Drug information of Glibenclamide
Glibenclamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin.
Mechanism of effect
Sulfonylureas such as Glibenclamide bind to ATP-sensitive potassium channels on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.
Glibenclamide 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.
Significant absorption within 1 hour and peak plasma levels are reached in 2 to 4 hours. Onset of action occurs within one hour. Unchanged drug is ~99% bound to serum proteins. Metabolism: Primarily hepatic (mainly cytochrome P450 3A4). Glibenclamide is excreted as metabolites in the bile and urine, approximately 50% by each route Half life :1.4-1.8 hours (unchanged drug only); 10 hours (metabolites included). Duration of effect is 12-24 hours.
The starting dose is 5 mg a day, taken during or straight after breakfast (or the first main meal of the day). This may then be adjusted by your doctor, to a maximum of 15 mg a day.
• Elderly and very frail patients
The normal adult starting dose should be reduced to 2.5 mg a day.
Drug contraindicationsRenal dysfunction , Active liver disease , Acute or chronic metabolic acidosis , patients with porphyria , Deep burns
Side effectsnausea , vomiting , allergic reaction , rash , fever , anorexia , jaundice , Hypoglycemia , Photosensitivity , increased appetite , metallic taste in mouth
InteractionsUrtidin , Oxymetholone , Aripiprazole , Amitriptyline , Erythromycin , Acetaminophen+caffein+acetylsalic , Olanzapine , Ursodeoxycholic acid , Ethinyl Estradiol , Prednisolone , Endometrine , Clozapine , insulin regular , Insulin glargine , Insulin isophane , Insulin aspart , Quetiapine , Metolazone , Nilotinib , Hydrochlorothiazide , Hydrocortisone , Voriconazole , Clarithromycin , Cimetidine , Cyclosporine , Fluconazole , Phenytoin , Furosemide , Gliclazide , Triamcinolone , Triptorelin , Desogestrol , Ranitidine , Repaglinide , Sunitinib , Everolimus , Octreotide acetate , Oxandrolone , Paroxetine , Hydroxyprogesterone Caproate , Tranylcypromine
• Glibenclamide tablets like any other medicine belonging to its class, is not recommended for use in children.
Points of recommendation
• Avoid alcohol.
• Take 30-60 minutes before breakfast.