CLINICAL USE

Angiotensin-II antagonist:Hypertension

DOSE IN NORMAL RENAL FUNCTION

20–80 mg daily

PHARMACOKINETICS

  • Molecular weight                           :514.6
  • %Protein binding                           :>99.5
  • %Excreted unchanged in urine     : <1
  • Volume of distribution (L/kg)       :500 litres
  • half-life – normal/ESRD (hrs)      :24/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           : Start with 20 mg and adjust according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed. Dose as in GFR <10 mL/min
  • HD                     :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unlikely to be 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 NSAIDsCardiac glycosides: concentration of digoxin increased
  • 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

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Hyperkalaemia and other side effects are more common in patients with impaired renal functionClose monitoring of renal function required during therapy in patients with renal insufficiencyRenal failure has been reported in association with angiotensin-II inhibitors in patients with renal artery stenosis, post renal transplant, and those with congestive heart failure.

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