Drug information of Glibenclamide

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.

Pharmacodynamic

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.

Pharmacokinetics

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.

Dosage

• Adults
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 contraindications

Renal dysfunction , Active liver disease , Acute or chronic metabolic acidosis , patients with porphyria , Deep burns

Side effects

nausea , vomiting , allergic reaction , rash , fever , anorexia , jaundice , Hypoglycemia , Photosensitivity , increased appetite , metallic taste in mouth

Interactions

Urtidin , 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

Alerts

• 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.

Pregnancy level

C

Related drugs

Glimepiride