Granisetron

Granisetron is a serotonin 5-HT? receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

Granisetron

Granisetron; 109889-09-0; Kevatril; Sancuso; Sustol

Cadigran, Emegran, Graitic, Grandem, Granexa, Granicip, Graniforce, Graniset, Granisol, Granitero, Granon, Nisley, Tapit, Zetron

1-methyl-N-[(1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]-1H-indazole-3-carboxamide

NA

Granisetron is a selective inhibitor of type 3 serotonergic (5-HT₃) receptors. 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 dopamine D 2 receptors; for alpha 1 -, alpha 2 -, or beta-adrenoreceptors; 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 serotonin then stimulates the splanchnic and vagal 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. 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. 

Oral-The recommended dose is 2 mg once daily or 1 mg twice daily. 

For the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).

Headache; sensation of flushing; constipation; hypersensitivity reactions; chest pain; CV disturbances; dizziness; transient visual disturbances. Rarely, liver disorders; development of seizures; extrapyramidal reactions.

Phenobarbital may induce metabolism of granisetron.

Hypersensitivity

Store at 25°C

Molecular weight

312.417

Molecular formula

C18H24N4O`

CAS number

109889-09-0

Precautions

• Subacute intestinal obstruction or ileus.
• Moderate to severe hepatic impairment.
• Risk factors for QT prolongation (e.g. electrolyte abnormalities and cumulative high-dose anthracycline therapy) or other congenital long QT syndrome.
• Pregnancy, lactation