Glibenclamide

Glibenclamide, also known as glyburide, is an antidiabetic drug in a class of medications known as sulfonylureas, closely related to sulfonamide antibiotics.

Glibenclamide

Glyburide; Glibenclamide; Glybenclamide; Diabeta

Afdiex, Aviglen, Betanase, C-Mide, Codica, D-Con, Daonil, Diabetnil, Diolin, Euglucon, G-Nil, GLCO, Glibet, Glinil, Gluconil, Glucosafe, Glyboral, Glybovin, Semi Codica, Semi Daonil, Semi- Euglucon, Semi-Glyboral, Sugnl

5-chloro-N-[2-(4-{[(cyclohexylcarbamoyl)amino]sulfonyl}phenyl)ethyl]-2-methoxybenzamide

Oral absorption with hepatic metabolism.

Glyburide, a second-generation sulfonylurea antidiabetic agent, lowers blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. 

Initially, 2.5-5 mg daily may increase wkly by increments of 2.5 mg daily, up to 15 mg daily. 

Indicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone.

Hypoglycaemia; cholestatic jaundice; agranulocytosis; aplastic anaemia; haemolytic anaemia. Blood dyscrasias (reversible), liver dysfunction, hypoglycaemia, GI symptoms, and allergic skin reactions.

• Increased risk of liver toxicity when used with bosentan; avoid concurrent use.
• 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 pegvisomant, cyclic antidepressants, 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 administration of glibenclamide with chloestyramine resin may leads to reduce absorption.
• Concurrent use may increase adverse effects of phenytoin.
• Serum levels may be reduced by colesevelam.
• Quinolone antibiotics may affect the efficacy of glibenclamide
• Hypoglycaemic effect may be reduced by somatropin.
• Concurrent use with coumarin derivatives may cause changes in INR. 

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.

Store at 15-30°C.

Molecular weight

494.004

Molecular formula

C23H28ClN3O5S

CAS number

10238-21-8

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.