Granisetron 4mg/4ml Inj, 4ml
It is used to prevent upset stomach and throwing up.
Drug Class
Antiemetic
Pharmacologic Class
Selective 5-HT3 Receptor Antagonist
Pregnancy Category
B
FDA Approved
Dec 1993
DEA Schedule
Not Controlled
Overview
What is this medicine?
Granisetron is a medicine given by injection to help prevent nausea and vomiting. It works by blocking a natural substance in your body (serotonin) that can cause you to feel sick, especially after chemotherapy or surgery.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This drug is administered via intravenous injection.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Report any unusual side effects, especially headache, constipation, or dizziness.
- Stay hydrated, especially if experiencing vomiting or diarrhea.
- Avoid driving or operating machinery if you experience dizziness or fatigue.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For CINV: 10 mcg/kg IV (or 1 mg IV) administered over 5 minutes, 30 minutes prior to chemotherapy. For PONV: 1 mg IV administered over 30 seconds, prior to induction of anesthesia or immediately pre-operatively.
Dose Range:
0.01 - 9 mg
Condition-Specific Dosing:
Chemotherapy-Induced Nausea and Vomiting (CINV):
10 mcg/kg IV (up to 1 mg) administered over 5 minutes, 30 minutes prior to chemotherapy. A single dose is usually sufficient. Maximum 9 mg/day.
Postoperative Nausea and Vomiting (PONV):
1 mg IV administered over 30 seconds, prior to induction of anesthesia or immediately pre-operatively. A single dose is usually sufficient.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For CINV (2-16 years): 10 mcg/kg IV (up to 1 mg) administered over 5 minutes, 30 minutes prior to chemotherapy.
Adolescent:
For CINV (2-16 years): 10 mcg/kg IV (up to 1 mg) administered over 5 minutes, 30 minutes prior to chemotherapy.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment generally required.
Moderate:
No dose adjustment generally required.
Severe:
No dose adjustment generally required.
Dialysis:
No specific recommendations; granisetron is not significantly removed by hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment generally required.
Moderate:
No dose adjustment generally required.
Severe:
Caution advised due to increased plasma concentrations and half-life; however, no specific dose adjustment recommendations are provided in the labeling. Monitor for adverse effects.
Pharmacology
Mechanism of Action
Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist. Serotonin 5-HT3 receptors are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema. Chemotherapeutic agents and radiation therapy release serotonin from enterochromaffin cells in the small intestine, which then activates 5-HT3 receptors, initiating the vomiting reflex. Granisetron blocks this action, preventing nausea and vomiting.
Pharmacokinetics
Absorption:
Bioavailability:
100% (IV)
Tmax:
Not applicable (IV)
FoodEffect:
Not applicable (IV)
Distribution:
Vd:
2-3 L/kg
ProteinBinding:
Approximately 65%
CnssPenetration:
Limited, but acts on central 5-HT3 receptors in the CTZ.
Elimination:
HalfLife:
Approximately 9 hours (range 3-15 hours)
Clearance:
Approximately 400 mL/min
ExcretionRoute:
Renal (urine) and fecal (bile)
Unchanged:
Approximately 12% (urine)
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes for IV administration)
PeakEffect:
Within minutes of administration
DurationOfAction:
Up to 24 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Chest pain or pressure
Fast or abnormal heartbeat
Shortness of breath
Stomach pain
Swelling of the belly
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Additionally, a severe and potentially life-threatening condition called serotonin syndrome may occur, especially if you are taking certain other medications. If you experience any of the following symptoms, contact your doctor immediately:
Agitation
Changes in balance
Confusion
Hallucinations
Fever
Fast or abnormal heartbeat
Flushing
Muscle twitching or stiffness
Seizures
Shivering or shaking
Excessive sweating
Severe diarrhea
Upset stomach
Vomiting
Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Diarrhea or constipation
Heartburn
Decreased appetite
Trouble sleeping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Chest pain or pressure
Fast or abnormal heartbeat
Shortness of breath
Stomach pain
Swelling of the belly
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling extremely tired or weak
Additionally, a severe and potentially life-threatening condition called serotonin syndrome may occur, especially if you are taking certain other medications. If you experience any of the following symptoms, contact your doctor immediately:
Agitation
Changes in balance
Confusion
Hallucinations
Fever
Fast or abnormal heartbeat
Flushing
Muscle twitching or stiffness
Seizures
Shivering or shaking
Excessive sweating
Severe diarrhea
Upset stomach
Vomiting
Severe headache
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Diarrhea or constipation
Heartburn
Decreased appetite
Trouble sleeping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe headache
- Severe constipation or abdominal pain
- Dizziness or lightheadedness, especially when standing up
- Fast or irregular heartbeat (palpitations)
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
- Symptoms of serotonin syndrome (agitation, confusion, hallucinations, rapid heart rate, sweating, muscle stiffness or twitching, loss of coordination, nausea, vomiting, diarrhea)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, any of its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking another medication that contains the same active ingredient as this drug.
If you are taking apomorphine, as this may interact with this medication.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes:
All prescription medications you are currently taking
Over-the-counter (OTC) medications
Natural products, such as herbal supplements
* Vitamins
Additionally, inform your doctor about any existing health problems. It is vital to verify that it is safe to take this medication with all of your current medications and health conditions. Do not start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, any of its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking another medication that contains the same active ingredient as this drug.
If you are taking apomorphine, as this may interact with this medication.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. This includes:
All prescription medications you are currently taking
Over-the-counter (OTC) medications
Natural products, such as herbal supplements
* Vitamins
Additionally, inform your doctor about any existing health problems. It is vital to verify that it is safe to take this medication with all of your current medications and health conditions. Do not start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require your full attention, such as driving, wait until you understand how this drug affects you.
