Drug intelligence / Profile preview

diclofenac + gabapentin + morphine

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Subcutaneous, Topical, Rectal, Intrathecal, Epidural
01

Overview

This is a combination of three pharmaceutical agents—diclofenac, gabapentin, and morphine—used for pain management. Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and thereby decreasing inflammation and pain. Gabapentin is an anticonvulsant that binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, inhibiting excitatory neurotransmitter release and providing analgesic effects particularly in neuropathic pain. Morphine is an opioid analgesic that acts primarily as an agonist at the mu-opioid receptor, leading to inhibition of nociceptive transmission in the central nervous system. The combination aims to provide multimodal analgesia by targeting different mechanisms involved in pain pathways. Clinical studies have shown synergistic or additive effects when these drugs are used together or in pairs (e.g., gabapentin with morphine[1][5], diclofenac with morphine[3][4], gabapentin with diclofenac[2]), allowing for improved pain control at lower doses of each component compared to monotherapy. This can reduce dose-limiting side effects associated with higher doses of individual drugs but may also increase risks such as sedation, constipation, dry mouth, dizziness, and respiratory depression due to overlapping adverse effect profiles.

02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)MOR (Mu opioid receptor)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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