CLINICAL USE

Hypoglycaemic agent for non-insulin dependent diabetes

DOSE IN NORMAL RENAL FUNCTION

0.5–2 g daily in divided doses

PHARMACOKINETICS

  • Molecular weight                           : 270.3
  • %Protein binding                           : 95–97
  • %Excreted unchanged in urine     : 0
  • Volume of distribution (L/kg)       : 0.1–0.15
  • half-life – normal/ESRD (hrs)      : 4–7/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function. Use with caution
  • 10 to 20     : Dose as in normal renal function. Use with caution
  • <10           : Dose as in normal renal function. Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                : Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HD                     : Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   : Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      : Not dialysed. Dose as in GFR=10– 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Analgesics: effects enhanced by NSAIDs – avoid with azapropazone
  • Antibacterials: effects enhanced by chloramphenicol, sulphonamides, and trimethoprim; effect reduced by rifamycins
  • Anticoagulants: effect possibly enhanced by coumarins; also possibly changes to INR
  • Antifungals: concentration increased by fluconazole and miconazole, and possibly voriconazole Sulfinpyrazone: enhanced effect of sulphonylureas

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Tolbutamide is not removed by dialysis. It is contraindicated in severe renal impairment, and should be used with great caution in mild to moderate renal impairment because of risk of hypoglycaemia .

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