Glibenclamide

From Wikipedia, the free encyclopedia

You have new messages (last change).
Glibenclamide chemical structure
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
Licence data

US
Pregnancy cat.

C(AU) B(US)
Legal status

POM(UK) ℞-only(US)
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.

Recently published data suggests that glibenclamide is associated with significantly higher annual mortality when combined with metformin than other insulin secreting medications, after correcting for other potentially confounding patient characteristics. The safety of this combination has been questioned.[1]

[edit] References

  1. ^ Monami M, Luzzi C, Lamanna C, Chiasserini V, Addante F, Desideri CM, Masotti G, Marchionni N, Mannucci E (2006). "Three-year mortality in diabetic patients treated with different combinations of insulin secretagogues and metformin.". Diabetes Metab Res Rev. DOI:10.1002/dmrr.642. PMID 16634115.

[edit] External links


Oral antidiabetic drugs (A10B) edit
Biguanides: Metformin
Sulfonylureas: Chlorpropamide, glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitor: Acarbose, Miglitol
Thiazolidinediones (TZD): Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides: Nateglinide, Repaglinide, Mitiglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors: Saxagliptin, Sitagliptin, Vildagliptin


Pills  This pharmacology-related article is a stub. You can help Wikipedia by expanding it.
Retrieved from "http://en.wikipedia.org../../../g/l/i/Glibenclamide.html"