Sections
Antagonists of Opioids: Introduction | Opioid Antagonists | Key Points | References | Suggested Reading
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.