disulfiram

CLINICAL USE


Adjunct in the treatment of chronic alcohol dependence

DOSE IN NORMAL RENAL FUNCTION

800 mg on day 1 reducing over 5 days to 100–200 mg daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :296.5
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :96
  • %Excreted unchanged in urine &nbsp &nbsp : 70–76 (as metabolites)

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :No data

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :12/–

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Use with caution
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Avoid

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Avoid

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be dialysed. Avoid
  • HDF/high flux &nbsp :Unlikely to be dialysed. Avoid
  • CAV/VVHD &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsAlcohol: risk of severe disulfiram reaction Anticoagulants: enhanced anticoagulant effect with coumarinsAnti-epileptics: inhibition of metabolism of phenytoin (increased risk of toxicity)Paraldehyde: increased risk of toxicity with paraldehyde

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Review after 6 months Patients should be warned about severe nature of alcohol and disulfiram reactionContraindicated in cardiovascular disease, psychoses or severe personality disordersDisulfiram blocks the metabolism of alcohol and leads to an accumulation of acetaldehyde in the bloodstream. Use with caution in diabeticsDisulfiram is rapidly metabolised to diethyldithiocarbamic acid (DDC); is conjugated with glucuronic acid, oxidised to sulphate, methylated, and decomposed to diethylamine and carbon disulphide. Excretion is primarily through the kidneys
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