CLINICAL USE

Analgesia for intrathecal use

DOSE IN NORMAL RENAL FUNCTION

2.4–21.6 mcg daily; majority require <9.6 mcg/day

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 2639.1 (2699.2 as acetate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 53
  • %Excreted unchanged in urine &nbsp &nbsp : <1

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 30 litres

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 1.3/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Unknown dialysability. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp : Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Contraindicated with IT chemotherapy

    ADMINISTRATION

    Reconstition

    –

    Route

    Intrathecal

    Rate of Administration

    Over 24 hours

    Comments

    Dilute with preservative-free sodium chloride 0.9%; concentration should be no lower than 5 mcg/mL in an external pump and 25 mcg/mL in an internal pump

    OTHER INFORMATION

    Use with caution in renal impairment due to lack of studies Has rarely caused rhabdomyolysis, myositis, acute renal failure and urinary retention .
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