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Why is this important?
Buprenorphine (Subutex, Tamgesic, Suboxone, Norspan) is a partial opioid agonist with high mu-receptor affinity, though limited by a ceiling effect. Because of its favourable safety profile it is used for opioid dependence, chronic and, increasingly, acute pain.1
Patients historically often have regular buprenorphine (BUP) ceased post-operatively when needing opioid analgesia. It was assumed that because of it’s high mu-receptor affinity, BUP blocks the efficacy of additional opioid analgesics. In reality, ceasing buprenorphine creates more complexity and may precipitate acute withdrawal.
Be smart
Haber, DeFries & Martin point out that despite the high receptor affinity of BUP, there are still additional receptors remaining for full-agonist opioids to bind and activate. This is supported by the literature (Kornfeld 2010 & Harrison 2018). Even in the post-operative period buprenorphine can be easily continued, although with patients sometimes needing higher doses of acute opioid analgesics (Goel 2019 & Hansen 2016).
“Temporarily discontinuing buprenorphine introduces unnecessary complexity to a hospitalization, places the patient at risk of exacerbation of pain, opioid withdrawal...“
Bottom-line
If buprenorphine is regularly being taken then it should not be ceased for hospital admission. Additional short-acting opioids can be added if needed. Doses required may be higher, but this is primarily due to opioid tolerance rather than receptor competition with BUP. Alternatively, a maintenance BUP dose can be split into 3-4 divided doses and/or increased to cover acute analgesic needs.
summary
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Buprenorphine is also a kappa and delta receptor antagonist, a weak partial NOP/Nociceptin receptor agonist, and has potent local anaesthetic effects. It behaves as a full agonist for analgesia in the opioid-naive, but a partial agonist for respiratory depression. ↩
- Lawrence A Haber, Triveni DeFries, and Marlene Martin.
- Division of Hospital Medicine, Priscilla Chan and Mark Zuckerberg San Francisco General Hospital and Trauma Center, Department of Medicine, University of California, San Francisco, San Francisco, California.
- J Hosp Med. 2019 Oct 1; 14 (10): 633-635.
no abstract available
Notes
Why is this important?
Buprenorphine (Subutex, Tamgesic, Suboxone, Norspan) is a partial opioid agonist with high mu-receptor affinity, though limited by a ceiling effect. Because of its favourable safety profile it is used for opioid dependence, chronic and, increasingly, acute pain.1
Patients historically often have regular buprenorphine (BUP) ceased post-operatively when needing opioid analgesia. It was assumed that because of it’s high mu-receptor affinity, BUP blocks the efficacy of additional opioid analgesics. In reality, ceasing buprenorphine creates more complexity and may precipitate acute withdrawal.
Be smart
Haber, DeFries & Martin point out that despite the high receptor affinity of BUP, there are still additional receptors remaining for full-agonist opioids to bind and activate. This is supported by the literature (Kornfeld 2010 & Harrison 2018). Even in the post-operative period buprenorphine can be easily continued, although with patients sometimes needing higher doses of acute opioid analgesics (Goel 2019 & Hansen 2016).
“Temporarily discontinuing buprenorphine introduces unnecessary complexity to a hospitalization, places the patient at risk of exacerbation of pain, opioid withdrawal...“
Bottom-line
If buprenorphine is regularly being taken then it should not be ceased for hospital admission. Additional short-acting opioids can be added if needed. Doses required may be higher, but this is primarily due to opioid tolerance rather than receptor competition with BUP. Alternatively, a maintenance BUP dose can be split into 3-4 divided doses and/or increased to cover acute analgesic needs.
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Buprenorphine is also a kappa and delta receptor antagonist, a weak partial NOP/Nociceptin receptor agonist, and has potent local anaesthetic effects. It behaves as a full agonist for analgesia in the opioid-naive, but a partial agonist for respiratory depression. ↩
Daniel Jolley
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