Penicillamine.txt

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 &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :149.2

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :80

%Excreted unchanged in urine &nbsp &nbsp : 10–40

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.8

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :1–3/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Avoid if possible or reduce dose. 125 mg for first 12 weeks. Increase by same amount every 12 weeks

10 to 20 &nbsp &nbsp : Avoid – nephrotoxic

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Avoid – nephrotoxic

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Avoid – nephrotoxic

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. 125–250 mg 3 times a week after

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :

HDF/high flux &nbsp :Dialysed. 125–250 mg 3 times a week after

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :

CAV/VVHD &nbsp &nbsp &nbsp: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

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Route

Oral

Rate of Administration

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Comments

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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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