Drug intelligence / Profile preview

paracetamol + pregabalin + dexamethasone

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

Overview

This is a combination drug consisting of paracetamol (acetaminophen), pregabalin, and dexamethasone. Paracetamol is an analgesic and antipyretic that works primarily by inhibiting prostaglandin synthesis in the central nervous system. Pregabalin is a synthetic analog of gamma-aminobutyric acid (GABA) with analgesic, anticonvulsant, and anxiolytic effects; it binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing neurotransmitter release. Dexamethasone is a potent synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressant properties; it acts by binding to glucocorticoid receptors to modulate gene expression and suppress inflammatory mediators. This combination has been studied for perioperative pain management, particularly for reducing postoperative pain and opioid requirements after surgeries such as abdominal hysterectomy or tonsillectomy[1][2][4]. While some studies show benefits in reducing nausea, vomiting, or rescue analgesia use when dexamethasone is included[1][3], overall evidence suggests no significant reduction in morphine consumption or pain scores compared to paracetamol alone for certain procedures[1].

02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)GR (Glucocorticoid receptor)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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