Granisetron Uses, Dosage, Side Effects, FAQ - MedicinesFAQ (2023)

Granisetron Oral Tablet, Intravenous Solution, Subcutaneous Suspension, Extended Release, Injection, Transdermal Film, Transdermal, Tablet

Granisetron is a highly selective 5-HT3 receptor antagonist with little or no affinity for other serotonin receptors. It blocks serotonin peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone.

Serotonin receptors of the 5-HT3type are located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema. During chemotherapy that induces vomiting, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT3receptors. This evokes vagal afferent discharge, inducing vomiting. Animal studies demonstrate that, in binding to 5-HT3receptors, granisetron blocks serotonin stimulation and subsequent vomiting after emetogenic stimuli such as cisplatin. In the ferret animal model, a single granisetron injection prevented vomiting due to high-dose cisplatin or arrested vomiting within 5 to 30 seconds.

In most human studies, granisetron has had little effect onblood pressure,heart rateor ECG. No evidence of an effect on plasma prolactin oraldosteroneconcentrations has been found in other studies.

Granisetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. Granisetron has little or no affinity for other serotonin receptors, including 5-HT 1 , 5-HT 1A , 5-HT 1B/C , or 5-HT 2 ; for alpha 1 -, alpha 2 -, or beta-adrenoreceptors; for dopamine D 2 receptors; for histamine H 1 receptors; for benzodiazepine receptors; for picrotoxin receptors; or for opioid receptors. In most human studies, granisetron has had little effect on blood pressure, heart rate, or electrocardiogram (ECG). The drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.


Granisetron Tablet is used for: Nausea and vomiting associated with initial and repeat course of emetogenic cancer therapy, including high dose of cisplatin. Nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation.

Granisetron Injection is used for: The prevention of nausea and vomitng associated with initial and repeat courses of emetogenic cancer chemotherapy, therapy including high dose cisplatin. The prevention and treatment of post operative nausea and vomiting.

Granisetron is also used to associated treatment for these conditions: Nausea and vomiting

How Granisetron works

Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.


Trade Name Granisetron
Availability Prescription only
Generic Granisetron
Granisetron Other Names Granisétron, Granisetrón, Granisetron, Granisetronum
Related Drugs lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide, Reglan, amisulpride, droperidol, Zofran ODT
Weight 1mg, , 0.1mg/ml, 1mg/ml, 10mg/0.4ml, 3.1mg/24hr
Type Oral Tablet, Intravenous Solution, Subcutaneous Suspension, Extended Release, Injection, Transdermal Film, Transdermal, Tablet
Formula C18H24N4O
Weight Average: 312.417
Monoisotopic: 312.195011409
Protein binding


Groups Approved, Investigational
Therapeutic Class
Manufacturer Mylan, Otto Pharmaceuticals, Pertiwi Agung
Available Country United Kingdom, United States, Indonesia, Netherlands
Last Updated: June 7, 2022 at 8:54 pm


Granisetron Uses, Dosage, Side Effects, FAQ - MedicinesFAQ (1)

Table Of contents

  • Granisetron
  • Uses
  • Dosage
  • Side Effect
  • Precautions
  • Interactions
  • Uses during Pregnancy
  • Uses during Breastfeeding
  • Accute Overdose
  • Food Interaction
  • Half Life
  • Volume of Distribution
  • Clearance
  • Interaction With other Medicine
  • Contradiction
  • Storage


Granisetron dosage


Emetogenic Chemotherapy: The recommended adult dosage of oral Granisetronis 2 mg once daily or 1 mg twice daily. In the 2 mg once-daily regimen, two 1 mg tablets is given up to 1 hour before chemotherapy. In the 1 mg twice-daily regimen, the first 1 mg tablet is given up to 1 hour before chemotherapy, and the second tabletis given 12 hours after the first. Either regimen is administered only on the day(s) chemotherapy is given. Continued treatment, while not on chemotherapy, has not been found to be useful.


Chemotherapy Induced Nausea and Vomiting:

  • Adults: The recommended dosage for Granisetron Injection is 10 mcg/kg administered intravenously within 30 minutes before initiation of chemotherapy, and only on the day(s) chemotherapy is given. Granisetron Injection may be administered intravenously either undiluted over 30 seconds, or diluted with 0.9% Sodium Chloride or 5% Dextrose and infused over 5 minutes. As a general precaution, Granisetron Injection should not be mixed in solution with other drugs.
  • Paediatric Patients: The recommended dose in paediatric patients 2 to 16 years o f age is 10 mcg/kg. Paediatric patients under 2 years o f age have not beenstudied.
  • Geriatric Patients, Renal Failure Patients or Hepatically Impaired Patients: No dosage adjustment is required.

Treatment of Postoperative Nausea and Vomiting:

  • Adults: The recommended dosage for prevention of postoperative nausea and vomiting is, a single dose of 1 mg of Granisetron should be diluted to 5 ml andadministered as a slow intravenous injection (over 30 seconds). Administration should be completed prior toinduction of anesthesia. The recommended dosage for the treatment of nausea and vomiting after surgery is 1 mg of Granisetron undiluted, administered intravenously over 30 seconds.
  • Paediatric Patients: Safety and effectiveness of Granisetron Injection have not been established in paediatric patients for the prevention or treatment of post operative nausea or vomiting.
  • Geriatricpatients, Renal Failure Patients or Hepatically Impaired Patients: No dosage adjustment is required.

