CLINICAL USE

Rheumatoid arthritis

DOSE IN NORMAL RENAL FUNCTION

125–250 mg daily for first month; increase by same amount every 4–12 weeks until remission occursMaintenance dose: usually 500–750 mg daily in divided dosesMaximum 1.5 g daily

PHARMACOKINETICS

  • Molecular weight                           :149.2
  • %Protein binding                           :80
  • %Excreted unchanged in urine     : 10–40
  • Volume of distribution (L/kg)       :0.8
  • half-life – normal/ESRD (hrs)      :1–3/Increased

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Avoid if possible or reduce dose. 125 mg for first 12 weeks. Increase by same amount every 12 weeks
  • 10 to 20     : Avoid – nephrotoxic
  • <10           : Avoid – nephrotoxic

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Avoid – nephrotoxic
  • HD                     :Dialysed. 125–250 mg 3 times a week after
  • HD                     :
  • HDF/high flux   :Dialysed. 125–250 mg 3 times a week after
  • HD                     :
  • CAV/VVHD      :Unknown dialysability. Avoid – nephrotoxic

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antipsychotics: avoid concomitant use with clozapine (increased risk of agranulocytosis)

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Proteinuria occurs frequently and is partially dose-related. In some patients it may progress to glomerulonephritis or nephrotic syndromeUrinalysis should be carried out weekly for the first two months of treatment, after any change in dosage, and monthly thereafter. Increasing proteinuria may necessitate withdrawal of treatment.

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