Granisetron

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Generic Name of Granisetron - Learn More

Granisetron

Granisetron Precaution - What You Need to Know

Granisetron is a selective serotonin (5-HT3) receptor antagonist primarily used to prevent nausea and vomiting caused by chemotherapy, radiation therapy, and post-operative recovery. While generally safe, caution should be used when prescribing granisetron to patients with a history of cardiac arrhythmias or those taking medications that affect heart rhythm, as it may cause QT prolongation, leading to an increased risk of arrhythmias. Granisetron should also be used cautiously in patients with liver impairment, as its clearance may be reduced in such individuals, requiring dosage adjustments or increased monitoring. It is recommended to monitor patients for signs of electrolyte imbalances, as these can exacerbate the potential for QT prolongation. Granisetron is not recommended for use in pregnant women, especially in the first trimester, unless the potential benefit justifies the risk to the fetus. Granisetron may be excreted in breast milk, so breastfeeding mothers should use it with caution or consider alternative treatments. Additionally, patients with hypersensitivity to granisetron or any of its components should avoid this medication. Monitoring for adverse reactions, particularly within the first few days of administration, is advised, especially in high-risk populations.

Granisetron Indication - Uses and Benefits

Granisetron is primarily used to prevent and treat nausea and vomiting associated with chemotherapy (including highly emetogenic chemotherapy), radiation therapy, and post-operative recovery. As a 5-HT3 receptor antagonist, it works by blocking the action of serotonin at the 5-HT3 receptors in the gastrointestinal tract and the brain, which are responsible for initiating the vomiting reflex. This makes granisetron highly effective for controlling both acute and delayed nausea and vomiting in cancer patients undergoing chemotherapy or radiation. It is also used in the post-surgical setting, particularly after procedures with a high risk of post-operative nausea and vomiting (PONV). In addition to its primary indications, granisetron may also be used off-label in the treatment of other conditions associated with nausea and vomiting, including certain gastroenterological disorders and in patients with hyperemesis gravidarum (severe nausea and vomiting during pregnancy) when other treatments are ineffective.

Granisetron Contraindications - Important Warnings

Granisetron is contraindicated in patients with known hypersensitivity to the drug or any of its components. This includes individuals who have experienced allergic reactions such as rash, urticaria, or anaphylaxis upon previous exposure. It should not be used in combination with other 5-HT3 antagonists, as the additive effects could increase the risk of adverse reactions, including QT prolongation. Granisetron is also contraindicated in patients with significant QT prolongation or a history of arrhythmias, especially those who have pre-existing electrolyte imbalances (such as low potassium or magnesium levels) that may increase the risk of cardiac complications. Caution is advised in patients with moderate to severe hepatic impairment, as the drug is metabolized in the liver, and its clearance may be reduced, leading to an increased risk of adverse effects. In pregnancy, particularly during the first trimester, granisetron should only be used when the potential benefits outweigh the risks. It is not recommended during breastfeeding due to limited data on its excretion in breast milk.

Granisetron Side Effects - What to Expect

The most common side effects of granisetron include headache, constipation, and fatigue. These effects are generally mild and transient, but they may be bothersome for some patients. In some cases, granisetron may cause dizziness or lightheadedness, especially in patients who are dehydrated or those with electrolyte imbalances. Serious, but rare, side effects include severe allergic reactions (e.g., anaphylaxis), chest pain, and significant changes in heart rhythm, including QT prolongation. Patients receiving granisetron should be monitored for signs of an abnormal heart rhythm, particularly if they are at higher risk (e.g., those with pre-existing heart conditions or those taking other medications that affect the heart). Gastrointestinal disturbances such as nausea and abdominal discomfort may occur but are less common than with other antiemetic agents. Some patients may also experience injection site reactions, such as pain, redness, or swelling when receiving the injectable form. Long-term use of granisetron may increase the risk of developing serotonin syndrome, particularly if taken in combination with other serotoninergic drugs. This potentially life-threatening condition can present with symptoms such as agitation, rapid heartbeat, high body temperature, muscle rigidity, and confusion. If any of these symptoms occur, immediate medical attention should be sought.

