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Created February 7, 2021, last updated almost 4 years ago.
Collection: 131, Score: 1000, Trend score: 0, Read count: 1412, Articles count: 3, Created: 2021-02-07 11:03:18 UTC. Updated: 2021-02-07 11:26:45 UTC.Notes
A. Physiochemistry
- Semi-synthetic thebaine derivative (like oxycodone).
- Partial µ-agonist.
B. Pharmacokinetics
- Dose: 0.5 mg q6h IV/IM
- 30x morphine potency
- 200mcg-400mcg sublingual qid for analgesia
- Absorption - IV, IM, s/l, epidural (po undesirable as ++ 1st pass met)
- Distribution - 3 L/kg
- Protein binding - 96%
- Onset 30 min; Offset 4 h (longer latency & duration than morph)
- Metabolism - ß½ 5 h; hepatic dealkylation & glucuronidation. Excreted in bile & hydrolysed by GIT bacteria.
- Clearance - 14 mL/min/kg (dec 30% by GA)
C. Pharmacodynamics
- Mechanism: µ partial agonist.
- 50x greater mu rec affinity than morphine.
- May be used to treat heroin/morphine dependence.
- Greater lipid solubility than morphine.
- Ceiling effect to both analgesia & respiratory depression.
- Long duration as slow to dissociate from receptor & thus difficult to reverse.
Daniel Jolley
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Collected Articles
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Reg Anesth Pain Med · Aug 2020
CommentBuprenorphine management: a conundrum for the anesthesiologist and beyond - a one-act play.
We have witnessed a worldwide upsurge of streamlined enhanced recovery after surgery (ERAS) pathways advocating for consistency and compliance within their guidelines. At a recent national conference, two experts defended their institutional policies on perioperative management of buprenorphine, one defending its continuation, while the other suggesting its discontinuation. ⋯ Although the moderator made a valid statement, we demonstrate via our one-act play the importance of recognizing a subset of the population within an ERAS pathway that necessitates multidisciplinary discussion, communication, and patient-centric care to formulate a perioperative plan coordinating a patient's care. More robust research is needed to minimize variability in current practices and to further develop comprehensive evidence-based guidelines that encompass risk factors and anticipated postsurgical and peripartum pain for patients on buprenorphine.
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There is no evidence supporting routinely ceasing buprenorphine perioperatively, even up to SL doses of 16mg/d.
pearl -
Review Meta Analysis
Efficacy and adverse effects of buprenorphine in acute pain management: systematic review and meta-analysis of randomised controlled trials.
Buprenorphine appears to have a ceiling effect on respiratory depression, but not analgesia in healthy young patients. However, the efficacy and side-effects of buprenorphine in the setting of acute pain are poorly characterized. The aim of this study was to characterize the analgesic efficacy and adverse effects of buprenorphine compared with morphine in the acute pain setting. ⋯ There was only one secondary outcome with an overall significant difference; buprenorphine use was associated with significantly less pruritus (OR=0.31; 95% CI=0.12-0.84; I2=6%; P=0.02). Whilst a theoretical ceiling effect may exist with respect to buprenorphine and respiratory depression, in a clinical setting, it can still cause significant adverse effects on respiratory function. However, given that buprenorphine is an equally efficacious analgesic agent, it is a useful alternative opioid because of its ease of administration and reduced incidence of pruritus.