CLINICAL USE

Opiate analgesic

DOSE IN NORMAL RENAL FUNCTION

5–20 mg every 4 hours (higher in very severe pain or terminal illness)PR: 15–30 mg every 4 hours

PHARMACOKINETICS

  • Molecular weight                           :285.3 (758.8 as sulphate); (774.8 as tartrate)
  • %Protein binding                           :20–35
  • %Excreted unchanged in urine     : 10
  • Volume of distribution (L/kg)       :3–5
  • half-life – normal/ESRD (hrs)      :2–3/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : 75% of normal dose
  • 10 to 20     : Use small doses, e.g. 2.5–5 mg and extended dosing intervals. Titrate according to response
  • <10           : Use small doses, e.g. 1.25–2.5 mg and extended dosing intervals. Titrate according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antidepressants: possible CNS excitation or depression with MAOIs – avoid concomitant use, and for 2 weeks after stopping MAOI; possible CNS excitation or depression with moclobemide; increased sedative effects with tricyclics
  • Antivirals: concentration possibly increased by ritonavirSodium oxybate: enhanced effect of sodium oxybate – avoid concomitant use

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral, SC, IM, IV, PR

    Rate of Administration

    2 mg/minute. (Titrate according to response)

    Comments

    –

    OTHER INFORMATION

    Extreme caution with all opiates in patients with impaired renal functionPotential accumulation of morphine-6- glucuronide (a renally excreted active metabolite, more potent than morphine) and morphine-3-glucuronide. Half-life of morphine-6-glucuronide is increased from 3–5 hours in normal renal function to about 50 hours in ERFENSURE NALOXONE READILY AVAILABLESome units avoid slow release oral preparations as any side effects may be prolonged.

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