Drug intelligence / Profile preview

Naltrexone + Acetaminophen

Development stage
Unknown
Lead developer
Allodynic Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Naltrexone + acetaminophen is a combination of two small molecule drugs. Naltrexone is an opioid receptor antagonist primarily used in the treatment of opioid use disorder and alcohol use disorder, acting by blocking opioid receptors and reducing cravings for opioids and alcohol. Acetaminophen (also known as paracetamol) is a widely used analgesic and antipyretic that works by inhibiting prostaglandin synthesis in the central nervous system, providing pain relief and fever reduction. The combination has been investigated at low doses for acute migraine treatment, with studies suggesting it may provide greater pain relief than placebo. Naltrexone also exhibits anti-inflammatory effects by blocking production of pro-inflammatory cytokines such as interleukin-6, tumor necrosis factor-alpha, interferon-beta, calcitonin gene-related peptide (CGRP), nitric oxide (NO), and reactive oxygen species (ROS) in nerve cells[3][5]. There are no widely marketed brand names or approved products for this specific combination. Both components can affect liver function; caution should be exercised when co-administering due to increased risk of hepatotoxicity[1][2].

Other names
naltrexone/acetaminophen
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)MOR (Mu opioid receptor)TLR4 (Toll-like receptor 4)DOR (Opioid Receptor Delta 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)KOR (Kappa opioid receptor)

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