Drug intelligence / Profile preview

gabapentin + etoricoxib

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Gabapentin + etoricoxib is a **combination drug** composed of two active pharmaceutical ingredients: gabapentin, an anticonvulsant with established antihyperalgesic and analgesic properties, and etoricoxib, a selective cyclooxygenase-2 (COX-2) inhibitor classified as a nonsteroidal anti-inflammatory drug (NSAID). This combination is investigated as a **multimodal analgesic regimen**, especially for perioperative use. Gabapentin modulates voltage-gated calcium channels (alpha-2-delta subunit) in the central nervous system, reducing excitatory neurotransmitter release and dampening neuropathic and postoperative pain. Etoricoxib selectively inhibits COX-2, resulting in decreased prostaglandin synthesis and providing anti-inflammatory and analgesic action without the gastrointestinal toxicity commonly associated with non-selective NSAIDs. Clinical studies report that premedication with this combination can **prolong and improve postoperative analgesia and reduce opioid requirements** after surgery[1][7]. Both drugs are typically used orally.

02

Targets

CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)

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