Drug intelligence / Profile preview

gabapentin + dexamethasone + ketamine

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of three pharmaceutical agents—gabapentin, dexamethasone, and ketamine—used together primarily for multimodal analgesia in perioperative and postoperative pain management. Gabapentin is an anticonvulsant that modulates voltage-gated calcium channels to reduce neuropathic pain. Dexamethasone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties, acting via the glucocorticoid receptor to inhibit pro-inflammatory pathways. Ketamine is a dissociative anesthetic that acts as an NMDA receptor antagonist, providing analgesia and anesthesia by blocking excitatory neurotransmission involved in pain perception. The combination leverages different mechanisms of action to provide synergistic or additive effects on pain control while potentially reducing opioid requirements[1][3][4][8].

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)GR (Glucocorticoid receptor)NMDAR (Glutamate receptor ionotropic, NMDA)

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