Naltrexone

Naltrexone is a medication for opioid use disorder (OUD) that is administered as a once monthly long-acting injection. It is used less often than medications like methadone and buprenorphine, but can effectively reduce illicit opioid use and the risk of death from an opioid overdose.

Evidence-based Scale

Naltrexone is an FDA-approved medication for opioid use disorder (OUD) that is administered as a once monthly long-acting injection (also referred to as extended release or “XR” naltrexone). Although there is also a pill form of naltrexone, this formulation is approved only for the treatment of alcohol use disorder. The use of oral naltrexone for OUD is considered “off-label” and not approved by the FDA. Naltrexone works by blocking the effects of opioids in the brain and body. This makes it fundamentally different from other medications for opioid use disorder, such as buprenorphine and methadone, which maintain a steady level of opioid effects. Because of these blocking properties, naltrexone can cause uncomfortable withdrawal symptoms if given to someone while other opioids are still in the body. As a result, naltrexone is typically given to individuals who have already abstained from opioids for a period of time or who complete a period of medically supervised withdrawal referred to as detoxification.. Naltrexone then helps to prevent future opioid cravings and blocks the effects of any opioids that are taken. When compared head-to-head to buprenorphine and methadone, naltrexone has been shown to be less effective at reducing opioid use and opioid-related death and is less frequently used in real-world practice, but is more effective than taking no medication for opioid use disorder.