HEALTHY LIFESTYLE




Aliskiren fumarate
Aliskiren fumarate.JPG

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                           : 1219.6
  • %Protein binding                           : 47–51
  • %Excreted unchanged in urine     : 0.6
  • Volume of distribution (L/kg)       : 135 litres
  • half-life – normal/ESRD (hrs)      : 34–41/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                : Unlikely to be dialysed. Dose as in normal renal function
  • HD                     : Unlikely to be dialysed. Dose as in normal renal function
  • HDF/high flux   : Unlikely to be dialysed. Dose as in normal renal function
  • CAV/VVHD      : 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%
  • other drugs