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Medications to Treat Opioid Addiction

How Do Medications to Treat Opioid Addiction Work?

Opioid Agonists and Partial Agonists (Maintenance Medications)

Studies show that people with opioid addiction who follow detoxification with complete abstinence are very likely to return to using the drug (relapse).10 While relapse is a normal step on the path to recovery, it can also be life threatening, raising the risk for a fatal overdose.11 Thus, an important way to support recovery from heroin or prescription opioid addiction is to maintain abstinence from those drugs using medications that reduce the negative effects of withdrawal and craving without producing the euphoria that the original drug of abuse caused. Methadone and buprenorphine are medications approved for this purpose.

Methadone is a synthetic opioid agonist that eliminates withdrawal symptoms and relieves drug cravings by acting on opioid receptors in the brain—the same receptors that other opioids such as heroin, morphine, and opioid pain medications activate. Although it occupies and activates these opioid receptors, it does so more slowly than other opioids and, in an opioid-dependent person, treatment doses do not produce euphoria. It has been used successfully for more than 40 years to treat opioid addiction and must be dispensed through specialized opioid treatment programs.12

Buprenorphine is a partial opioid agonist, meaning that it binds to those same opioid receptors but activates them less strongly than full agonists do. Like methadone, it can reduce cravings and withdrawal symptoms in a person with an opioid use disorder without producing euphoria, and patients tolerate it well. Research has found buprenorphine to be similarly effective as methadone for treating opioid use disorders, as long as it is given at a sufficient dose and for sufficient duration.13 Unlike methadone, buprenorphine can be prescribed by certified physicians in an office setting. It has been available since 2002 as a tablet and since 2010 as a sublingual film,14 and the U.S. Food and Drug Administration (FDA) approved a 6-month subdermal buprenorphine implant in May 2016 and a once-monthly buprenorphine injection in November 2017. Both formulations are available to patients stabilized on buprenorphine and will eliminate the treatment barrier of daily dosing for these patients. (Also see "Misconceptions About Maintenance Treatment")

Opioid Antagonists

Naltrexone is an opioid antagonist, which means that it works by blocking the activation of opioid receptors. Instead of controlling withdrawal and cravings, it treats addiction by preventing any opioid drug from producing rewarding effects such as euphoria. Its use for ongoing addiction treatment has been somewhat limited because of poor adherence and tolerability by patients. However, in 2010 an injectable, long-acting form of naltrexone (Vivitrol®), originally approved for treating alcohol use disorder, was FDA-approved for treating opioid addiction. Because its effects last for weeks, Vivitrol® is a good option for patients who do not have ready access to healthcare or who struggle with taking their medications regularly.

Because each medication works differently, a treatment provider should decide on the optimal medication in consultation with the individual patient and should consider the patient’s case unique history and circumstances (see "Efficacy of Medications for Opioid Use Disorder").

This page was last updated May 2017

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NIDA. (2017, May 25). Medications to Treat Opioid Addiction. Retrieved from https://www.drugabuse.gov/publications/research-reports/medications-to-treat-opioid-addiction

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