Background: Premedication in pediatric cases plays a critical role in achieving anxiolysis, which facilitates a smoother separation from parents and simplifies the induction of anesthesia. This research assessed the efficacy of pregabalin as a premedication agent in pediatric anesthesia relative to the commonly used midazolam. Methods: This randomized, double-blind controlled study involved 90 children aged 1 to 7 years undergoing tonsillectomy. Participants were randomly allocated into three equal groups receiving pregabalin syrup at 3.5 mg/kg (Group P), midazolam at 0.5 mg/kg (Group M), or a placebo solution (Group C). The primary outcome was assessed using the postoperative pediatric agitation scale (Watcha), while secondary outcomes included parental separation anxiety, acceptance of the anesthesia mask, FLACC (Face, Legs, Activity, Cry, Consolability) pain scores, and extubating time. Results: Postoperative Watcha scale were significantly reduced in Groups P and M in comparison with the controls (p