Drug intelligence / Profile preview

oxycodone + ketorolac

Development stage
Phase 2
Lead developer
Merck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Oxycodone + ketorolac is a combination analgesic therapy consisting of two active pharmaceutical ingredients: - **Oxycodone** is an opioid analgesic that acts primarily as an agonist at the mu opioid receptor, with additional activity at kappa and delta opioid receptors. It modulates pain perception in the central nervous system by inhibiting ascending pain pathways, altering both the emotional and sensory response to pain[4][6]. - **Ketorolac** is a nonsteroidal anti-inflammatory drug (NSAID) that provides analgesia by inhibiting cyclooxygenase (COX) enzymes, thereby reducing prostaglandin synthesis involved in inflammation and pain signaling[2][3]. This combination aims to provide enhanced relief for moderate-to-severe acute pain by leveraging both central (opioid-mediated) and peripheral (NSAID-mediated) mechanisms. The use of such combinations may allow for lower doses of each component, potentially reducing side effects associated with higher doses of opioids or NSAIDs alone[5]. Oxycodone + ketorolac may be used in settings such as postoperative or trauma-related acute pain management.

Other names
羟考酮 + 酮咯酸丁三醇
02

Targets

DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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