Flumazenil

CLINICAL USE

Reversal of sedative effects of benzodiazepines in anaesthetic, intensive care, and diagnostic procedures

DOSE IN NORMAL RENAL FUNCTION

Initially 200 micrograms over 15 seconds, then 100 micrograms at 60 second intervals if required; usual dose range 300–600 micrograms; maximum dose 1 mg, or 2 mg in intensive care situationsIf drowsiness recurs, an

IV infusion

of 100–400 micrograms per hour may be given

PHARMACOKINETICS

  • Molecular weight                           :303.3
  • %Protein binding                           :50
  • %Excreted unchanged in urine     : <0.1
  • Volume of distribution (L/kg)       :0.6–1.1
  • half-life – normal/ESRD (hrs)      :0.7–1.3/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
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in normal renal function
  • HD                     :Unknown dialysability. Dose as in normal renal function
  • HDF/high flux   :Unknown dialysability. Dose as in normal renal function
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • None known

    ADMINISTRATION

    Reconstition

    Route

    IV injection,

    IV infusion

    Rate of Administration

    See ‘Dose in normal renal function’

    Comments

    Infusion: suitable diluents include sodium chloride 0.9%, sodium chloride 0.45% and glucose 5%

    OTHER INFORMATION

    The half-life of flumazenil is shorter than those of diazepam and midazolam – patients should be closely monitored to avoid the risk of them becoming re-sedated

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