Disclosed are compositions for treatment of pain comprising, a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking Toll-like receptor (TLR4) and the second compound is an alpha-2-delta ligand that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone, naloxone and nalmefene. Examples of an alpha-2-delta ligand include gabapentin and pregabalin, synergistic pharmaceutical compositions thereof, and their use in the treatment, prevention, and reversal of neuropathic pain.
