Benzbromarone

CLINICAL USE


Treatment of hyperuricaemia, chronic gout and tophaceous gout

DOSE IN NORMAL RENAL FUNCTION

50–200 mg daily(Usual dose 50–100 mg daily)

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :424.1
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :>99
  • %Excreted unchanged in urine &nbsp &nbsp : 6–18 (as metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :19 litres
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2–4

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    40–60 50–200 mg daily120–40 50–100 mg daily1<20 Avoid. Ineffective

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Avoid. Ineffective

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Avoid. Ineffective
  • HDF/high flux &nbsp :Avoid. Ineffective
  • CAV/VVHD &nbsp &nbsp &nbsp:Use with caution. Dose as in GFR=20–40 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsA
  • spirin and salicylates: antagonise uricosuric effects of benzbromarone
  • Anticoagulants: may enhance effect of warfarinPyrazinamide: antagonise uricosuric effects of benzbromarone
  • Hepatotoxic agents: enhanced hepatotoxicity

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Monitor LFTs while on benzbromarone as can cause fulminant liver failure
  • As with other uricosurics, treatment with benzbromarone should not be started during an acute attack of gout
  • Maintain an adequate fluid intake to reduce the risk of uric acid renal calculi
  • Biological effect of 100 mg benzbromarone is equivalent to 1.5 g probenecid or greater than 300 mg of allopurinol.
  • Benzbromarone is considered unsafe in patients with acute porphyria