Glibenclamide
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Glibenclamide
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| 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 | |
| Pregnancy cat. | |
| Legal status | |
| 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
- ^ 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
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