HEALTHY LIFESTYLE




Glibenclamide
Glibenclamide.JPG

Glibenclamide

CLINICAL USE

Non-insulin dependent diabetes mellitus

DOSE IN NORMAL RENAL FUNCTION

Initially 5 mg daily (elderly patients – 2.5 mg) adjusted according to response; maximum 15 mg daily

PHARMACOKINETICS

  • Molecular weight                           :494
  • %Protein binding                           :97
  • %Excreted unchanged in urine     : <5
  • Volume of distribution (L/kg)       :0.125
  • half-life – normal/ESRD (hrs)      :2.1–10/–

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Initial dose of 1.25–2.5 mg once a day. Monitor closely
  • 10 to 20     : Initial dose of 1.25–2.5 mg once a day. Monitor closely
  • <10           : Initial dose of 1.25–2.5 mg once a day. Use cautiously, with continuous monitoring

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Analgesics: effects enhanced by NSAIDs
  • Antibacterials: effects enhanced by chloramphenicol, sulphonamides, and trimethoprim; effects possibly enhanced by ciprofloxacin and norfloxacin; effect reduced by rifamycins
  • Anticoagulants: effect possibly enhanced by coumarins; also possibly changes to INR
  • Antifungals: concentration increased by fluconazole and miconazole and possibly voriconazoleBosentan: increased risk of hepatoxicity – avoid concomitant use
  • Ciclosporin: may increase ciclosporin levelsSulfinpyrazone: enhanced effect of sulphonylureas

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    Take with breakfast

    OTHER INFORMATION

    Metabolites of glibenclamide are only weakly hypoglycaemic; this is not clinically relevant where renal and hepatic functions are normal. If creatinine clearance
  • <10           : mL/min, accumulation of metabolite and unchanged drug in plasma may cause prolonged hypoglycaemiaCompany information states that use is contraindicated in severe renal impairmentCompensatory excretion via bile in faeces occurs in renal impairment.
  • other drugs