CLINICAL USE


Treatment of type 2 diabetes in combination with metformin or a thiazolidinedione

DOSE IN NORMAL RENAL FUNCTION

100 mg once daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :523.3 (as phosphate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :38
  • %Excreted unchanged in urine &nbsp &nbsp : 79

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :198 litres

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :12.4/Probably increased

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    30–50 50 mg once daily<30 25 mg once daily

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR>30 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR>30 mL/min
  • HDF/high flux &nbsp :Dialysed. Dose as in GFR>30 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR>30 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • None known

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    13.5% of dose is removed during a 3–4 hour haemodialysis sessionIn severe renal impairment (GFR<30 mL/min) the AUC was increased 4-fold50 mg and 25 mg tablets are only available in the USA at present.
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