Methadone is a synthetic, long-term opioid agonist medication used in the management and treatment of opioid use disorder (OUD) and for analgesic purposes in chronic pain. The drug is approved by the U.S. Food and Drug Administration (FDA) for treating moderate-to-severe pain that has not responded to nonopioid medications or as an alternative if the pain is unresponsive to other opioid drugs. Methadone is frequently prescribed to address severe pain associated with cancer, neuropathy, or other conditions in pediatric populations. This activity comprehensively reviews the indications, mechanism of action, and contraindications of methadone as a valuable agent in treating chronic pain and managing OUDs. This activity highlights the role of the interprofessional healthcare team in the utilization of methadone for detoxifying and treating OUD as a crucial component of medication-assisted treatment, which is significant in light of the ongoing opioid use epidemic.