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.

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