Aliskiren fumarate

CLINICAL USE

Renin inhibitor, used for hypertension and
diabetic nephropathy

DOSE IN NORMAL RENAL FUNCTION

150–300 mg once daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
1219.6

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
47–51

%Excreted unchanged in urine &nbsp &nbsp :
0.6

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

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
34–41/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

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

Other antihypertensive agents: enhanced

antihypertensive effect; concentration
possibly reduced by irbesartan

Antifungals: plasma concentration of

aliskiren increased by ketoconazole

Diuretics: may reduce concentration

of furosemide; hyperkalaemia with
potassium-sparing diuretics

Heparins: increased risk of hyperkalaemia

Potassium salts: increased risk of

hyperkalaemia

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Potassium should be monitored in patients

with renal impairment, diabetes or heart
failure

Oral bioavailability is only 2–3%

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