Losartan

CLINICAL USE

Angiotensin-II receptor antagonist:Hypertension Type 2 diabetic nephropathy

DOSE IN NORMAL RENAL FUNCTION

25–100 mg daily

PHARMACOKINETICS

  • Molecular weight                           :461
  • %Protein binding                           :>98
  • %Excreted unchanged in urine     : 4
  • Volume of distribution (L/kg)       :0.4
  • half-life – normal/ESRD (hrs)      :1.5–2.5 (active metabolite 3–9)/4–6

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Initial dose 25 mg and titrate according to response
  • <10           : Initial dose 25 mg and titrate 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   :Not dialysed. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Not dialysed. Dose as in GFR=10–20 mL/min

    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

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Adverse reactions, especially hyperkalaemia are more common in patients with renal impairmentRenal failure has been reported in association with angiotensin-II antagonists in patients with renal artery stenosis, post renal transplant, and in those with congestive heart failureClose monitoring of renal function during therapy is necessary in those with renal insufficiencyLosartan potassium.

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