Aim: Few studies have investigated pregabalin use as preemptive analgesia in the management of acute pain and anxiety following arthroscopic shoulder surgery. We hypothesized that the preemptive use of oral pregabalin might decrease pain and postoperative anxiety on arthroscopic shoulder surgery pain during the initial 48 hours. Patients and methods: In this prospective, randomized, double-blind, placebo-controlled study, 65 eligible patients were randomly divided into two groups, the preemptive pregabalin 150 mg (group P) and the control group (group C). The primary outcomes were pain levels measured both rest and during active motion based on a visual analog scale (VAS). Secondary outcomes were the level of anxiety (STAI-S and STAI-T), patient satisfaction, and complications. Results: Group P showed lower pain (p < 0.001), lower opioid consumption (p < 0.001), longer time to first requirement of analgesia (p < 0.001), and lower rescue analgesic dose (p < 0.001) than the control group at postoperative 48 h follow-up. Also, group P showed less preoperative and postoperative anxiety (p < 0.001) and greater patient satisfaction (p < 0.001) than group C. The rate of postoperative adverse effects was similar between the groups (p > 0.05). Conclusion: The preemptive use of oral pregabalin received 150 mg daily for 2 days before surgery provided postoperative analgesia in both rest and active motion, and improved preoperative and postoperative anxiety levels and greater patient satisfaction in patients undergoing arthroscopic surgery.