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 :296.5

%Protein binding :96

%Excreted unchanged in urine : 70–76 (as metabolites)

Volume of distribution (L/kg) :No data

half-life – normal/ESRD (hrs) :12/–

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Use with caution

<10 : Avoid

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unlikely to be dialysed. Avoid

HD :Unlikely to be dialysed. Avoid

HDF/high flux :Unlikely to be dialysed. Avoid

CAV/VVHD :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

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Route

Oral

Rate of Administration

–

Comments

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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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