sitagliptin
sitagliptin.JPG

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                           :523.3 (as phosphate)
  • %Protein binding                           :38
  • %Excreted unchanged in urine     : 79
  • Volume of distribution (L/kg)       :198 litres
  • half-life – normal/ESRD (hrs)      :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                :Not dialysed. Dose as in GFR>30 mL/min
  • HD                     :Not dialysed. Dose as in GFR>30 mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR>30 mL/min
  • CAV/VVHD      :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.



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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