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  Buprenorphine

  Analgesia Buprenorphine Drugs Opioid

   

  A. Physiochemistry

  • Semi-synthetic thebaine derivative (like oxycodone).
  • Partial µ-agonist.

  B. Pharmacokinetics

  1. Dose: 0.5 mg q6h IV/IM
     • 30x morphine potency
     • 200mcg-400mcg sublingual qid  for analgesia
  2. Absorption - IV, IM, s/l, epidural (po undesirable as ++ 1st pass met)
  3. Distribution - 3 L/kg
  4. Protein binding - 96%
  5. Onset 30 min; Offset 4 h (longer latency & duration than morph)
  6. Metabolism - ß½ 5 h; hepatic dealkylation & glucuronidation. Excreted in bile & hydrolysed by GIT bacteria.
  7. Clearance - 14 mL/min/kg (dec 30% by GA)

  C. Pharmacodynamics

  1. 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.

  reference

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  • Comment

    Buprenorphine management: a conundrum for the anesthesiologist and beyond - a one-act play.

    Reg Anesth Pain Med. 2020 Aug 1; 45 (8): 656-659.

  • Article

    The perioperative patient on buprenorphine: a systematic review of perioperative management strategies and patient outcomes.

    Can J Anaesth. 2019 Feb 1; 66 (2): 201-217.

    There is no evidence supporting routinely ceasing buprenorphine perioperatively, even up to SL doses of 16mg/d.

    pearl

  • Review

    Efficacy and adverse effects of buprenorphine in acute pain management: systematic review and meta-analysis of randomised controlled trials.

    Br J Anaesth. 2018 Apr 1; 120 (4): 668-678.

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