One of the most widely used medications approved by the FDA for the treatment of opioid use disorder (OUD), buprenorphine serves two main purposes. It can be beneficial during both stabilizations to ease withdrawal symptoms as well as throughout the maintenance phase by minimizing cravings. In fact, recent studies by the U.S. Dept. of Health and Human Services have actually found better outcomes with maintenance therapy than by tapering buprenorphine. The drug can also be combined with naloxone, the popular medication used to reverse the effects opioid overdose, in order to help prevent misuse.
Buprenorphine, or bupe, is an opioid partial agonist, meaning it can produce similar, although weaker effects than full agonists like heroin and Vicodin. Furthermore, these effects have a ceiling at moderate dosages which deters abuse. The drug works by binding to and partially activating mu opioid receptors in the brain, enough to suppress the effects of withdrawal and cravings. For MAT, it is prescribed as either a dissolvable film which also contains naloxone (Suboxone), a sublingual tablet containing only buprenorphine (Subutex), a once-monthly injection (Sublocade), or six-month implant (Probuphine).
It may seem as though, since buprenorphine is partial agonist and naloxone is a full antagonist, the two would interact and send the user into opioid withdrawal. However, the naloxone has poor bioavailability when taken orally and thus only helps deter abuse of buprenorphine. But it is absorbed better when injected. Thus, if the oral bup/naloxone tablets were to be crushed and injected, the user would likely enter full opioid withdrawal.
Available as either a once-daily oral tablet or monthly injection (Vivitrol), naltrexone is approved by the FDA for treatment of both alcohol and opioid addiction. Like naloxone, naltrexone is an opioid antagonist, meaning it completely blocks the effects of opioid agonists such as oxycodone and methadone. This discourages future use of opioids, as one would not receive the high produced by opioid agonists.
As a medication-assisted treatment option, Naltrexone offers several benefits. When combined with individual and group therapy, it can prevent relapse through deterring opioid use, as you know getting high is not possible. Naltrexone has also been reported by SAMHSA (Substance Abuse and Mental Health Services Administration) to reduce cravings, although other studies suggest that it may not be as strong at reducing urges for opioids as it is for alcohol. But the science says that if you are aware opioids are no longer rewarding, cravings should logically subside.
Another benefit of naltrexone is that it has virtually no potential for abuse. Since it is an opioid agonist, the drug will not produce the same euphoric effects of opioid agonists. And when the monthly injectable form is used, you are limited to only receiving the medication in a doctor’s office. However, in order for naltrexone to work, you must be completely detoxed from opioids from starting the medication. And because it essentially blocks the high you would normally receive from opioids, there is a potential for overdose with a relapse. Therefore, as with all medications used in MAT, prescriptions should be used in conjunction with counseling and psychosocial support for relapse prevention.
The oldest of current FDA-approved medications for medication-assisted treatment of opioid addiction, methadone can be effective for both withdrawal management and maintenance. Methadone is opioid full agonist that works by binding to and activating the Mu-opioid receptor, producing milder, longer lasting effects than agonists like heroin or prescription pain-killers. It can reduce withdrawal symptoms as well as block the euphoric effects of other agonists. When combined with counseling and behavioral therapies, methadone is an effective treatment for opioid addiction, allowing you to once again partake in daily actives.
Once the “gold standard” in opioid addiction treatment, methadone has recently been overshadowed by newer forms of MAT. Though methadone clinics still exist, those offering buprenorphine and/or naltrexone have grown at a much higher rate. In order to prescribe buprenorphine or suboxone, a qualified healthcare provider must only complete an eight-hour certification class and apply for a waiver. Naltrexone can be prescribed by any physician licensed to prescribe medications. Methadone, on the other hand, can only be dispensed at SAMHSA-certified Opioid Treatment Programs (OTPs).
Another reason for the push toward buprenorphine and naltrexone is that methadone can be addictive. Doses are customized to each individual, often adjusted and readjusted, so adherence to the prescription is vital. Methadone also can present a fair amount of side effects, some serious, such as difficulty breathing, faint and hallucinations. As with all opioids, its effects can be increased, often to dangerous levels, when combined with alcohol, benzodiazepines and other opiates. Despite the controversy and dangers associated with methadone still maintains a large user base that has grown to over 350,000.