Glibenclamide

Indications
Oral
Type 2 diabetes mellitus
Adult: Initially, 2.5-5 mg daily, may increase wkly by increments of 2.5 mg daily, up to 15 mg daily. Doses >10 mg daily should be given in 2 divided doses. Max: 20 mg daily.
Elderly: Initially, 1.25-2.5 mg daily, may increase by 1.25-2.5 mg daily every 1-3 wk, if needed.
Contraindications
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.
Warnings / 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.
Adverse Reactions
Hypoglycaemia; cholestatic jaundice; agranulocytosis; aplastic anaemia; haemolytic anaemia. Blood dyscrasias (reversible), liver dysfunction, hypoglycaemia, GI symptoms, allergic skin reactions.
Potentially Fatal: Prolonged hypoglycaemia seen in elderly or debilitated patients with hepatic or renal diseases.
Drug Interactions
Increased risk of hypoglycaemia when used with β-blockers. Additive hypoglycaemic effect with insulin and other antidiabetic drugs. Metabolism may be reduced by chloramphenicol and cimetidine. Increased hypoglycemic effect when used with cyclic antidepressants, pegvisomant, corticosteroids, salicylates, sulfonamide derivatives (except sulfacetamide) or fibric acid derivatives. Concurrent use may increase serum levels of ciclosporin. Increased serum levels when used with fluconazole. Metabolism of glibenclamide may be increased when used with rifampin. Concurrent use with coumarin derivatives may cause changes in INR. Concurrent admin with chloestyramine resin may lead to reduced absorption of glibenclamide. Serum levels may be reduced by colesevelam. Therapeutic efficacy may be diminished by luteinizing-hormone releasing hormone analogs. Concurrent use may increase adverse effects of phenytoin. Quinolone antibiotics may affect the efficacy of glibenclamide; monitor blood sugar levels. Hypoglycaemic effect may be reduced by somatropin.
Potentially Fatal: Increased risk of liver toxicity when used with bosentan; avoid concurrent use.
See Below for More glibenclamide Drug Interactions
Mechanism of Actions
Glibenclamide exerts pancreatic and extrapancreatic actions. It stimulates an increase in insulin release by the pancreatic β-cells. It may also reduce hepatic gluconeogenesis and glycogenolysis. Increased glucose uptake in the liver and utilization in the skeletal muscles.
Duration: 24 hr.
Absorption: Readily absorbed from the GI tract (oral); peak plasma concentrations after 2-4 hr.
Distribution: Protein-binding: Extensive.
Metabolism: Hepatic; converted to very weakly active metabolite.
Excretion: Urine (50%); faeces (50%).
Administration
Glibenclamide: Should be taken with food.
Storage Conditions
Oral: Store at 15-30°C.
ATC Classification
A10BB01 - glibenclamide ; Belongs to the class of sulfonamides, urea derivatives. Used in the treatment of diabetes.
Storage
Oral: Store at 15-30°C.
Available As
  • Glibenclamide 1.25 mg
  • Glibenclamide 10 mg
  • Glibenclamide 2.25 mg
  • Glibenclamide 2.5 mg
  • Glibenclamide 5 mg
  • Glibenclamide IP 5 mg
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