Acarbose

CLINICAL USE


Antidiabetic agent

DOSE IN NORMAL RENAL FUNCTION


50–200 mg 3 times a day

PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    645.6
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    15
  • %Excreted unchanged in urine &nbsp &nbsp :
    1.7 (35% including
    inactive metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    0.32
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    3–9/Increased

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


    25–50 Dose as in normal renal function
    10–25 Avoid
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :
    Avoid

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Unknown dialysability. Avoid

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    Unknown dialysability. Avoid. See
    ‘Other Information’
  • HDF/high flux &nbsp :
    Unknown dialysability. Avoid. See
    ‘Other Information’
  • CAV/VVHD &nbsp &nbsp &nbsp:
    Unknown dialysability. Avoid

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • Antibacterials: hypoglycaemic effect

    possibly enhanced and increased
    gastrointestinal side effects with neomycin

  • Lipid lowering agents: hypoglycaemic

    effect possibly enhanced by colestyramine

    ADMINISTRATION


    Reconstition



    Route


    Oral

    Rate of Administration



    Comments

    OTHER INFORMATION

  • Only 1–2% of active drug is absorbed
  • In renal impairment, peak concentrations

    are 5 times higher than in the general
    population and the AUC is 6 times higher

  • One paper records the use of acarbose

    in a haemodialysis patient who had
    undergone a total gastrectomy to treat
    oxyhyperglycaemia: using a dose of
    100 mg before meals.

    with food