Granisetronum

Granisetronum Uses, Dosage, Side Effects, Food Interaction and all others data.

Granisetronum 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-HT3 type 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-HT3 receptors. This evokes vagal afferent discharge, inducing vomiting. Animal studies demonstrate that, in binding to 5-HT3 receptors, 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 on blood pressure, heart rate or ECG. No evidence of an effect on plasma prolactin or aldosterone concentrations has been found in other studies.

Granisetronum is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. Granisetronum 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.

Trade Name Granisetronum
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
Type
Formula C18H24N4O
Weight Average: 312.417
Monoisotopic: 312.195011409
Protein binding

65%

Groups Approved, Investigational
Therapeutic Class  
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Granisetronum
Granisetronum

Uses

Granisetronum 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.

Granisetronum 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.

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

How Granisetronum works

Granisetronum 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.

Dosage

Granisetronum dosage

Tablet-

Emetogenic Chemotherapy: The recommended adult dosage of oral Granisetronumis 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.

Injection-

Chemotherapy Induced Nausea and Vomiting:

  • Adults: The recommended dosage for Granisetronum Injection is 10 mcg/kg administered intravenously within 30 minutes before initiation of chemotherapy, and only on the day(s) chemotherapy is given. Granisetronum 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, Granisetronum 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 Granisetronum 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 Granisetronum undiluted, administered intravenously over 30 seconds.
  • Paediatric Patients: Safety and effectiveness of Granisetronum 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.

Toxicity

LD50>2000 mg/kg (rat, oral)

Precaution

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.

Interaction

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.

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

Clearance

  • 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.

Contraindication

Granisetronum 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

You find simplified version here Granisetronum

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

FAQ

What is Granisetronum used for?

Granisetronum 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 Granisetronum?

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

How does Granisetronum work?

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

What are the common side effects of Granisetronum?

Common side effects of Granisetronum 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 Granisetronum safe during pregnancy?

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

Is Granisetronum safe during breastfeeding?

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

Can I drink alcohol with Granisetronum?

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

Can I drive after taking Granisetronum?

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

How long does Granisetronum take to work?

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

How long does Granisetronum stay in my system?

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

When should be taken of Granisetronum?

Granisetronum 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 Granisetronum?

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

Who should not take Granisetronum?

You should not take Granisetronum if you are allergic to it. To make sure Granisetronum 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 Granisetronum?

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

Does Granisetronum cause constipation?

The most common side-effects are constipation and headache.

Does Granisetronum make me sleepy?

This Granisetronum may make you dizzy or drowsy.

Can I just stop taking Granisetronum?

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

Can Granisetronum affects my heart ?

Granisetronum 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 Granisetronum increase blood pressure?

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

*** Taking medicines without doctor's advice can cause long-term problems.
Share