Background: Appropriate management of pain is needed during the postpartum hospitalization period for preventing cesarean section (CS) related complications. Gabapentin and pregabalin have been used in treatment of neuropathic pain as well as postoperative pain with good results. However, there is paucity of studies in comparison with each other. The aim of current study was to compare the analgesic efficacy with respect to increase in duration of analgesia, reduction in total postoperative requirements of analgesics and study side effects and complications. Methods: A randomized, double-blind, placebo-controlled study was conducted in 90 women undergoing cesarean section who were anesthetized in a standardized fashion. Patients received 300 mg pregabalin, 600 mg gabapentin or placebo, 2 hours prior to surgery. Postoperative analgesia was given at visual analogue scale (VAS) ≥ 3. The primary outcome of present study was consumption of analgesic over 24 hours and patients were followed for time to rescue analgesia, pain scores, and side effects as secondary outcomes. Results: The consumption of diclofenac was statistically significant between both pregabalin and control groups, and gabapentin and control groups; however, pregabalin and gabapentin groups were comparable. Patients in pregabalin and gabapentin groups had lower pain scores in the initial hour of recovery. However, pain scores were subsequently similar in all the groups. Time to first request for analgesia was longer in pregabalin group followed by gabapentin and control groups. Conclusion: Prior to CS, a single dose of 300 mg pregabalin given 2 hours is equally effective to 600 mg gabapentin but superior to placebo. Both the drugs are better than placebo.