格拉司琼 (Sancuso, Sustol)

概览

Granisetron is a 5HT3 antagonist used to treat nausea and vomiting in cancer therapy and postoperatively.

作用机制

Granisetron is a potent, selective antagonist of 5-HT 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.

适应症

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).

• Nausea and vomiting