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Opioid antagonists have an important role in the treatment of opioid use disorder (OUD), including reversing an opioid overdose and reducing the risk of relapse. Opioid antagonists block or diminish the reinforcing effects of opioids and decrease the risk of overdose with resumption of opioid use. Research suggests that injectable extended-release naltrexone may attenuate craving (Lee et al. 2018; Tanum et al. 2017). In this chapter we focus on opioid antagonists—specifically, the use of oral and injectable extended-release naltrexone to treat OUD, as well as the use of naloxone to reverse opioid overdose. Topics that will be addressed include indications, antagonist pharmacology, routes of administration, adverse effects, effectiveness, and treatment choice considerations.
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