Drug intelligence / Profile preview

palonosetron + dexamethasone + promethazine

Development stage
Unknown
Lead developer
The Ohio State University
Modality
Small Molecules
Administration
Intravenous
01

Overview

This triple therapy combination regimen consists of palonosetron, dexamethasone, and promethazine, and was specifically investigated by Ohio State University for the prevention of postoperative nausea and vomiting (PONV) in high-risk patients undergoing neurological surgery, such as craniotomies. Palonosetron is a second-generation 5-HT3 receptor antagonist with a significantly higher affinity and longer half-life compared to first-generation antagonists. Dexamethasone is a corticosteroid that provides antiemetic effects likely through the reduction of inflammation and prostaglandin synthesis. Promethazine is a phenothiazine derivative that acts as an antagonist at H1, dopaminergic (D2), and muscarinic receptors. The combination is administered intravenously at the induction of anesthesia to provide multi-modal prophylaxis against PONV by targeting multiple emetic pathways simultaneously.

Other names
Triple therapy with palonosetron, dexamethasone and promethazine
02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)HRH1 (Histamine H1 Receptor)mAChR (Muscarinic acetylcholine receptors)DRD2 (Dopamine D2 Receptor)GR (Glucocorticoid receptor)

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