CLINICAL USE

Type 2 diabetes mellitus

DOSE IN NORMAL RENAL FUNCTION

0.5–16 mg daily, doses given 15–30 minutes before a meal; doses up to 4 mg can be given as a single dose

PHARMACOKINETICS

  • Molecular weight                           :452.6
  • %Protein binding                           :>98
  • %Excreted unchanged in urine     : <8 (mainly as metabolites)
  • Volume of distribution (L/kg)       :30 litres
  • half-life – normal/ESRD (hrs)      :1/2

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    30–80 Dose as in normal renal function5–29 Start at a low dose and gradually increase according to response<5 Start at a low dose and gradually increase according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely to be dialysed. Dose as in GFR<5 mL/min.
  • HD                     :Not dialysed. Dose as in GFR<5 mL/min.
  • HDF/high flux   :Not dialysed. Dose as in GFR<5 mL/min.
  • CAV/VVHD      :Unlikely to be dialysed. Dose as in GFR=5–29 mL/min.

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: effects enhanced by clarithromycin and possibly trimethoprim; hypoglycaemic effect antagonised by rifampicin
  • Antifungals: effect possibly enhanced by itraconazole
  • Ciclosporin: possibly enhanced hypoglycaemic effectLipid-lowering agents: increased risk of severe hypoglycaemia with gemfibrozil – avoid concomitant use

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Major route of elimination is hepatic metabolism to inactive metabolites which are excreted via the bile.

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