Glibenclamide
Indications
Glibenclamide is used for:
Type 2 DM
Adult Dose
Oral
Type 2 diabetes mellitus
Adult: Initially, 2.5-5 mg daily, may increase wkly by increments of 2.5-15 mg daily. Doses >10 mg daily should be given in 2 divided doses. Max: 20 mg daily.
Elderly: Initially, 1.25 mg daily.
Hepatic impairment: Severe: Contraindicated.
Child Dose
Safety and efficacy not established
Renal Dose
Renal impairment: Severe: Contraindicated.
Administration
Should be taken with food. Take w/ breakfast or the 1st main meal of the day.
Contra Indications
Severe or life-threatening hyperglycaemia, severe liver or renal failure, type 1 diabetes, diabetic ketoacidosis with or without coma, patients with severe infection or trauma.
Precautions
Elderly; malnourished; mild to moderate renal and hepatic disorders. Impaired alertness. Avoid alcohol. Careful monitoring of blood-glucose concentration. Adrenocortical insufficiency. Changes in diet or prolonged exercise may also provoke hypoglycaemia. Increased risk of hypoglcaemia due to its long half-life. Avoid in severe hepatic impairment. Pregnancy, lactation.
Lactation: Not known if crosses into breast milk; avoid use in nursing women
Pregnancy-Lactation
Interactions
Serum levels may be reduced by colesevelam. May increase hypoglycaemic effect w/ MAOIs, chloramphenicol, fluoroquinolones (e.g. ciprofloxacin), probenecid, NSAIDs, ACE inhibitors, fluoxetine, disopyramide, clarithromycin, salicylates, sulfonamides, beta-blockers. Increased serum levels w/ antifungal antibiotics (e.g. miconazole, fluconazole). May decrease hypoglycaemic effect w/ nonthiazide (e.g. furosemide) and thiazide diuretics, corticosteroids, phenothiazines, thyroid agents, oestrogens, OC, phenytoin, nicotinic acid, sympathomimetic agents, rifampicin, Ca channel blockers, isoniazid.
Potentially Fatal: May increase hepatotoxic effect of bosentan.
Adverse Effects
Side effects of Glibenclamide :
Hypoglycaemia; cholestatic jaundice; agranulocytosis; aplastic anaemia; haemolytic anaemia. Blood dyscrasias (reversible), liver dysfunction, GI symptoms, allergic skin reactions.
Potentially Fatal: Prolonged hypoglycaemia seen in elderly or debilitated patients with hepatic or renal diseases.
Mechanism of Action
Glibenclamide lowers blood glucose concentration principally by stimulating secretion of endogenous insulin from the pancreatic beta-cells. Hypoglycaemic action associated w/ short-term therapy appears to include reduction of basal hepatic glucose production and enhancement of peripheral insulin action at target sites.