Metformin, a drug of biguanide class, is now one of the most widely used drugs in the treatment of type 2 diabetes. It activates adenosine monophosphate-activated protein kinase (AMPK) and through AMPK activation, inhibits the mammalian target of rapamycin (mTOR) pathway. Recent literature has explored metformin as an option in pain management, given its role in the AMP-activated protein kinase (AMPK) pathway and its ability to modulate pain in animal models. Based on a variety of preclinical pain models, it is now clear that mTOR signaling plays a major role in the sensitization of the nervous system in chronic pain conditions. The activation of AMPK with metformin has led to decreased pain in neuropathic and postsurgical pain models, suggesting that these drugs and this mechanism of actin might be effective in humans. Despite the strong preclinical rationale, there are only very few data considered the utility of metformin as a potential pan therapeutic in humans. Further, randomized studies were needed to identify the role of metformin in pain perception and chronic pain conditions in humans.