Drug information of Granisetron

Granisetron

Drug group: Antiemetic

Granisetron blocks the actions of chemicals in the body that can trigger nausea and vomiting. Granisetron is used to prevent nausea and vomiting that may be caused by medicine to treat cancer (chemotherapy or radiation).

Mechanism of effect

Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors

Pharmacodynamic

Granisetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptor.

Pharmacokinetics

Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism. Plasma protein binding is approximately 65% and Granisetron distributes freely between plasma and red blood cells. Metabolism: Primarily hepatic. approximately 11% of the orally administered dose is eliminated unchanged in the urine in 48 hours. The remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces. Half life: 4-6 hours in healthy patients, 9-12 hours in cancer patients.

Dosage

Usual Adult Dose for Nausea/Vomiting - Chemotherapy Induced
IV: 10 mcg/kg over 5 minutes, beginning 30 minutes before initiation of chemotherapy.
Orally: 2 mg, given up to 1 hour before chemotherapy, or 1 mg twice a day (the first dose is given up to 1 hour before chemotherapy, and the second dose is given 12 hours later)
Usual Pediatric Dose for Nausea/Vomiting - Chemotherapy Induced
Greater than or equal to 2 to 16 years: 10 mcg/kg IV 30 minutes before start of chemotherapy.

Alerts

1-Patients should be informed of the increased risk of serotonin syndrome, especially if Granisetron is used concomitantly with other serotonergic drugs.
2-Granisetron should be used with caution in patients with pre-existing arrhythmias or cardiac conduction disorders,

Points of recommendation

• Take without regard to meals.
• Advise patients to seek immediate medical attention if the following symptoms occur: changes in mental status, autonomic instability, neuromuscular symptoms with or without gastrointestinal symptoms

Pregnancy level

B


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