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Ketamine is a powerful dissociative anesthetic with a rich history in medicine due to its remarkably complex, dose-dependent pharmacology. Originally synthesized in 1962 as a safer and more effective alternative to phencyclidine (PCP), ketamine has expanded its clinical applications to include analgesia and immunomodulation. Approximately 11–40% of adults in the United States report suffering from chronic pain, affecting more people than diabetes, heart disease, and cancer combined. Current therapies such as opioid agonists, non-steroidal anti-inflammatory drugs (NSAIDs), gabapentinoids, antidepressants, and topical anesthetic agents are first-line treatments for various pain conditions. However, prolonged use of such medications can lead to debilitating side effects ranging from tolerance or dependence (physical and psychological) to exacerbation of other chronic health conditions, making it essential to explore alternative interventions. This approach creates clinical opportunities for ketamine’s use as a monotherapy and multimodal agent due to its unique qualities. From its origins as a potent anesthetic and analgesic agent to its current exploration as a novel treatment in psychosomatic disorders, ketamine’s pharmacology continues to be an area of active research and development