granisetron

Ligand id: 2300

Name: granisetron

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 3
Topological polar surface area 50.16
Molecular weight 312.2
XLogP 2.57
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
This antiemetic and antinauseant drug is used to prevent nausea and vomiting in cancer patients receiving chemotherapy. It may be administered orally (Kytril®) or via transdermal patch (Sancuso®). An extended-release injectable formulation (Sustol®) is also available.
Mechanism Of Action and Pharmacodynamic Effects
Granisetron is a selective 5-HT3 serotonin receptor antagonist. Serotonin released as a result of chemotherapy, is thought to stimulate the vagal and splanchnic nerve receptors that project to the medullary vomiting center, and the 5-HT3 receptors in the area postrema, and that this initiates the vomiting reflex. Antagonising the serotonin effect on the 5-HT3 receptors therefore reduces nausea and vomiting.