Ezetimibe

CLINICAL USE

Hypercholesterolaemia either in combination with a statin or as monotherapy

DOSE IN NORMAL RENAL FUNCTION

10 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :409.4

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :99.7

%Excreted unchanged in urine &nbsp &nbsp : 11

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

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :22/–

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Unlikely to be dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Ciclosporin: concentration of both drugs possibly increasedFibrates: avoid concomitant administration

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

When used with a statin LFTs should be monitored before initiation of therapy and then at regular intervalsIf GFR<30 mL/min there is a 1.5 increase in the AUC of ezetimibe but no dose adjustment is requiredVery rarely, cases of rhabdomyolysis have occurred – discontinue if myopathy is suspected

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