How does Buprenorphine work?
Buprenorphine is a relatively new medication, approved in 2002 for the treatment of opioid addiction both during and after detoxification. It is also sometimes used in the hospital for pain relief after surgery. Like other opioid drugs, buprenorphine binds to “mu” opioid receptors in the brain. However, buprenorphine is only a “partial agonist” for these opioid receptors, and cannot stimulate the brain as strongly as other opioids. This allows buprenorphine to have a “ceiling effect.” When taken by mouth, it is rare for buprenorphine to stimulate opioid receptors strongly enough to cause fatal overdose.
Buprenorphine is also a long-acting medication, providing stable, low-level activation of opioid receptors in the brain, preventing withdrawal symptoms and cravings.
What is Buprenorphine treatment like?
Buprenorphine is given as a sublingual tablet, and dissolves under the tongue. It comes in two forms:
Subutex: Buprenorphine alone
Suboxone: Buprenorphine + Naloxone
How do patients start taking buprenorphine?
Doses of buprenorphine work best when they are given after symptoms of withdrawal have already started. Patients must wait 12-18 hours after their last use of a shorter-acting opioid drug, such as heroin or prescription painkiller. Buprenorphine can cause withdrawal if taken after a stronger dose of another opioid, as it can “kick out” and replace other opioids in the brain. However, after withdrawal has already started, beginning buprenorphine doses can then help to relieve withdrawal symptoms and prevent relapse.[4]
Low-dose buprenorphine treatment has less patient retention than methadone treatment. However, higher doses of buprenorphine have similar levels of patient retention as methadone. High-dose buprenorphine and methadone patients also have similar rates of relapse and self-reported heroin use during treatment.[5] Buprenorphines other advantages make it preferable for some patients.
Convenience and Flexibility of Buprenorphine
While methadone must be prescribed and distributed daily in special clinics, patients with prescriptions for buprenorphine do not need to visit special drug clinics to pick up their medication. Because buprenorphine is generally safer to use than methadone, certified physicians in a “regular” medical office can prescribe it.
Continuing Treatment with Buprenorphine
After their treatment plan is stable, patients will be required to see their physician for continued treatment at least every two to four weeks. If patients miss an appointment, they may not be able to refill their medication on time and experience uncomfortable withdrawal symptoms.
Opioid-dependent patients maintained with buprenorphine treatment may remain physically dependent on this opioid medication, but are not “addicted” if these medications are used only as help with the process of recovery. Withdrawal symptoms can still occur if more than one dose is missed.
What happens in A patient’s regular visits?
The patient will be asked to bring the medication container to each visit.
The patient may also be asked to give urine, blood, or breath samples at the time of the visit.
The patient may also sometimes be called in randomly to have his or her pills counted and/or to give a urine sample to test for the presence of other drugs and alcohol. This is a regular part of drug treatment, and helps keeps patients safe by preventing drug abuse.
Safety of Buprenorphine
Because of its “ceiling effect,” buprenorphine is much safer in the case of an overdose than other opioids. Buprenorphine is only a partial agonist of opioid receptors in the brain, and is less likely to suppress breathing to the point of death than opioids like heroin or methadone. Buprenorphine also has less risk of causing problems in heart rhythm. When treatment is stopped, buprenorphine causes milder withdrawal than methadone. Because buprenorphine is safer to use than methadone, it is easier to prescribe and doesn’t require visits to special methadone clinics.
Risks of Buprenorphine
However, Buprenorphine can still be dangerous when mixed with other drugs, and life-threatening overdose and death have occurred when it is not taken as recommended by a physician. Patients interested in buprenorphine should be aware of how to use this medication safely.
It is important for anyone taking buprenorphine to make their entire medical team aware of their use of buprenorphine, even doctors not directly involved in their addiction treatment. Sharing this knowledge can help prevent dangerous prescription interactions.
It is important not to use street drugs or excess alcohol with buprenorphine. These combinations can make life-threatening overdoses more likely. Patients need to tell their doctors about any other illicit drug use. Overdose deaths may occur when buprenorphine is injected against medical instructions in combination with benzodiazepines (Klonopin, Ativan, Halcion, Valium, Xanax, Serax, Librium, etc.).
Buprenorphine should also be kept away from children, as life-threatening overdoses have occurred when children take this medicine.
What is the right dose of Buprenorphine?
After patients and their family members have dealt with opioid addiction, they may be concerned about buprenorphines potential for abuse, potentially substituting one “high” for another. The “right” dose of buprenorphine is one that allows the patient to feel and act normally. It may take anywhere from a few days to a few weeks to find the right dose. Every opioid can have stimulating or sedating effects, especially in the first weeks of treatment. Patients new to Suboxone may seem drowsy, stimulated, or restless. While their dose is being adjusted, patients may experience withdrawal, daytime sleepiness, or trouble sleeping at night. However, once a patient is stabilized on the correct dose of buprenorphine, the patient should not feel “high,” and there should be no excessive sleepiness or intoxication.
Family members can help keep track of these symptoms to help the doctor find the best dose for the patient. Once the right dose is found, it’s important to take the dose on time, daily.
How long do patients need to take buprenorphine?
The optimum time for buprenorphine treatment isn’t yet clear. Buprenorphine has been shown to be very effective in helping patients with detoxification, but detoxification is only the first step in what can be a long and difficult road to recovery. Patients who choose to stop buprenorphine after detoxification should be aware that they are still at a very high risk for relapse over the next few months to years. Many patients relapse shortly after stopping buprenorphine maintenance of less than 6 months.[7]
Buprenorphine Taper
Many patients attempt to transition away from use of methadone or buprenorphine through a “tapering” process. A “taper” is a series of reductions in dose over a few weeks to months. However, relapse rates are very high for patients who taper off buprenorphine/naloxone.[8]
Many studies have followed patients before and after being tapered off of buprenorphine/naloxone maintenance. A 2011 study found that patients that have been stabilized with buprenorphine/naloxone treatment often relapse after tapering off MAT, even when therapies like counseling are continued. This study found that more than 90% of patients relapsed after an initial 3-week taper. After re-stabilization with MAT for 12 weeks, over 90% of these patients relapsed again when tapered off buprenorphine/naloxone, even when they received additional counseling.[9] Another study in 2009 followed patients who tapered off buprenorphine/naloxone after 4 weeks of maintenance treatment. At the end of a 7-day taper, less than half (44%) of patients were still opioid-free. When the tapering process was extended to 28 days, only 30% of patients were opioid-free at the end of the taper. Only 18% of patients were still completely abstinent from opioids 30 days after the taper ended.[10] Thus, tapering from buprenorphine is associated with high rates of relapse. The optimum duration of buprenorphine treatment has not yet been determined, but tapering very slowly over 4 weeks is more successful than shorter tapers.
How can the tapering process be more effective?
Researchers are still working on ways to reduce the risk of relapse after tapering off of buprenorphine. When patients and their doctors decide to gradually reduce their dose of buprenorphine, studies have shown that a slow tapering process is a safer option in preventing relapse.[11] There has been little research on the outcome of patients tapered off buprenorphine after longer periods of stabilization with MAT. Some patients may choose to transition to injection naltrexone (Vivitrol) after tapering off buprenorphine, since this opioid blocker can prevent relapse to any opioid.