Naltrexone

Naltrexone is a medication that blocks opioid receptors. It is used to treat alcohol use disorder and to reduce the risk of opioid relapse after detoxification.

Opioid receptor: A cell-surface receptor activated by endogenous opioid peptides and opioid drugs. Naltrexone's central action is blocking these receptors, especially the mu opioid receptor.
Alcohol use disorder: A medical condition involving impaired control over alcohol use and continued drinking despite harm. Naltrexone can reduce heavy drinking and the risk of return to drinking.
Opioid withdrawal: A group of symptoms that can occur when prolonged opioid use is reduced or stopped. Naltrexone can abruptly intensify withdrawal if opioid dependence remains active.
Methadone: A long-acting opioid medication used to treat opioid use disorder and pain. Unlike naltrexone, methadone activates opioid receptors and can be started without an opioid-free interval.
Endorphins: Endogenous opioid peptides that bind opioid receptors and influence pain, stress, and reward. Research into endogenous opioid signaling helped establish the pharmacology relevant to naltrexone.
Mu-opioid receptor: An opioid receptor involved in analgesia, reward, respiratory depression, and physical dependence. Blocking this receptor helps prevent opioid effects and may reduce alcohol reward.
Opioid use disorder: A chronic condition characterized by problematic opioid use and clinically significant impairment or distress. Naltrexone is one medication option after opioids have been stopped and cleared.
Opioid dependence: A physiological adaptation to opioids that can produce tolerance and withdrawal when use stops. Dependence determines why naltrexone must not be started while opioids remain in the body.
Buprenorphine: A partial opioid agonist used to treat opioid use disorder and, in some formulations, pain. Buprenorphine reduces withdrawal and craving by activating receptors rather than blocking them.
Naloxone: A short-acting opioid antagonist used chiefly to reverse opioid overdose. Earlier antagonist medicines demonstrated that opioid receptors could be blocked clinically.

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