Buprenorphine for Chronic Pain: A Review of the Clinical Effectiveness [Internet].

Buprenorphine is an opioid analgesic available in Canada as transdermal patches and sublingual tablets (tablets also contain naloxone)., Buprenorphine/naloxone is indicated for substitution treatment in opioid drug dependence in adults whereas transdermal buprenorphine is indicated for the management of pain severe enough to require daily, continuous, long-term opioid treatment. Buprenorphine produces typical opioid agonist effects and in higher doses its agonist effects reach a ceiling and it can act as an antagonist. This property distinguishes it from morphine. It has high affinity for mu opioid receptors but only weakly activates them. For this reason, buprenorphine may be less likely to cause respiratory depression than full opioid agonists such as fentanyl or morphine. When buprenorphine is given concomitantly with other opioids, it antagonizes the effects of the other opioids by displacing them from the mu receptors. This can lead to withdrawal syndrome if buprenorphine is added to another opioid. If buprenorphine is withdrawn while the dose of the other opioid is being increased, it can increase the risk of overdose.

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