Sedation in pediatric patients presents unique challenges due to their developmental and physiological differences compared to adults. Oral ketamine, a dissociative anesthetic, has emerged as a promising alternative to traditional sedatives, offering a non-invasive method for achieving sedation in children. This comprehensive review evaluates the efficacy and safety of oral ketamine for pediatric sedation, consolidating evidence from recent studies and clinical trials. The review details the pharmacological properties of oral ketamine, including its mechanism of action and its role in achieving effective sedation. It examines dosing guidelines, clinical applications, and the outcomes of sedation procedures utilizing oral ketamine. Additionally, the review addresses the safety profile of oral ketamine, including standard and serious adverse effects, and provides recommendations for monitoring and managing potential risks. Comparative analyses with other sedation methods highlight the advantages and limitations of oral ketamine, including its effectiveness and ease of administration compared to intravenous (IV) and inhaled sedatives. The review also identifies gaps in the current literature and suggests areas for future research, including long-term safety and potential developmental impacts. In conclusion, oral ketamine represents a valuable option for pediatric sedation, offering a balance of efficacy and ease of use. This review aims to guide clinicians in making informed decisions regarding the use of oral ketamine, contributing to safer and more effective sedation practices in pediatric care.