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Glibenclamide
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 C 23H28ClN3O5S 
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

US FDA:link

Pregnancy cat. C(AU) B(US)
Legal status POM (UK) -only (US)
Routes Oral
 Yes check.svgY(what is this?)  (verify)

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.

Contents

Uses

It is used in the treatment of type II diabetes. As of 2007, 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.

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.

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]

References

  1. ^ (March 2007) WHO Model List of Essential MedicinesPDF (612 KiB), 15th edition, World Health Organization, p. 21. Retrieved on 2007-11-19.
  2. ^ 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:10.1210/jc.2002-021971. PMID 12574174. http://jcem.endojournals.org/cgi/pmidlookup?view=long&pmid=12574174.  
  3. ^ 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:10.1128/AAC.00617-06. PMID 17015627. PMC 1693980. http://aac.asm.org/cgi/pmidlookup?view=long&pmid=17015627.  
  4. ^ 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:10.1002/dmrr.642. PMID 16634115.  
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