Side Effects

Headache, insomnia, constipation, diarrhoea, elevated hepatic transaminases; QT prolongation; bradycardia, palpitations, sick sinus syndrome, chest pain. Application site reactions (transdermal): Rash, pain, erythema, pruritus, irritation, burn, vesicles, urticaria, discolouration; patch non-adhesion.


LD50>2000 mg/kg (rat, oral)


Patient with cardiac co-morbidities, on cardiotoxic chemotherapy and/or woth concomitant electrolyte abnormalities. May mask progressive ileus and/or gastric distention. Childn. Pregnancy and lactation.


Induced metabolism with phenobarbital. Risk of serotonin syndrome with other serotonergic agents e.g. SSRIs, and serotonin and norepinephrine reuptake inhibitors (SNRIs). Altered clearance with CYP enzyme inducers or inhibitors. Concomitant use with drugs known to prolong QT interval may result in clinical consequences.

Food Interaction

  • Take with or without food. The absorption is unaffected by food.

Granisetron Drug Interaction

Major: fentanyl, fentanyl

Minor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim

Unknown: diphenhydramine, diphenhydramine, pregabalin, pregabalin, acetaminophen, acetaminophen, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, ondansetron, ondansetron

Elimination Route

Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.

Half Life

4-6 hours in healthy patients, 9-12 hours in cancer patients


  • 0.52 L/h/kg [Cancer Patients with 1 mg bid for 7 days]
  • 0.41 L/h/kg [Healthy subject with a single 1 mg dose]

Elimination Route

The remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces.

Pregnancy & Breastfeeding use

Pregnancy: Category B. No evidence of impaired fertility or harm to the animal fetus have been found. However, this drug may be used in pregnancy only if clearly needed.

Lactation: It is not known whether granisetron is excreted in human milk. So cautions hould be exercised when granisetron is administered to a nursing mother.


Granisetron is contraindicated in patients with known hypersensitivity to granisetron.

Special Warning

Pediatric Uses: Safety and effectiveness of granisetron in paediatric patients under 2 years have not been established.

Geriatric use: Efficacy and safety were maintained with increasing age

Acute Overdose

Symptoms: Mild headache.

Management: Symptomatic treatment.

Storage Condition

Store between 15-30°C. Protect from light.

Innovators Monograph

Granisetron contains Granisetron see full prescribing information from innovator Granisetron Monograph, Granisetron MSDS, Granisetron FDA label


What is Granisetron used for?

Granisetron is a serotonin 5-HT₃ receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata.

How safe is Granisetron?

Granisetron appears to be a safe and effective drug for pediatric patients receiving emetogenic chemotherapy.

How does Granisetron work?

Granisetron works by blocking serotonin, a natural substance in the body that causes nausea and vomiting.

What are the common side effects of Granisetron?

Common side effects of Granisetron are diarrhea, constipation, stomach pain, weakness, headache, fever, dizziness, drowsiness, trouble sleeping, and anxiety may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Is Granisetron safe during pregnancy?

Current guidelines suggest that Granisetron is an optional treatment for nausea and vomiting in pregnancy (NVP) despite lack of evidence to support fetal safety.

Is Granisetron safe during breastfeeding?

No information is available on the use of Granisetron during breastfeeding. Until more data become available, Granisetron should be used with caution during breastfeeding.

Can I drink alcohol with Granisetron?

Your doctor may suggest that you avoid alcohol or reduce the amount of alcohol you drink while you are taking Granisetron.

Can I drive after taking Granisetron?

Granisetron may make you feel dizzy that affects your mental ability. Do not drive or operate machinery if you experience dizziness.

How long does Granisetron take to work?

When taken to prevent nausea and vomiting caused by radiation, Granisetron is usually taken within 1 hour before treatment.

How long does Granisetron stay in my system?

Granisetron is a long-acting medication that can stay in your system for a week after just one dose.

When should be taken of Granisetron?

Granisetron is usually taken 1 hour before chemotherapy is begun. A second dose may be taken 12 hours after the first dose depending on the strength.

How often can I take Granisetron?

The recommended adult dosage of oral is 2 mg once daily or 1 mg twice daily.

Who should not take Granisetron?

You should not take Granisetron if you are allergic to it. To make sure Granisetron is safe for you, tell your doctor if you have: heart disease; a heart rhythm disorder; a personal or family history of long QT syndrome; an electrolyte imbalance (such as low levels of potassium or magnesium in your blood); or if you have recently had stomach or intestinal surgery.

What happens if I miss a dose?

Tell your doctor if you forget to take your dose within 1 hour before chemotherapy or radiation. Do not take extra medicine to make up the missed dose.

What happen if I overdose on Granisetron?

If you take too much Granisetron, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

Does Granisetron cause constipation?

The most common side-effects are constipation and headache.

Does Granisetron make me sleepy?

This Granisetron may make you dizzy or drowsy.

Can I just stop taking Granisetron?

Do not exceed the recommended dose. Treatment with Granisetron Tablets should not be withdrawn suddenly, particularly if the medicine has been used by the patient for a long time.

Can Granisetron affects my heart ?

Granisetron can cause a serious heart problem, especially if you use certain medicines at the same time, including antibiotics, antidepressants, heart rhythm medicine, antipsychotic medicines, and medicines to treat cancer, malaria, HIV or AIDS.

Can Granisetron increase blood pressure?

In most human studies, Granisetron has had little effect on blood pressure, heart rate or ECG.

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