Buprenorphine has been used to treat opioid dependency and addiction since the Food and Drug Administration approved Suboxone and Subutex in 2002. The medication is derived from thebaine, one of the main chemicals in opium. Other prescription drugs, such as oxycodone and oxymorphone, are also derived from thebaine.
Suboxone and other buprenorphine medications are chemically similar to other opioids. They can reduce cravings and withdrawal symptoms associated with opioid addiction.
Buprenorphine is used during maintenance therapy, which is designed to gradually wean individuals off of opioids that have a high risk for abuse, such as heroin and hydrocodone, by using opioids with a lower risk for abuse, such as buprenorphine and methadone.
People receiving methadone maintenance therapy must go to federally approved methadone clinics to receive the medication. Buprenorphine is more accessible because doctors who have received special training can prescribe it in outpatient settings. Buprenorphine is also less addictive than methadone.
Several medications contain buprenorphine, including:
The first medications containing buprenorphine, Buprenex and Butrans, were approved in 1981. Today, Buprenex is commonly used as a pain reliever for cats and dogs, and Butrans is sometimes prescribed to treat moderate pain.
Few buprenorphine medications were developed until Congress passed a law in 2000 that increased the availability of opioid-based medications. The federal government expanded access to buprenorphine treatments again in 2016, making the medication more available today than ever before.
When a person is physically dependent on opioids, their brain is used to receiving a certain dosage of opioids each day. Opioids attach to receptors in the brain that affect pleasure, respiration and pain. Without opioids, the addicted brain goes into withdrawal.
Buprenorphine works by binding to opioid receptors, but it doesn’t bind in the same way that other opioids do. It prevents the brain from experiencing withdrawal, but its effects on pleasure, respiration and pain are milder than those of other opioids.
Buprenorphine also blocks other opioids from binding to receptors in the brain. If a person uses heroin after taking buprenorphine, the illicit drug can’t attach to opioid receptors. As a result, the person is unlikely to feel any effects. However, the person may experience the effects of heroin once buprenorphine wears off.
Like methadone, buprenorphine is a long-acting opioid. Its effects can last from one to three days. Treatment using buprenorphine usually involves three stages.
Patients should be in the early stages of withdrawal during the induction phase. If they aren’t in withdrawal, buprenorphine may kick other opioids off the receptors in the brain. When an opioid antagonist, such as buprenorphine or naloxone, kicks another opioid off of a receptor, a person experiences precipitated withdrawal. Compared to regular withdrawal, precipitated withdrawal occurs more rapidly and causes more intense symptoms.
If the person is already in withdrawal before treatment, buprenorphine will attach to the open receptors. Experiencing mild or moderate withdrawal before treatment may be unpleasant, but it’s more comfortable than experiencing precipitated withdrawal. If illicit drug use is discontinued, most people begin to feel normal after about a week of buprenorphine treatment.
Most people enter the stabilization phase after a week of treatment. At this point, buprenorphine prevents withdrawal symptoms and cravings. Doctors may adjust the dosage of buprenorphine, and patients may begin taking the drug every other day.
Some people feel so comfortable during stabilization that they think they have recovered from opioid addiction. However, you should never discontinue buprenorphine without talking to your doctor. Stopping buprenorphine too soon can lead to severe withdrawal and relapse.
Once patients are stabilized and doing relatively well on buprenorphine, they enter the maintenance phase. If they’re attending inpatient or outpatient opioid rehab, they may begin intensive counseling and therapy.
Some people stay in the maintenance phase indefinitely. Others taper off of buprenorphine and overcome physical dependency on opioids. The length of buprenorphine maintenance treatment depends on each patient’s medical history.
The main differences between medications containing buprenorphine are the method and timing of administration and whether naloxone is present.
Suboxone contains a combination of buprenorphine and naloxone. It comes in both tablet and film forms. The tablets dissolve under the tongue, and the film can be placed under the tongue or inside the cheek. Suboxone is used during the maintenance stage of opioid addiction treatment.
Subutex was the brand name for a medication that contained buprenorphine and came in the form of sublingual tablets that dissolved under the tongue. Subutex did not contain naloxone. It was intended for use during the initial stages of opioid addiction treatment, but the brand-name drug is no longer available. Generic alternatives that are similar to Subutex may still be available.
