Buprenorphine (BYOO-pre-NOR-feen)

Buprenorphine is a drug used to treat patients who have become dependent on or addicted to pain-killers or heroin.  It was approved for clinical use by the FDA in 2002.  When taken as prescribed, it is safe and highly effective.  Buprenorphine has been marketed in different forms under the names Suboxone, Subutex, Zubsolv and Bunavail.  All of these brands work the same way and are taken under the tongue where they dissolve and enter the blood stream through the veins.  Unlike methadone, which must be administered daily through a structured clinic, buprenorphine is the first medication to treat opioid dependency that is permitted to be prescribed or dispensed in physician offices.  Only certified physicians may prescribe buprenorphine.

How Buprenorphine Works

Opioids attach to receptors in the brain, with three main effects; respiration depression (slowed breathing), euphoria (sensation of pleasure), decreased pain. The more opioids ingested the more of an effect. The process of opioids binding to receptors can be thought of as a mechanical union, the better the fit the more the opioid effect. Opioids that fit perfectly are called full agonists.  Examples are heroin, oxycodone and morphine. Buprenorphine is different. It too binds to opioid receptors, however, without a perfect fit.  It is therefore referred to as a “partial” agonist.  As a result, the Buprenorphine tends to occupy the receptors without all of the opioid effects. Essentially the receptor is “tricked” into thinking it has been satisfied with opioids thereby alleviating cravings and withdrawal without producing strong feelings of euphoria and without causing significant respiratory depression. This, in turn, prevents that receptor from binding with other opioids; therefore if the patient uses heroin or painkillers, they are unlikely to experience any effect. Buprenorphine also tends to bind strongly with opioid receptors, blocking them much longer than other opioids. This strong binding makes buprenorphine last longer.  These characteristics make Buprenorphine uniquely suited to treat opioid dependence.

Side effects of Buprenorphine

Buprenorphine has many of the same side effects as other opioids including constipation and sedation.  However, the most common complained of side effects include headache and insomnia.  Other side effects that can occur include nausea, vomiting and abdominal pain.  That said, the vast majority of patients tolerate buprenorphine well.


Layne K. Kamalu MD
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