Leflunomide

CLINICAL USE

Disease modifying agent:Active rheumatoid arthritis Psoriatic arthritis

DOSE IN NORMAL RENAL FUNCTION

Rheumatoid arthritis: 100 mg daily for 3 days then

10 to 20 : mg dailyPsoriatic arthritis: 100 mg daily for 3 days then 20 mg daily

PHARMACOKINETICS

Molecular weight :270.2

%Protein binding :>99

%Excreted unchanged in urine : 0

Volume of distribution (L/kg) :11 litres

half-life – normal/ESRD (hrs) :2 weeks (metabolite)/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Use with caution.

<10 : Use with caution.

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Not dialysed. Use with caution

HD :Not dialysed. Use with caution

HDF/high flux :Not dialysed. Use with caution

CAV/VVHD :Not dialysed. Use with caution

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsHepatotoxic or haemotoxic drugs: increased risk of toxicityLipid-lowering agents: effect significantly reduced by colestyramineLive vaccines: avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

–

Comments

Administer with food

OTHER INFORMATION

Contraindicated by manufacturer due to insufficient evidenceUS licence says it can be used in renal impairment with cautionProtein binding is variable in CKD In haemodialysis and PD the free fraction of the active metabolite in plasma is doubled

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