Buprenorphine

CLINICAL USE

Opioid analgesic

DOSE IN NORMAL RENAL FUNCTION

  • Sublingual: 200–400 mcg every 6–8 hours
  • IM, Slow IV: 300–600 mcg every 6–8 hours
  • Transdermal:
  • Transtec: 35–140 mcg/hour every 96 hours
  • Butrans: 5–40 mcg/hour, change patch every 7 days

    PHARMACOKINETICS

  • Molecular weight                           :467.6
  • %Protein binding                           :96
  • %Excreted unchanged in urine     : Minimal
  • Volume of distribution (L/kg)       :2.5
  • half-life – normal/ESRD (hrs)      :20–25 (Transdermal 30 hours)/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function, but avoid very large doses
  • <10           : Reduce dose by 25–50% initially and increase as tolerated; avoid very large single doses Transdermal: Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HD                     :Dialysed. Dose as in GFR
  • <10           : mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR
  • <10           : mL/min
  • CAV/VVHD      :Not dialysed. Dose as in GFR=10–20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antidepressants: possible CNS excitation or depression (hypotension or hypertension) if administered with MAOIs or moclobemide – avoid concomitant use; sedative effects possibly increased when given with tricyclics
  • Antifungals: metabolism inhibited by ketoconazole –reduce buprenorphine dose
  • Sodium oxybate: avoid concomitant use

    ADMINISTRATION

    Reconstition

    –

    Route

    Sublingual, IM, IV, transdermal

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

  • It may take up to 30 hours for plasma buprenorphine concentration to decrease by 50% after the Transtec or Butrans patch has been removed
  • Do not give another opiate for 24 hours after the Transtec or Butrans patch has been removed
  • Naloxone 5–12 mg may reverse the effects of Transtec or Butrans but the effect may be delayed by 30 minutes
  • Patches are not suitable for acute pain
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