Drug intelligence / Profile preview

paracetamol + palmitoylethanolamide

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

Overview

This is a fixed-dose combination of paracetamol (also known as acetaminophen), a widely used analgesic and antipyretic, and palmitoylethanolamide (PEA), an endogenous fatty acid amide with anti-inflammatory and analgesic properties. The combination is designed to provide synergistic pain relief and anti-inflammatory effects at lower doses than traditional paracetamol monotherapy. Paracetamol primarily acts by inhibiting cyclooxygenase enzymes in the central nervous system, reducing prostaglandin synthesis involved in pain and fever. PEA modulates neuroinflammation through multiple mechanisms including activation of peroxisome proliferator-activated receptor alpha (PPAR-α) and downregulation of mast cell activation, leading to reduced cytokine release. Preclinical studies suggest that the combination reduces hyperalgesia, neuroinflammation, nerve growth factor expression, histological damage, cytokine release, apoptosis, and may act via inhibition of the NF-κB pathway with decreased COX-2/prostaglandin E2 production[1][2][3]. The rationale for this combination includes enhanced efficacy for acute/chronic/neuropathic pain or fever management while potentially lowering the risk of liver toxicity associated with higher doses of paracetamol[2].

Other names
acetaminophen + palmitoylethanolamideparacetamol + PEA
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)RELA (Nuclear Factor Kappa B Subunit p65)PPARA (Peroxisome proliferator-activated receptor alpha)

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