This invention relates to the use of a composition comprising opioid/Toll-like receptor 4 (TLR4) antagonists and dextro enantiomers thereof for the treatment of pain, where the opioid antagonists treat pain by blocking TLR4. More preferably, the dextro opioid/TLR4 antagonist enantiomer treats pain by blocking TLR4 while not affecting the opioid receptors and therefore avoiding adverse effects associated with blocking the opioid receptors. 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.
