Chlorpropamide

CLINICAL USE

Diabetes mellitus Diabetes insipidus

DOSE IN NORMAL RENAL FUNCTION

Diabetes mellitus: initially 250 mg daily (elderly 100–125 mg, but avoid). Maximum 500 mg dailyDiabetes insipidus: 100–350 mg daily

PHARMACOKINETICS

  • Molecular weight                           :276.7
  • %Protein binding                           :88–96
  • %Excreted unchanged in urine     : 47
  • Volume of distribution (L/kg)       :0.09–0.27
  • half-life – normal/ESRD (hrs)      :35/50–200

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : 50% of normal dose
  • 10 to 20     : Avoid. See ‘Other Information’
  • <10           : Avoid. See ‘Other Information’

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed. Avoid
  • HD                     :Not dialysed. Avoid
  • HDF/high flux   :Unknown dialysability. Avoid
  • CAV/VVHD      :Unknown dialysability. Avoid

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsAnalgesics: effects enhanced by NSAIDs Antibacterials: effects enhanced by chloramphenicol, sulphonamides, and trimethoprim; effect reduced by rifamycinsAnticoagulants: effect possibly enhanced by coumarins; also possibly changes to INRAntifungals: concentration increased by fluconazole and miconazole and possibly voriconazoleSulfinpyrazone: enhanced effect of sulphonylureas

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    Take with breakfast

    OTHER INFORMATION

    Chlorpropamide can enhance antidiuretic hormone and very rarely cause hyponatraemiaContraindicated in patients with serious impairment of hepatic, renal or thyroid function – severe risk of metabolic acidosis Prolonged hypoglycaemia can occur in azotaemic patients

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