Eprosartan

CLINICAL USE

Angiotensin-II antagonist:Hypertension

DOSE IN NORMAL RENAL FUNCTION

300–800 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :520.6 (as mesilate)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :98

%Excreted unchanged in urine &nbsp &nbsp : <2 (as metabolites)

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :13 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :5–9/unchanged

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 Initially 300 mg daily and increase according to response

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 :Not dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Not dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

Analgesics: antagonism of hypotensive effect and increased risk of renal impairment with NSAIDs; hyperkalaemia with ketorolac and other NSAIDs

Ciclosporin: increased risk of hyperkalaemia and nephrotoxicity

Diuretics: enhanced hypotensive effect; hyperkalaemia with potassium-sparing diuretics

Epoetin: increased risk of hyperkalaemia; antagonism of hypotensive effect

Lithium: reduced excretion, possibility of enhanced lithium toxicity

Potassium salts: increased risk of hyperkalaemia

Tacrolimus: increased risk of hyperkalaemia and nephrotoxicity

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Side effects (e.g. hyperkalaemia, metabolic acidosis) are more common in patients with impaired renal functionClose monitoring of renal function during therapy is necessary in those with renal insufficiencyRenal failure has been reported in association with AT-II antagonists in patients with renal artery stenosis, post renal transplant, and in those with severe congestive heart failure.

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