Glibenclamide
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| Systematic (IUPAC) name | |
|---|---|
| 5-chloro-N-(4-[N-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-methoxybenzamide | |
| Identifiers | |
| CAS number | 10238-21-8 |
| ATC code | A10BB01 |
| PubChem | 3488 |
| DrugBank | APRD00233 |
| ChemSpider | 3368 |
| Chemical data | |
| Formula | C23H28ClN3O5S |
| Mol. mass | 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 |
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Glibenclamide (INN), also known as glyburide (USAN), is an anti-diabetic drug in a class of medications known as sulfonylureas.
It is sold in doses of 1.25 mg, 2.5 mg and 5 mg, 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.
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[edit] Uses
It is used in the treatment of type II diabetes. As of 2007[update], it is one of only two oral anti-diabetics in the World Health Organization Model List of Essential Medicines (the other being metformin).[1] As of 2003, in the United States, it was the most popular sulfonyurea.[2]
Additionally, recent research shows that glyburide improves outcome in animal stroke models by preventing brain swelling. A retrospective study showed that in type 2 diabetic patients already taking glyburide there was improved NIH stroke scale scores on discharge compared to diabetic patients not taking glyburide.
[edit] Mechanism of action
The drug works by inhibiting ATP-sensitive potassium channels[3] in pancreatic beta cells. This inhibition causes cell membrane depolarization, which causes voltage-dependent calcium channels to open, which causes an increase in intracellular calcium in the beta cell, which stimulates insulin release.
[edit] Side effects and contraindications
This drug is a major cause of drug induced hypoglycemia. Cholestatic jaundice is noted.
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.[4]
[edit] References
- ^ (March 2007) WHO Model List of Essential MedicinesPDF (612 KiB), 15th edition, World Health Organization, p. 21. Retrieved on 2007-11-19.
- ^ Riddle MC (February 2003). "Editorial: sulfonylureas differ in effects on ischemic preconditioning--is it time to retire glyburide?". J. Clin. Endocrinol. Metab. 88 (2): 528–30. doi:. PMID 12574174. http://jcem.endojournals.org/cgi/pmidlookup?view=long&pmid=12574174.
- ^ Serrano-Martín X, Payares G, Mendoza-León A (December 2006). "Glibenclamide, a blocker of K+(ATP) channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasis". Antimicrob. Agents Chemother. 50 (12): 4214–6. doi:. PMID 17015627. PMC 1693980. http://aac.asm.org/cgi/pmidlookup?view=long&pmid=17015627.
- ^ 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 22 (6): 477–82. doi:. PMID 16634115.
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