Acarbose

CLINICAL USE

Antidiabetic agent

DOSE IN NORMAL RENAL FUNCTION

50–200 mg 3 times a day

PHARMACOKINETICS

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

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    25–50 Dose as in normal renal function
    10–25 Avoid

  • <10           :
    Avoid

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: hypoglycaemic effectpossibly enhanced and increased
    gastrointestinal side effects with neomycin
  • Lipid lowering agents: hypoglycaemiceffect 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 concentrationsare 5 times higher than in the general
    population and the AUC is 6 times higher
  • One paper records the use of acarbosein a haemodialysis patient who had
    undergone a total gastrectomy to treat
    oxyhyperglycaemia: using a dose of
    100 mg before meals.

    with food

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