Be aware that some formulations of this medication may contain benzyl alcohol. If possible, it is recommended to avoid using products with benzyl alcohol in newborns and infants, as certain doses of benzyl alcohol can cause severe side effects in these children, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if this product contains benzyl alcohol.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Be aware that some formulations of this medication may contain benzyl alcohol. If possible, it is recommended to avoid using products with benzyl alcohol in newborns and infants, as certain doses of benzyl alcohol can cause severe side effects in these children, particularly when combined with other medications containing benzyl alcohol. Consult your doctor to determine if this product contains benzyl alcohol.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Headache
- Constipation
- Mild hypotension
- QT prolongation (rare, but possible with very high doses)
What to Do:
There is no specific antidote for granisetron overdose. Treatment should be symptomatic and supportive. Call 1-800-222-1222 (Poison Control Center) immediately for advice.
Drug Interactions
Major Interactions
- QT-prolonging agents (e.g., amiodarone, sotalol, quinidine, procainamide, disopyramide, dofetilide, cisapride, pimozide, thioridazine, ziprasidone, moxifloxacin, erythromycin, haloperidol, methadone, ondansetron, dolasetron)
- Serotonergic drugs (e.g., SSRIs, SNRIs, TCAs, MAOIs, triptans, fentanyl, tramadol, linezolid, St. John's Wort)
Moderate Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin)
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir)
Monitoring
Baseline Monitoring
Electrolytes (Potassium, Magnesium)
Rationale: To identify pre-existing electrolyte imbalances that may increase the risk of QT prolongation.
Timing: Prior to administration, especially in patients at risk for QT prolongation.
Electrocardiogram (ECG)
Rationale: To assess baseline QTc interval, particularly in patients with pre-existing cardiac conditions, electrolyte abnormalities, or those receiving other QT-prolonging drugs.
Timing: Prior to administration, if risk factors for QT prolongation are present.
Routine Monitoring
Signs and symptoms of Serotonin Syndrome
Frequency: Continuously during and after administration, especially if co-administered with other serotonergic drugs.
Target: Absence of symptoms (e.g., mental status changes, autonomic instability, neuromuscular abnormalities, GI symptoms)
Action Threshold: If symptoms develop, discontinue granisetron and initiate supportive treatment.
Nausea and Vomiting control
Frequency: As needed, post-administration.
Target: Effective control of nausea and vomiting.
Action Threshold: If inadequate control, consider alternative or adjunctive antiemetic therapy.
Symptom Monitoring
- Headache
- Constipation
- Asthenia
- Diarrhea
- Fever
- Dizziness
- Insomnia
- Anxiety
- QT prolongation (palpitations, syncope)
- Serotonin syndrome (agitation, hallucinations, rapid heart rate, fever, sweating, muscle rigidity, twitching, loss of coordination, nausea, vomiting, diarrhea)
Special Patient Groups
Pregnancy
Granisetron is classified as Pregnancy Category B. Animal reproduction studies have shown no evidence of harm to the fetus. There are no adequate and well-controlled studies in pregnant women. Granisetron should be used during pregnancy only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Limited human data, animal studies show no increased risk of malformations.
Second Trimester:
Limited human data, animal studies show no increased risk of malformations.
Third Trimester:
Limited human data, animal studies show no increased risk of malformations.
Lactation
It is not known whether granisetron is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when granisetron is administered to a nursing woman. The decision to discontinue nursing or discontinue the drug should take into account the importance of the drug to the mother.
Infant Risk:
Unknown. Potential for adverse effects on the breastfed infant cannot be excluded. Consider monitoring the infant for potential side effects (e.g., constipation, sedation).
Pediatric Use
Granisetron injection is approved for the prevention of nausea and vomiting associated with chemotherapy in pediatric patients 2 years of age and older. Safety and effectiveness in pediatric patients younger than 2 years of age have not been established.
Geriatric Use
No dosage adjustment is recommended based on age alone. However, elderly patients may have reduced renal or hepatic function, which could affect drug clearance. Monitor for adverse effects and consider co-morbidities and concomitant medications.
Clinical Information
Clinical Pearls
- Granisetron is generally well-tolerated with a low incidence of side effects, making it a preferred choice for CINV and PONV.
- Administer IV granisetron slowly (over 5 minutes for CINV, 30 seconds for PONV) to minimize potential for adverse reactions.
- While generally not requiring dose adjustment in renal or hepatic impairment, caution is advised in severe hepatic impairment due to potential for increased plasma concentrations.
- Be mindful of potential for QT prolongation, especially in patients with pre-existing cardiac conditions, electrolyte imbalances, or those on other QT-prolonging medications.
- Educate patients and caregivers about the signs and symptoms of serotonin syndrome, particularly if the patient is on other serotonergic agents.
Alternative Therapies
- Ondansetron (Zofran)
- Palonosetron (Aloxi)
- Dolasetron (Anzemet)
- Netupitant/Palonosetron (Akynzeo)
- Rolapitant (Varubi)
- Aprepitant (Emend)
- Fosaprepitant (Emend IV)
- Dexamethasone
- Prochlorperazine
- Metoclopramide
Cost & Coverage
Average Cost:
Not available per 4mg/4ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, avoid flushing medications down the toilet or pouring them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for advice. Additionally, you may want to inquire about potential drug take-back programs in your area. Some medications may come with a separate patient information leaflet, so it is a good idea to check with your pharmacist. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek medical attention. Be prepared to provide information about the medication taken, the amount, and the time it was taken to ensure prompt and effective treatment.