The 5-HT3 type serotonin receptor is located peripherally in the vagus nerve terminal and is central to the chemoreceptor trigger zone in the postrema area. During the process of chemotherapy that induces vomiting, enterochromaffin mucous cells release serotonin, where serotonin will stimulate the 5-HT3 receptor and activate the vagus afferent which then induces vomiting.
Granisetron is a potent antiemetic and is a very selective antagonist of the 5-hydroxytryptamine (5-HT) receptor 3. Granisetron has a very small (negligible) affinity for other types of receptors including 5-HT and on the dopamine D2 bond side.
Prevention of acute and delayed nausea and vomiting associated with chemotherapy.
Prevention of nausea and vomiting: Adult: 1 mg twice daily or 2 mg once daily, up to one week after chemotherapy. The first dose of GRANON is administered up to one hour before chemotherapy. Maximum dose of granisetron oral therapy: 9 mg.
There are no antidotes specific to granisetron. In cases of overdose, symptomatic treatment must be given. Overdose of granisetron hydrochloride up to 38.5 mg as a single injection has been reported to occur without symptoms or only experience a mild headache.
Patients with hypersensitivity to granisetron or one component of the drug.
Granisetron may reduce intestinal motility, so patients with signs of acute intestinal obstruction must be monitored after administration of granisetron.
Cross sensitivity between 5-HT3 antagonists has been reported. GRANON film-coated tablets are not recommended for patients with rare hereditary problems including galactose intolerance, lactase deficiency, or glucose-galactose malabsorption.
Like the other 5-HT3 antagonists, cases of serotonin syndrome (including changes in mental status, autonomic dysfunction and neuromuscular abnormalities) have been reported to occur after joint use between granisetron and other serotonergic drugs. If concomitant use between granisetron and other serotonergic drugs is clinically needed, it is recommended to monitor the patients' condition closely.
Pregnancy and lactation.
Headache and constipation. Rare cases of hypersensitivity reactions, including rashes and anaphylaxis have been reported. Increased liver transaminases have been observed.
Granisetron is known to be safe when given with benzodiazepines, neuroleptics, and anti-ulcer drugs.
Store in the temperature 30°C. Keep away from sunlight.
A04AA02 - granisetron ; Belongs to the class of serotonin (5HT3) antagonists. Used for the prevention of nausea and vomiting.