Several different medications can treat opioid addiction. Methadone and buprenorphine are two drugs that decrease withdrawal symptoms and cravings. These help people stop or lessen opioid use, reduce withdrawal, and prevent overdose deaths. People with opioid use disorder who receive methadone or buprenorphine treatment are less likely to have an overdose or die, compared with those who don’t receive treatment. Naltrexone blocks the effects of opioids and can reduce cravings and the risk of opioid deaths, but it doesn’t reduce withdrawal symptoms.
Opioid Receptor Agonists
Medications in this class interact with the same targets in the brain as other opioids, but without creating a high. This partially or fully blocks their effects, reducing cravings without producing feelings of pleasure. Opioid receptor agonists also treat withdrawal symptoms to help a person stop misusing opioids.
Opioid receptor agonists include:
- buprenorphine (Brixadi, Subutex, Suboxone, Zubsolv, Sublocade)
- methadone (Methadose, Dolophine)
“Buprenorphine is a partial agonist of the opioid receptor. This means that it only partially turns on the opioid receptors, which are primarily located in the brain,” explains Sarah Leitz, MD, national physician lead for harm reduction and addiction medicine at Kaiser Permanente. “It also attaches really tightly to the opioid receptor, which makes it hard for other substances like heroin, fentanyl, or other opioids to knock it off. This helps an individual who is in a lot of withdrawal to start to feel better and less sick with fewer cravings to use.”
Dr. Leitz also cleared up some key differences between methadone and buprenorphine. “Methadone, in contrast to buprenorphine, fully turns on the opioid receptor, but it also is slow to onset, binds tightly, and stays attached for a long time,” Leitz says. “So, by gradually starting methadone and taking it once daily, individuals will find that their withdrawal symptoms improve and their cravings to use decrease. They also don’t get any ‘high’ or euphoria because the onset is so gradual.”
Since opioid receptor agonists fall into the same class of medications as the ones that can lead to opioid use disorder, you’ll need to enroll in a treatment program to use them. Methadone is only available at a specially licensed opioid treatment program facility under clinical supervision, or you may be able to start it in the hospital. While methadone is available as an oral tablet or liquid medication, buprenorphine is taken as an under-the-tongue tablet or film or as an injection. Injectable buprenorphine is available through pharmacies and healthcare professionals registered with a specific opioid use disorder treatment program (specifically, the Brixadi and Sublocade REMS). However, people can also access buprenorphine through other outpatient clinics or physicians who offer office-based opioid treatment.
Methadone side effects may include headaches, nausea, vomiting, sweating, constipation, drowsiness, and reduced libido. Buprenorphine can cause similar side effects as methadone, as well as insomnia. Both medications can cause withdrawal symptoms if a person suddenly stops taking them. If a healthcare professional advises that stopping use is safe, they’ll recommend a slow taper off of the drugs.
Doctors generally recommend that people use these medications long term, although fewer than half of all people who get treatment for opioid use disorder continue taking them. People who stop taking methadone or buprenorphine within one to two years of starting it have a higher risk of relapse and overdose, according to the Leonard Davis Institute of Health Economics.
Opioid Antagonists
Instead of activating opioid receptors like methadone or buprenorphine, this type of medication blocks receptors altogether. This means that those misusing opioids can no longer experience pleasurable sensations after taking them.
- naltrexone (Depade, ReVia)
Naltrexone is available in a daily pill form and as a long-lasting monthly injection, and any healthcare professional can administer it. Usually, people start taking naltrexone after completely stopping opioid use for 7 to 14 days, to prevent withdrawal symptoms, which can make it more challenging to start than methadone or buprenorphine.
“We typically recommend taking these medications for at least 6 to 12 months, but many people choose to take them for longer,” Leitz says. “Once someone has found stability with their medication and feels that their opioid use disorder is not an active part of their lives, they may want to try reducing or stopping their OUD medication.”
Centrally Acting Alpha-2 Adrenergic Agonists
Opioid withdrawal symptoms can make treating OUD challenging. Centrally acting alpha-2 adrenergic agonists relax blood vessels to support better blood flow, which may reduce withdrawal symptoms, including nausea, stomach cramps, muscle spasms, chills, a pounding heartbeat, aches, pain, and muscle tension, insomnia, and excessive yawning.
Lofexidine is a short-term treatment for opioid use disorder, with courses usually lasting up to 14 days and involving four daily tablets for use at around the same time daily. The medication can temporarily support ongoing treatment by helping decrease withdrawal symptoms and improve comfort. Despite this, it may not completely prevent withdrawal, and it may cause side effects, including insomnia, a dry mouth, tinnitus, fainting, or dizziness.
If you are on medication to treat opioid use disorder and would like to stop, talk to your healthcare provider to determine a plan for stopping, rather than attempting to stop on your own. They’ll work with you to map out a very slow tapering schedule, in which you gradually use less and less medication over time.
“To explore a dose reduction or stopping buprenorphine or methadone, it is recommended that the individual meet with their addiction medicine prescriber and their addiction counselor and discuss a taper plan,” advises Leitz. “These taper plans can be adjusted throughout the process, but having an idea of what it might look like to start is a good idea. It is also important to set up regular check-ins to see how the taper is going.”
A typical taper involves dose changes, check-ins, and flexibility. “I like to make changes in the dose every two to four weeks and to speak with patients about every three to four weeks while they are tapering down,” Leitz says. “Often, the individual increases withdrawal symptoms or cravings for one to two weeks after a dose decrease, but that should stabilize.”
Leitz affirms that the need to slow or stop the tapering process doesn’t indicate failure. It just means that the dose needs to be adjusted to ensure success.
The goal is to prevent a relapse. The danger of a relapse, Leitz explains, is that they may have built up a high tolerance during their previous period of use that they no longer have. Tolerance means needing to take more of a substance to experience the same effect that a lower dose gave someone before.
“If a person returns to substance use, specifically with fentanyl or heroin, they may attempt to use the same amount they previously used,” says Leitz. “However, this dosage is often far too high for their tolerance level at that point. This can lead to an unintentional overdose, which can be fatal.”
Leitz emphasizes that it’s extremely important to ensure that naloxone (Narcan), a medication for treating overdoses, is always available, especially if a person has stopped medications for OUD, and that individuals returning to opioid use remember not to use alone.
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