Amiloride hydrochloride

CLINICAL USE

  • Oedema
  • Potassium conservation with thiazide and

    loop diuretics

    DOSE IN NORMAL RENAL FUNCTION


    5–10 mg daily; maximum 20 mg daily

    PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    302.1
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    30–40
  • %Excreted unchanged in urine &nbsp &nbsp :
    50
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    5
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    6–20/100

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


  • 20 to 50 &nbsp &nbsp : Use 50% of dose
  • 10 to 20 &nbsp &nbsp : Use 50% of dose
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :
    Avoid

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Not applicable. Avoid

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    Not applicable. Avoid
  • HDF/high flux &nbsp :
    Not applicable. Avoid
  • CAV/VVHD &nbsp &nbsp &nbsp:
    Unknown dialysability. Dose as in
    GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • ACE inhibitor and angiotensin-

    II antagonists: increased risk of
    hyperkalaemia and hypotension
    Antibacterials: avoid concomitant use with

    lymecycline

  • Antidepressants: increased risk of postural

    hypotension with tricyclics; enhanced
    hypotensive effect with MAOIs
    Antihypertensives: enhanced hypotensive

    effect

  • Ciclosporin: increased risk of

    hyperkalaemia and nephrotoxicity
    Lithium excretion reduced

  • NSAIDS: increased risk of hyperkalaemia;

    increased risk of

  • nephrotoxicity;
    antagonism of diuretic effect

  • Potassium salts: increased risk of

    hyperkalaemia

  • Tacrolimus: increased risk of

    hyperkalaemia

    ADMINISTRATION


    Reconstition



    Route


    Oral

    Rate of Administration



    Comments



    OTHER INFORMATION

  • Monitor for hyperkalaemia
  • Greatly increased risk of hyperkalaemia in

    patients with a GFR<30 mL/min, especially
    in diabetics

  • Increased risk of hyperchloraemic

    metabolic acidosis in patients with
    reduced GFR

  • Bioavailability is 50% and can be reduced

    by administering with food

  • Reduced natriuretic effect once the

    GFR<50 mL/min

  • Diuretic effect starts 2 hours after

    administration, peaks after 6–10 hours
    and can last up to 24 hours