Glibenclamide detailed information

Glibenclamide detailed information

Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	US FDA: Glyburide
Pregnancy category	AU: C US: B (No risk in non-human studies)
Routes of administration	Oral
ATC code	A10BB01 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Protein binding	Extensive
Metabolism	Hepatic hydroxylation (CYP2C9-mediated)
Elimination half-life	10 hours
Excretion	Renal and biliary
Identifiers
IUPAC name 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl) phenyl]ethyl]-2-methoxy-benzamide
CAS Number	10238-21-8
PubChem CID	3488
DrugBank	APRD00233
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C23H28ClN3O5S
Molar mass	494.004 g/mol

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

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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. 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).

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.

Additionally, recent research shows that glyburide improves outcome in amimal 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 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.

Side effects and contraindications

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

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.

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