Misoprostol

CLINICAL USE

Benign gastric and duodenal ulceration and NSAID associated ulcerationProphylaxis of NSAID induced ulceration

DOSE IN NORMAL RENAL FUNCTION

Treatment: 800 mcg daily in 2 or 4 divided dosesProphylaxis: 200 mcg 2–4 times daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :382.5

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :<90 (as misoprostol acid)

%Excreted unchanged in urine &nbsp &nbsp : <1

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :858 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :20–40 minutes/ 40–80 minutes (as misoprostol acid)

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 :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

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Plasma concentrations of misoprostol are generally undetectable due to its rapid metabolic conversion to misoprostol acidDosage adjustment is not usually necessary in patients with varying degrees of renal impairment, even though there is an approximate doubling of half-life, maximum plasma concentration and area under the curve. If renal patients are unable to tolerate it, the dose can be reduced.

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