Article: Glibenclamide

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Glibenclamide
Systematic (IUPAC) name
5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl) phenyl]ethyl]-2-methoxy-benzamide
Identifiers
CAS number 10238-21-8
ATC code A10BB01
PubChem 3488
DrugBank APRD00233
Chemical data
Formula C23H28N3ClO5S 
Mol. weight 494.004 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding Extensive
Metabolism Hepatic hydroxylation (CYP2C9-mediated)
Half life 10 hours
Excretion Renal and biliary
Therapeutic considerations
Pregnancy cat.

C (Au), B (U.S.)

Legal status

POM (UK), â„ž-only (U.S.)

Routes Oral

Glibenclamide (INN), also known as glyburide (USAN), is an anti-diabetic drug in a class of medications known as sulfonylureas, used in the treatment of type II diabetes. The drug works by inhibiting ATP-sensitive potassium channels in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening of voltage-dependent calcium channels, thus triggering an increase in intracellular calcium into the beta cell which stimulates insulin release. It is sold in doses of 1.25mg, 2.5mg and 5mg, under the trade names Diabeta®, Glynase® and Micronase® in the United States and Daonil®, Semi-Daonil® and Euglucon® in the United Kingdom.

It is also sold in combination with metformin under the trade name Glucovance®.

The drug is contraindicated in pregnant women. It is also a major cause of drug induced hypoglycaemia.

Oral antidiabetic drugs (A10B) edit
A10BA - Biguanide - {02-metformin}
A10BB - Sulfonylureas - {01-glibenclamide (glyburide)} {02-chlorpropamide} {03-tolbutamide} {05-tolazamide} {07-glipizide} {08-gliquidone} {09-gliclazide} {12-glimepiride}
A10BF - Alpha-glucosidase inhibitor - {01-acarbose}
A10BG - Thiazolidinediones (TZD) - {01-troglitazone} {02-rosiglitazone} {03-pioglitazone}
A10BX - Meglitinide - {02-repaglinide} {03-nateglinide}
no ATC - Dipeptidyl peptidase-4 (DPP-4) inhibitors - {sitagliptin} {vildagliptin}
Retrieved from "http://en.wikipedia.org/wiki/Glibenclamide"

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