Setron(Granisetron)
Setron(Granisetron) Uses, Dosage, Side Effects, Food Interaction and all others data.
Setron(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-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.
Setron(Granisetron) is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. Setron(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.
| Trade Name | Setron(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 |
| Type | |
| Formula | C18H24N4O |
| Weight | Average: 312.417 Monoisotopic: 312.195011409 |
| Protein binding | 65% |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Israel, Taiwan, Turkey |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Setron(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.
Setron(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.
Setron(Granisetron) is also used to associated treatment for these conditions: Nausea and vomiting
How Setron(Granisetron) works
Setron(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.
Dosage
Setron(Granisetron) dosage
Tablet-
Emetogenic Chemotherapy: The recommended adult dosage of oral Setron(Granisetron)is 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 Setron(Granisetron) Injection is 10 mcg/kg administered intravenously within 30 minutes before initiation of chemotherapy, and only on the day(s) chemotherapy is given. Setron(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, Setron(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 Setron(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 Setron(Granisetron) undiluted, administered intravenously over 30 seconds.
- Paediatric Patients: Safety and effectiveness of Setron(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.
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.
Setron(Granisetron) Drug Interaction
Major: fentanyl, fentanylMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: 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
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
Setron(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
You find simplified version here Setron(Granisetron)
Setron(Granisetron) contains Granisetron see full prescribing information from innovator Setron(Granisetron) Monograph, Setron(Granisetron) MSDS, Setron(Granisetron) FDA label
FAQ
What is Setron(Granisetron) used for?
Setron(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 Setron(Granisetron)?
Setron(Granisetron) appears to be a safe and effective drug for pediatric patients receiving emetogenic chemotherapy.
How does Setron(Granisetron) work?
Setron(Granisetron) works by blocking serotonin, a natural substance in the body that causes nausea and vomiting.
What are the common side effects of Setron(Granisetron)?
Common side effects of Setron(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 Setron(Granisetron) safe during pregnancy?
Current guidelines suggest that Setron(Granisetron) is an optional treatment for nausea and vomiting in pregnancy (NVP) despite lack of evidence to support fetal safety.
Is Setron(Granisetron) safe during breastfeeding?
No information is available on the use of Setron(Granisetron) during breastfeeding. Until more data become available, Setron(Granisetron) should be used with caution during breastfeeding.
Can I drink alcohol with Setron(Granisetron)?
Your doctor may suggest that you avoid alcohol or reduce the amount of alcohol you drink while you are taking Setron(Granisetron).
Can I drive after taking Setron(Granisetron)?
Setron(Granisetron) may make you feel dizzy that affects your mental ability. Do not drive or operate machinery if you experience dizziness.
How long does Setron(Granisetron) take to work?
When taken to prevent nausea and vomiting caused by radiation, Setron(Granisetron) is usually taken within 1 hour before treatment.
How long does Setron(Granisetron) stay in my system?
Setron(Granisetron) is a long-acting medication that can stay in your system for a week after just one dose.
When should be taken of Setron(Granisetron)?
Setron(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 Setron(Granisetron)?
The recommended adult dosage of oral is 2 mg once daily or 1 mg twice daily.
Who should not take Setron(Granisetron)?
You should not take Setron(Granisetron) if you are allergic to it. To make sure Setron(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 Setron(Granisetron)?
If you take too much Setron(Granisetron), call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
Does Setron(Granisetron) cause constipation?
The most common side-effects are constipation and headache.
Does Setron(Granisetron) make me sleepy?
This Setron(Granisetron) may make you dizzy or drowsy.
Can I just stop taking Setron(Granisetron)?
Do not exceed the recommended dose. Treatment with Setron(Granisetron) Tablets should not be withdrawn suddenly, particularly if the medicine has been used by the patient for a long time.
Can Setron(Granisetron) affects my heart ?
Setron(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 Setron(Granisetron) increase blood pressure?
In most human studies, Setron(Granisetron) has had little effect on blood pressure, heart rate or ECG.
