nabumetone

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 :228.3

%Protein binding :>99

%Excreted unchanged in urine : <1

Volume of distribution (L/kg) :0.11

half-life – normal/ESRD (hrs) :24/391

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function, but avoid if possible

10 to 20 : 0.5–1 g daily, but avoid if possible

<10 : 0.5–1 g daily, but only use if on dialysis. See ‘Other Information’

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

HD :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Not dialysed. Dose as in GFR <10 mL/min

CAV/VVHD :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

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Route

Oral

Rate of Administration

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Comments

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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

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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