This disclosure relates to the use of a composition comprising opioid/Toll-like receptor 4 (TLR4) antagonists (opioid antagonists that treats pain by blocking Toll-like receptor 4 (TLR4)) and dextro enantiomers thereof for the treatment of pain. Examples of opioid antagonist and their dextro enantiomers include naltrexone, naloxone and nalmefene, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain. Also disclosed are compositions for treatment of pain comprising opioid/Toll-like receptor 4 (TLR4) antagonists, dextro enantiomers thereof or pharmaceutically acceptable salt thereof, and at least one of an alpha-2 adrenergic receptor agonist, acetyl-para-aminophenol (APAP), a cyclooxygenase (COX) inhibitor, and an alpha-2-delta ligand that enhances the pain treatment effect of the first compound.
