Enalapril maleate

CLINICAL USE


Angiotensin converting enzyme inhibitor:Hypertension Heart failure

DOSE IN NORMAL RENAL FUNCTION

2.5–40 mg daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :492.5
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :50–60
  • %Excreted unchanged in urine &nbsp &nbsp : 20

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.171

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :11/34–60

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Start with 2.5 mg per day and increase according to response
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start with 2.5 mg per day and increase according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min
  • HDF/high flux &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp: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

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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 ACE inhibitors in patients with renal artery stenosis, post renal transplant, and in those with severe congestive heart failureHigh incidence of anaphylactoid reactions has been reported in patients dialysed with high-flux polyacrylonitrile membranes and treated concomitantly with an ACE inhibitor – this combination should therefore be avoidedACE inhibitor cough may be helped by sodium cromoglycate inhalersEnalapril maleate is a prodrug that requires hepatic conversion to enalaprilatEnalaprilat injection available on a named patient basis
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