CLINICAL USE


NSAID and analgesic

DOSE IN NORMAL RENAL FUNCTION

1 g at night; in severe conditions 0.5–1 g in the morning as well; elderly 0.5–1 g daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :228.3
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>99
  • %Excreted unchanged in urine &nbsp &nbsp : <1

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.11

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :24/391

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function, but avoid if possible
  • 10 to 20 &nbsp &nbsp : 0.5–1 g daily, but avoid if possible
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 0.5–1 g daily, but only use if on dialysis. See ‘Other Information’

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsACE inhibitors and angiotensin-II antagonists: antagonism of hypotensive effect; increased risk of nephrotoxicity and hyperkalaemia
  • Analgesics: avoid concomitant use of 2 or more NSAIDs, including aspirin (increased side effects); avoid with ketorolac (increased risk of side effects and haemorrhage)
  • Antibacterials: possibly increased risk of convulsions with quinolones
  • Anticoagulants: effects of coumarins enhanced; possibly increased risk of bleeding with heparins and coumarins
  • Antidepressants: increased risk of bleeding with SSRIs and venlafaxineAntidiabetic agents: effects of sulphonylureas enhanced
  • Anti-epileptics: possibly increased phenytoin concentration
  • Antivirals: increased risk of haematological toxicity with zidovudine; concentration possibly increased by ritonavir
  • Ciclosporin: may potentiate nephrotoxicity Cytotoxic agents: reduced excretion of methotrexate; increased risk of bleeding with erlotinib
  • Diuretics: increased risk of nephrotoxicity; antagonism of diuretic effect; hyperkalaemia with potassium-sparing diuretics
  • Lithium: excretion decreased Pentoxifylline: increased risk of bleeding
  • Tacrolimus: increased risk of nephrotoxicity

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Nabumetone is absorbed from the GI tract and rapidly metabolised in the liver to the principal active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA). The metabolite is a potent inhibitor of prostaglandin synthesis. Excretion of the metabolite is predominantly in the urine. The SPC recommends a dose reduction if creatinine clearance <30 mL/minute
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