Zubsolv is similar to Suboxone. It comes in tablet form, and it contains both buprenorphine and naloxone. It’s usually used during the maintenance stage of treatment. However, Zubsolv has a higher bioavailability of buprenorphine than Suboxone, meaning a lower dose of Zubsolv delivers the same amount of buprenorphine as a higher dose of Suboxone.
Bunavail contains buprenorphine and naloxone, and it comes in a buccal film that is placed inside the cheek. The Bunavail film has a higher bioavailability of buprenorphine than the Suboxone film. It can be used to initiate or maintain buprenorphine treatment.
Probuphine is an implant that is placed under the skin in the upper arm. It slowly releases buprenorphine for six months. Probuphine can be beneficial for patients who forget to take medications on schedule. It also prevents patients from discontinuing buprenorphine therapy after they relapse. The implant is only effective in people who have already been stabilized with other buprenorphine products.
Opioid addiction is associated with high rates of relapse, but medication-assisted treatments have higher recovery outcomes than therapy without medication. Numerous studies have found that buprenorphine is more effective than placebo for recovery from opioid addiction.
“There is no doubt in [the VA’s] mind that opioid-agonist therapy — methadone or buprenorphone — is first-line treatment for opioid use disorders because it reduces bad outcomes, including death from overdose.”
Additional studies have shown that combination medications containing buprenorphine and naloxone are effective in treating opioid addiction. The presence of naloxone does not reduce the effectiveness of buprenorphine. Naloxone prevents abuse and diversion, but it doesn’t increase the effectiveness of substance abuse treatment.
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More long-term studies are needed to determine the lasting effectiveness of buprenorphine, but current research indicates that methadone and buprenorphine are comparable in effectiveness. Some research indicates that the medications may be more effective than naltrexone, but there aren’t enough reliable studies to draw firm conclusions.
In one of the largest studies on buprenorphine treatment, researchers compared the effectiveness of different lengths of Suboxone treatment in participants addicted to prescription opioids who had no history of heroin use.
The results of the study included:
According to the study, those who engaged in minimal or no opioid use after therapy with buprenorphine had a successful outcome.
The researchers concluded that longer durations of treatment may support long-term recovery from prescription opioid addiction. In a follow-up study, they kept in touch with 375 participants who had received Suboxone treatment during the first study.
After 42 months:
Participants who used heroin or injected other opioids for the first time during Suboxone treatment were more likely to experience worse long-term outcomes. The first study was published in the Archives of General Psychiatry in 2011, and the follow-up study was published in the journal Drug and Alcohol Dependence in 2015.
Buprenorphine belongs to a class of drugs called partial opioid agonist-antagonists. Opioid agonists, including heroin and oxycodone, activate parts of the brain that cause pain-relieving and euphoric effects. Partial opioid agonists such as buprenorphine have a much less drastic effect on the brain, but they still cause some pain-relieving and pleasurable effects. Buprenorphine is also an opioid antagonist because it blocks opioids from causing those effects.
If abused, buprenorphine can get someone high, and it can be addictive. However, buprenorphine has a ceiling effect. Unlike other opioids, buprenorphine’s effects level off as the dose increases.
Many drugs containing buprenorphine, such as Suboxone, also contain naloxone to prevent misuse. When the tablets are swallowed as prescribed, buprenorphine’s effects outweigh the effects of naloxone. When the tablets are crushed and injected, naloxone prevents the euphoria and relaxation normally caused by opioid use.
Because buprenorphine is a partial antagonist, it can relieve mild pain. Some doctors have prescribed Suboxone and other buprenorphine-combination drugs to relieve chronic pain in people with opioid addiction, according to a 2014 article in Anesthesiology. However, some experts believe buprenorphine isn’t an effective pain treatment in people who aren’t addicted to opioids.
If buprenorphine treatment is discontinued suddenly, individuals can experience withdrawal symptoms. If taken as prescribed and in combination with behavioral therapies, Suboxone and other buprenorphine medications increase a person’s ability to recover from addiction.