Estramustine phosphate

CLINICAL USE

Alkylating agent:Prostate cancer

DOSE IN NORMAL RENAL FUNCTION

0.14–1.4 g daily in divided doses (usual initial dose 560–840 mg daily)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :564.3 (as sodium phosphate)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :No data

%Excreted unchanged in urine &nbsp &nbsp : 22–36

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.431

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :10 (estromustine: 20)

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, use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

None known

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

Don’t give less than 1 hour before or 2 hours after meals

OTHER INFORMATION

Can cause fluid retention so use with caution in renal impairmentEstramustine phosphate sodium is rapidly dephosphorylated in the intestine and prostate to estramustine and estromustine, which accumulate in the prostatic tissue. The plasma half-lives of these metabolites are

10 to 20 &nbsp &nbsp : hours. Estramustine and estromustine are further metabolised before excretion

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