0
0

Chapter 22. Antagonists of Opioids

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

Sections

Excerpt

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.

Your session has timed out. Please sign back in to continue.
Sign In Your Session has timed out. Please sign back in to continue.
Sign In to Access Full Content
 
Username
Password
Sign in via Athens (What is this?)
Athens is a service for single sign-on which enables access to all of an institution's subscriptions on- or off-site.
Not a subscriber?

Subscribe Now/Learn More

PsychiatryOnline subscription options offer access to the DSM-IV-TR® library, books, journals, CME, and patient resources. This all-in-one virtual library provides psychiatrists and mental health professionals with key resources for diagnosis, treatment, research, and professional development.

Need more help? PsychiatryOnline Customer Service may be reached by emailing PsychiatryOnline@psych.org or by calling 800-368-5777 (in the U.S.) or 703-907-7322 (outside the U.S.).

+

CME Activity

Add a subscription to complete this activity and earn CME credit.
Sample questions:
1.
Which of the following is a partial opiate agonist?
2.
Which of the following statements about naltrexone is true?
3.
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
NOTE:
Citing articles are presented as examples only. In non-demo SCM6 implementation, integration with CrossRef’s “Cited By” API will populate this tab (http://www.crossref.org/citedby.html).
Related Content
Articles
Books
Gabbard's Treatments of Psychiatric Disorders, 4th Edition > Chapter 14.  >
DSM-IV-TR® Diagnostic and Statistical Manual of Mental Disorders > Chapter 4.  >
The American Psychiatric Publishing Textbook of Substance Abuse Treatment, 4th Edition > Chapter 18.  >
The American Psychiatric Publishing Textbook of Substance Abuse Treatment, 4th Edition > Chapter 20.  >
What Your Patients Need to Know About Psychiatric Medications, 2nd Edition > Chapter 88.  >
Topic Collections
Psychiatric News
PubMed Articles
 
  • Print
  • PDF
  • E-mail
  • Chapter Alerts
  • Get Citation