remifentanil
remifentanil.JPG

CLINICAL USE

Analgesic Induction of anaesthesia

DOSE IN NORMAL RENAL FUNCTION

Induction: 0.5–1 microgram/kg/min Maintenance: Ventilated patients: 0.05–2 mcg/kg/min —Spontaneous respiration: 25–100 —nanograms/kg/minAnalgesia and sedation in ventilated, intensive care patients: 6–740 nanograms/kg/minuteAdditional analgesia during painful procedures in ventilated, intensive care patients: 100–750 nanograms/kg/minute

PHARMACOKINETICS

  • Molecular weight                           :412.9 (as hydrochloride)
  • %Protein binding                           :70
  • %Excreted unchanged in urine     : 95 (as metabolites)
  • Volume of distribution (L/kg)       :0.35
  • half-life – normal/ESRD (hrs)      :3–10 minutes (biological activity)/unchangedTerminal elimination
  • 10 to 20     : minutes

    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                :Unlikely to be dialysed. Dose as in normal renal function
  • HD                     :Not dialysed. Dose as in normal renal function
  • HDF/high flux   :Unlikely to be dialysed. 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
  • Anti-arrhythmics: delayed absorption of mexiletine
  • Antidepressants: possible CNS excitation or depression (hypertension or hypotension) in patients also receiving MAOIs (including moclobemide) – avoid concomitant use; possibly increased sedative effects with tricyclics
  • Antipsychotics: enhanced sedative and hypotensive effect
  • Antivirals: concentration possibly increased by ritonavir (risk of toxicity) – avoidSodium oxybate: enhanced effect of sodium oxybate – avoid concomitant use

    ADMINISTRATION

    Reconstition

    To 1 mg/mL with infusion fluid

    Route

    IV

    Rate of Administration

    Dependent on indication

    Comments

    Dilute to 20–250 mcg/mL with glucose 5%, sodium chloride 0.9% or water for injection; usually 50 micrograms/mL for general anaesthesia

    OTHER INFORMATION

    Half-life of metabolite is increased to 30 hours in renal failure compared with 90 minutes in patients with normal renal functionMetabolite is essentially inactive Remifentanil would be expected to be metabolised before patient needs to be dialysed25–35% of metabolites are removed by dialysis.



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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