Drug intelligence / Profile preview

palonosetron + dexamethasone + droperidol

Development stage
Unknown
Lead developer
Helsinn
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

This is a combination therapy consisting of three drugs—palonosetron, dexamethasone, and droperidol—used primarily for the prevention and management of postoperative nausea and vomiting (PONV). - **Palonosetron** is a second-generation selective 5-hydroxytryptamine-3 (5-HT3) receptor antagonist with a long half-life, which blocks serotonin receptors in the chemoreceptor trigger zone and gastrointestinal tract to prevent nausea and vomiting. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with anti-inflammatory and antiemetic properties; its mechanism in PONV prophylaxis may involve central inhibition of prostaglandin synthesis or reduction of serotonin release. - **Droperidol** is a butyrophenone antipsychotic that acts as an antagonist at dopamine D2 receptors in the chemoreceptor trigger zone, providing additional antiemetic effects. The combination targets multiple emetic pathways to provide enhanced prophylaxis against PONV compared to monotherapy or dual therapy regimens. This triple regimen may be considered for patients at high risk for PONV or those undergoing surgeries associated with significant risk[1][2][4].

02

Targets

GR (Glucocorticoid receptor)HTR3A (5-hydroxytryptamine receptor 3A)DRD2 (Dopamine D2 Receptor)

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