Practical considerations for the clinical use of buprenorphine

Abstract

Buprenorphine is a new and attractive medication option for many opioid-addicted adults and their physicians. Before initiating buprenorphine treatment, providers must be aware of such critical factors as how the medication works, its efficacy and safety profile, how it is used in opioid withdrawal as well as maintenance treatment, and how patients can best be selected, educated about buprenorphine, and monitored throughout treatment. This article reviews these important issues as well as requirements for physician and staff training and needs for additional research on this unique medication.

Heroin, Buprenorphine, and Naloxone Effects at the Mu Opioid Receptor

Heroin, buprenorphine, and naloxone (represented above by blue polygons) produce contrasting effects because they interact differently with the brain’s mu opioid receptors (red pentagons). First, the chemicals differ in how much each stimulates the receptors (represented above by the percentage of receptor “activity zone” each fills). The stronger the stimulation, the more pronounced will be the opioid effects of pain relief, feelings of well-being, respiratory depression, and so on. Heroin, classified as a full receptor agonist (stimulator), nearly fills the activity zone. Buprenorphine, a partial receptor agonist, fills a smaller portion of it. Naloxone does not stimulate the receptor at all. Second, each chemical binds to the receptors more or less strongly (represented above by the percentage of receptor “affinity zone” it fills). A chemical that forms a tighter bond can push one with a weaker bond off the receptors and take its place. Thus, buprenorphine can push heroin off the receptors, and in doing so replace heroin’s full receptor stimulation with its own partial stimulation. Buprenorphine also binds more tightly than naloxone. Naloxone can compete with heroin for the receptors. Because naloxone can block heroin and other opioids from stimulating the receptors while not itself stimulating them, it can precipitate opioid withdrawal and is classified as an opioid receptor “antagonist.”