Drug intelligence / Profile preview

diclofenac + acetaminophen + codeine

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This drug is a fixed-dose combination of three active ingredients—diclofenac, acetaminophen (also known as paracetamol), and codeine—used for the management of moderate to severe pain. Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that works by inhibiting cyclooxygenase enzymes (COX-1 and COX-2), thereby reducing prostaglandin synthesis, which leads to decreased inflammation and pain[3][6][8]. Acetaminophen acts primarily in the central nervous system to inhibit prostaglandin synthesis, providing analgesic and antipyretic effects[1][5]. Codeine is an opioid analgesic that exerts its effect mainly through conversion to morphine via CYP2D6-mediated metabolism; it binds to mu-opioid receptors in the central nervous system, increasing pain threshold and altering pain perception[4][7]. The combination leverages different mechanisms of action for superior analgesia compared with individual components or dual combinations. Clinical studies have shown this triple combination provides enhanced pain relief after procedures such as dental surgery but may increase the risk of side effects due to additive adverse event profiles from each component[2][10].

Other names
diclofenac + paracetamol + codeine
02

Targets

MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)DOR (Opioid Receptor Delta 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)KOR (Kappa opioid receptor)COX-3 (Mitochondrially encoded cytochrome c oxidase subunit 3)

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