Leuprorelin acetate

CLINICAL USE

Treatment of advanced prostate cancer and endometriosis

DOSE IN NORMAL RENAL FUNCTION

11.25 mg every 3 months (SC depot injection, prostate cancer only)Or 3.75 mg every 4 weeks Endometriosis: 3.75 mg every month or 11.25 mg every 3 months for maximum 6 months (not to be repeated)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :1269.5

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :43–49

%Excreted unchanged in urine &nbsp &nbsp : <5 (+ metabolites)

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :27 litres

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

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 Monitor closely

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 :Unknown dialysability. 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

None known

ADMINISTRATION

Reconstition

With diluent provided

Route

IM, SC depot

Rate of Administration

–

Comments

–

OTHER INFORMATION

Women on dialysis may be at greater risk of ovarian hyperstimulation, possibly because dialysis affects circulating leuprorelin concentration so endogenous gonadotrophins were still excreted. Alternatively, haemodialysis patients may have increased responsiveness to endogenous gonadotrophinsLeuprorelin acetate.

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