Chapter 22. Antagonists of Opioids

Charles O'Brien, M.D., Ph.D.; Kyle M. Kampman, M.D.
DOI: 10.1176/appi.books.9781585623440.352692



For the treatment of opioid dependence, agonist treatment with methadone and buprenorphine has had the greatest impact. These medications are agonists in that they have affinity for opiate receptors resulting in binding to the receptor and activating it. Agonists are effective for the treatment of opiate dependence mainly because they reduce opiate craving, reduce opiate withdrawal symptoms, and confer tolerance to opiates, thus reducing the euphoric effects of additional opiates, such as heroin. Methadone is a full agonist, whereas buprenorphine is a partial opiate agonist. Partial agonists bind to opiate receptors but activate them only in a limited way so that there is a ceiling to their agonist effects. Partial agonists may also prevent the occupation of receptors by full agonists with lesser affinity, thus blocking the euphoric effects of abused opiates. A partial agonist such as buprenorphine provides some opiate subjective effects and thus is more acceptable to most opiate addicts than an antagonist that binds to opiate receptors without activating them, thus producing no opiate effects. In overall clinical outcome, buprenorphine is comparable with methadone for the majority of opiate addicts who do not require a high maintenance dosage of opioid.

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Table Reference Number

Antagonist treatment is a useful option in the treatment of opioid addiction.

Antagonists have an important role to play in treating overdose and in diagnosing physical dependence.

The major obstacle in the use of oral naltrexone is the high dropout rate because patients either change their minds about treatment or decide they no longer need the medication.

The long-acting depot preparation is a major improvement in maintaining medication adherence.

Antagonists are particularly effective in selected populations such as medical personnel, white collar addicts, and parolees with a history of opioid addiction.


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Sample questions:
Which of the following is a partial opiate agonist?
Which of the following statements about naltrexone is true?
All of the following statements describe either benefits of naltrexone treatment for opiate dependence or patient populations who may respond well to naltrexone treatment except
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