Granisetron Pregnancy Category ID - Safety Information

2

Granisetron Mode of Action - How It Works

Granisetron is a selective serotonin (5-HT3) receptor antagonist, which means it works by blocking the action of serotonin at the 5-HT3 receptors located in the gastrointestinal tract and the central nervous system. Serotonin is a neurotransmitter involved in the regulation of nausea and vomiting. In chemotherapy, radiation, and post-surgical settings, serotonin is released in the gut and brain, triggering the vomiting reflex. By blocking the 5-HT3 receptors, granisetron inhibits this process, thereby preventing nausea and vomiting. It is particularly effective in preventing acute nausea and vomiting induced by chemotherapy drugs, which are known to cause the release of large amounts of serotonin. Granisetron's ability to act peripherally in the gastrointestinal tract as well as centrally in the brain allows it to provide broad-spectrum control of nausea and vomiting. Granisetron has a high affinity for the 5-HT3 receptor, which makes it effective even at low doses and allows it to have fewer side effects compared to older antiemetics.

Granisetron Drug Interactions - What to Avoid

Granisetron can interact with a number of medications, particularly those that affect the QT interval, such as antiarrhythmics (e.g., amiodarone, sotalol), certain antidepressants (e.g., tricyclics, SSRIs), and antipsychotics (e.g., haloperidol). These interactions may increase the risk of QT prolongation, leading to potential cardiac arrhythmias. Co-administration with drugs that alter electrolyte levels, such as diuretics, should be done cautiously, as low levels of potassium or magnesium may increase the risk of heart rhythm disturbances when taking granisetron. Granisetron may also interact with drugs that affect its metabolism, such as cytochrome P450 enzyme inhibitors (e.g., ketoconazole, ritonavir), which could increase the plasma concentration of granisetron and increase the likelihood of adverse effects. On the other hand, inducers of the cytochrome P450 system (e.g., carbamazepine) may decrease the efficacy of granisetron by reducing its levels in the blood. Although granisetron’s use does not appear to be significantly impacted by food, it is still recommended to follow specific administration instructions regarding food and timing, particularly with the oral formulation.

Granisetron Adult Dose - Recommended Dosage

For the prevention of chemotherapy-induced nausea and vomiting (CINV), the standard adult dose of granisetron is typically 1 mg administered intravenously (IV) 30 minutes before chemotherapy. Alternatively, a single 2 mg oral dose may be administered once daily. In cases where radiation therapy is expected to cause nausea and vomiting, granisetron may be given as a 1 mg IV dose prior to treatment. For the prevention of post-operative nausea and vomiting (PONV), granisetron is often given as a single 1 mg IV dose immediately before or after surgery. For longer procedures or higher-risk surgeries, dosing may be adjusted according to the patient's response. Granisetron should be administered under the supervision of healthcare professionals, particularly when given via injection, to monitor for potential adverse effects, such as changes in heart rate or QT interval. If additional doses are required, they should be spaced out as per the healthcare provider’s recommendations.

Granisetron Child Dose - Dosage for Children

For children, the dosage of granisetron depends on the age, weight, and clinical condition of the patient. For chemotherapy-induced nausea and vomiting in pediatric patients, the usual dose is 10 to 40 micrograms per kilogram of body weight administered intravenously 30 minutes before chemotherapy, up to a maximum of 1 mg. For the prevention of post-operative nausea and vomiting, a single dose of granisetron is typically 10 micrograms per kilogram of body weight, administered intravenously just before or after surgery. Granisetron should be used cautiously in pediatric populations, particularly with younger children, as they may be more sensitive to the effects of medications. Children with a history of cardiac conditions or those taking other medications that affect the heart should be closely monitored for signs of QT prolongation or other adverse reactions.

Granisetron Renal Dose - Dosage for Kidney Conditions

In patients with renal impairment, adjustments to the granisetron dosage are generally not necessary, as the drug is primarily metabolized by the liver and excreted in the urine in only small amounts. However, in cases of severe renal impairment (e.g., creatinine clearance < 30 mL/min), the plasma concentration of granisetron may increase slightly. Therefore, close monitoring is recommended in these patients, especially if they are receiving other drugs that may affect renal function. Although dose adjustment is not typically required, clinicians should assess the potential for interactions with other medications that affect renal excretion and ensure electrolyte balance is maintained to reduce the risk of QT prolongation and other cardiac issues.