become pregnant, or breastfeeding should discuss the risks and benefits with their healthcare provider before receiving this medication.
References and Sources
This article is based on evidence from the following peer-reviewed and authoritative sources. All medical claims conform to Evidence Level 1A standards based on systematic reviews and international clinical guidelines.
- MASCC/ESMO Antiemetic Guideline 2023. Multinational Association of Supportive Care in Cancer / European Society for Medical Oncology. Annals of Oncology. 2023. doi:10.1016/j.annonc.2023.10.001
- Hesketh PJ, Kris MG, Basch E, et al. Antiemetics: ASCO Guideline Update. Journal of Clinical Oncology. 2023;41(28):4413-4441.
- Gralla R, Lichinitser M, Van Der Vegt S, et al. Palonosetron improves prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy: results of a double-blind randomized phase III trial. Ann Oncol. 2003;14(10):1570-1577.
- Aapro M, Gralla R, Roila F. Palonosetron: a second-generation 5-HT3 receptor antagonist. Ann Oncol. 2006;17(supplement 2):ii19-ii22.
- European Medicines Agency (EMA). Summary of Product Characteristics: Palonosetron. Last updated 2023.
- World Health Organization (WHO). WHO Model List of Essential Medicines – 23rd List. 2023.
- National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Antiemesis. Version 1.2024.
- Rojas C, Raje M, Tsukamoto T, Slusher BS. Molecular mechanisms of 5-HT3 and NK1 receptor antagonists in prevention of emesis. Eur J Pharmacol. 2014;722:26-37.
- Navari RM. Palonosetron for the prevention of chemotherapy-induced nausea and vomiting in patients with cancer. Future Oncol. 2010;6(7):1073-1084.
- Sepulveda-Vildosola AC, Betanzos-Cabrera Y, Lastiri GG, et al. Palonosetron hydrochloride is an effective and safe option to prevent chemotherapy-induced nausea and vomiting in children. Arch Med Res. 2008;39(6):601-606.
About This Article
This article was written and medically reviewed by the iMedic Medical Editorial Team, a group of licensed specialist physicians with expertise in oncology, clinical pharmacology, and supportive care in cancer treatment.
Medical Review Process
All content undergoes rigorous medical review following the GRADE evidence framework. Sources include international guidelines from MASCC/ESMO, ASCO, NCCN, WHO, and EMA, as well as peer-reviewed clinical trials published in high-impact medical journals.
Editorial Independence
iMedic maintains strict editorial independence. This content has no commercial funding and is free from pharmaceutical industry influence. Our editorial team has no conflicts of interest related to the medications described.
Published: | Last reviewed: | Next review due: