Optimal postoperative pain management presents a challenge for healthcare providers across all surgical specialties, since it is estimated that many patients submitted to major surgeries do not receive an adequate analgesic treatment, increasing the risk of complications, length-of-stay and costs for health assistance. The development of new agents for postoperative pain control creates possibilities for better combinations in preventive and multimodal analgesia. Recently, the use of gabapentinoids (gabapentin and pregabalin) in the perioperative period has become more popular. Several clinical studies and meta-analyses reveal that perioperative gabapentinoids may evoke a significant opioid-sparing effect and probably decrease the postoperative pain score. Gabapentinoids may be a good strategy for preventive and multimodal analgesia in major surgeries, particularly pregabalin, considering its pharmacokinetics profile. Situations where there are limitations of regional anesthesia techniques or in cases where there is an intention to reduce the use of opioids or anti-inflammatory drugs at the trans-operatory period are certainly good opportunities for their use. However, gabapentinoids are associated with several adverse effects, including sedation, dizziness, and peripheral edema. Therefore, further studies are needed to evaluate the real cost-effectiveness of this approach. Additionally, specific attention should be paid to minor and ambulatory surgeries as well as for the elderly patients to which gabapentinoids are clearly not beneficial and potentially harmful.