What is Buprenorphine?

What is Buprenorphine?

By Dr.Fourkan Ali

Buprenorphine Brand names:
Suboxone^®1, Subutex^®2, Zubsolv^®3, Bunavail^™4, Probuphine^®5

Summary: The purpose of buprenorphine treatment is not to assist in detox or to maintain a person's customary opioid use, but to suppress the debilitating symptoms of cravings and withdrawal. This enables the patient to engage in therapy, counseling and support, which they use to implement positive long-term changes in their lives. It's these changes that develop into the new healthy patterns of behavior necessary to achieve sustained addiction remission.

Recovery is a self-reconditioning process which buprenorphine makes possible by suppressing the cravings and withdrawal.

But as you will see, simply taking the medication isn't enough. To be effective the medication must be accompanied by the behavioral changes because that is what ultimately reverses the brain adaptations of addiction.⁶

Buprenorphine

Suboxone(bup/nx) tablets

Buprenorphine is an opioid medication used to treat opioid addiction in the privacy of a physician's office. It can be dispensed for take-home use, by prescription. This, in addition to the pharmacological and safety profile, makes it an attractive treatment for patients addicted to opioids.

At the correct dose, buprenorphine suppresses cravings and withdrawal symptoms and blocks the effects of other opioids.

Buprenorphine is not new. It was first patented in 1969 and has been used in the U.S. to treat pain and in Europe to treat pain and opioid addiction for over 20 years, and is a semi-synthetic opioid and is a partial agonist.

·         Opioid Agonists are drugs that cause an opioid effect like heroin, oxycodone, hydrocodone, and methadone.

·         Opioid Antagonists are drugs that block and reverse the effects of agonist drugs. Narcan^® is an antagonist and is used to reverse heroin overdoses.

Fig. 1. Unlike full agonist opioids, buprenorphine has a limit to its effects

Buprenorphine can act as both an agonist and antagonist. It attaches to the opioid receptors but only activates them partially, enough to suppress withdrawal and cravings, but not enough to cause extreme euphoria in opioid-tolerant patients. When all available receptors are occupied with buprenorphine, no additional opioid effect is produced by taking more. This is called the 'ceiling effect'. The antagonist property of the medication expels, replaces and blocks other opioids from the opioid receptor sites. Therefore, if the patient decides to misuse opioid drugs after taking buprenorphine, the effects can be blocked, depending on dosage. Alternately, if taken too soon after other opioids, by an opioid-physically dependent patient, the buprenorphine can precipitate withdrawal. The ceiling effect, blocking ability, and possibility of precipitating withdrawal, contribute to buprenorphine having a favorable safety profile and helps lower the risk of overdose and misuse.⁵

Buprenorphine (Bup) and 
Buprenorphine / Naloxone (bup/nx) combination

In October 2002 the FDA approved the first two prescription bup medications for the treatment of opioid addiction; Subutex^® (bup) and Suboxone^® (bup/nx). Since 2009 the FDA approved generic bup and bup/nx sublingual tablets, the brand-name bup/nx sublingual tablet called Zubsolv^® and a buccal film bup/nx product called Bunavail^™. Both Suboxone and Subutex tablets were discontinued and replaced with Suboxone Film^® which is a bup/nx sublingual film.

Suboxone Film single-unit packaging bup/nx 8/2mg.

The only reason for the addition of naloxone is to discourage misuse by injection. If the bup/nx combination is injected, the naloxone can help cause immediate withdrawal symptoms in opioid-physically dependent people. However, naloxone is poorly absorbed sublingually. Therefore, when taken as directed, very little naloxone enters the blood. Normally, patients are unaffected by the presence of it, and it is considered clinically insignificant. Buprenorphine itself can cause withdrawal in physically dependent people misusing full agonist opioids. Naloxone may only slightly attenuate the effects of buprenorphine if misused by injection.

Generic bup/nx 8/4mg 2/1mg

Isn't buprenorphine just switching one addiction for another?

No, because once stabilized in bup or bup/nx treatment, the compulsive behavior, the loss of control of drug use, the constant cravings, and all of the other hallmarks of addiction vanish. When all signs and symptoms of the disease of addiction vanish, we call that remission, not switching addictions. Remember, it is the uncontrollable compulsive behavior that we're looking to stop, because that's what's destructive, not taking a medication. Switching addictions, would mean you have lost control of your buprenorphine use, use it compulsively, and continually crave your buprenorphine. Generally none of this is experienced by typical buprenorphine patients, although it is possible and should be watched for. Instead most buprenorphine patients have complete control of their buprenorphine use, don't use it compulsively and don't crave it.

Yes, a physical dependence to opioids remains and is maintained by the buprenorphine, but physical dependence is not addiction, does not destroy lives, and is relatively easy to reverse with a slow taper off of the medication at the appropriate time.

With all the drug war propaganda we've been exposed to it's easy to mistake the problem as a drug problem when really it is the addiction that is destructive. Don't make the mistake of dismissing evidence-based treatments because you think you have a drug problem and taking drugs for a drug problem seems counter productive. It's not a drug problem, it's an addiction problem and if a drug is needed to stop the addiction then so be it.