The clinical use of buprenorphine in opiate addiction: evidence and practice

Abstract

Buprenorphine is a partial μ-opioid receptor agonist that is being increasingly used in clinical practice in the treatment of opioid dependence in the UK, USA, and, elsewhere. Its unique pharmacological properties mean it is a relatively safe drug, it can be given by alternate day dispensing, and it is associated with relatively mild symptoms on withdrawal. The interpretation of the research literature on buprenorphine is however, complex, and often appears to be in conflict with how buprenorphine is used in clinical practice. This article describes these apparent contradictions, their likely explanations, and how these may further inform our clinical practice. The article also describes the clinically relevant pharmacological properties of buprenorphine, compares it to methadone, relates the evidence to clinical experience, and provides practical advice on how to manage the most common clinical techniques. The best quality evidence suggests that very rapid buprenorphine induction is not associated with a higher drop-out rate than methadone, that buprenorphine is probably as good as methadone for maintenance treatment, and is superior to methadone and α-2 adrenergic agonists for detoxification. However, buprenorphine cannot yet be considered the 'gold standard' treatment for opiate dependence because of the higher drop-out rates that may occur on induction using current techniques, its high-cost relative to methadone, and because the place of buprenorphine in treatment is still continuing to evolve.

The novel depot of buprenorphine propionate has a long‐acting effect on physical dependence on morphine

“…Buprenorphine, a semi-synthetic opioid made from thebaine [Heel et al, 1979], is an effective drug in the treatment of opioid dependence [Bickel and Amass, 1995;Jasinski et al, 1989;Law et al, 2004]. Buprenorphine has partial agonist activity at the m-opioid receptors [Bickel and Amass, 1995;Law et al, 2004] and antagonist activity at the k-receptors [Bickel and Amass, 1995;Heel et al, 1979].…”

“…Buprenorphine has partial agonist activity at the m-opioid receptors [Bickel and Amass, 1995;Law et al, 2004] and antagonist activity at the k-receptors [Bickel and Amass, 1995;Heel et al, 1979]. Buprenorphine exhibits a unique profile that offers several advantages over other opioids for the management of opioid dependence.…”

“…Buprenorphine exhibits a unique profile that offers several advantages over other opioids for the management of opioid dependence. Firstly, its partial agonist activity on m-opioid receptors enables buprenorphine to attenuate the physical dependence on other opioids but with less abuse liability [Barnett et al, 2001;Davids and Gastpar, 2004;Kosten, 2003;Kosten and Fiellin, 2004;Law et al, 2004]. This activity also contributes to a superior safety profile with a ceiling effect on its side effects, e.g., respiratory depression [Davids and Gastpar, 2004;Law et al, 2004].…”

“…Firstly, its partial agonist activity on m-opioid receptors enables buprenorphine to attenuate the physical dependence on other opioids but with less abuse liability [Barnett et al, 2001;Davids and Gastpar, 2004;Kosten, 2003;Kosten and Fiellin, 2004;Law et al, 2004]. This activity also contributes to a superior safety profile with a ceiling effect on its side effects, e.g., respiratory depression [Davids and Gastpar, 2004;Law et al, 2004]. Secondly, its antagonist activity on the k-receptors precludes dysphoric effects, a common side effect related to opioid use [Barnett et al, 2001;Davids and Gastpar, 2004;Law et al, 2004].…”

“…This activity also contributes to a superior safety profile with a ceiling effect on its side effects, e.g., respiratory depression [Davids and Gastpar, 2004;Law et al, 2004]. Secondly, its antagonist activity on the k-receptors precludes dysphoric effects, a common side effect related to opioid use [Barnett et al, 2001;Davids and Gastpar, 2004;Law et al, 2004]. This activity also contributes to a sense of normality and less abuse liability [Law et al, 2004].…”