The demand for drug-induced sedation for magnetic resonance imaging (MRI) scans have substantially increased in response to increases in MRI utilization and growing interest in anxiety in children. Understanding the pharmacologic options for deep sedation and general anesthesia in an MRI environment is essential to achieve immobility for the successful completion of the procedure and ensure rapid and safe discharge of children undergoing ambulatory MRI. For painless diagnostic MRI, a single sedative/anesthetic agent without analgesia is safer than a combination of multiple sedatives. The traditional drugs, such as chloral hydrate, pentobarbital, midazolam, and ketamine, are still used due to the ease of administration despite low sedation success rate, prolonged recovery, and significant adverse events. Currently, dexmedetomidine, with respiratory drive preservation, and propofol, with high effectiveness and rapid recovery, are preferred for children undergoing ambulatory MRI. General anesthesia using propofol or sevoflurane can also provide predictable rapid time to readiness and scan times in infant or children with comorbidities. The selection of appropriate drugs as well as sufficient monitoring equipment are vital for effective and safe sedation and anesthesia for ambulatory pediatric MRI.