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.

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
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	US FDA:link
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,

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.

Glipizide

Glipizide
Systematic (IUPAC) name
N-(4-[N-(cyclohexylcarbamoyl)sulfamoyl]phenethyl)-5-methylpyrazine-2-carboxamide
Identifiers
CAS number	29094-61-9
ATC code	A10BB07
PubChem	3478
DrugBank	APRD00436
Chemical data
Formula	C21H27N5O4S
Mol. mass	445.536 g/mol
Pharmacokinetic data
Bioavailability	100% (regular formulation) 90% (extended release)
Protein binding	98 to 99%
Metabolism	Hepatic hydroxylation
Half life	2 to 5 hours
Excretion	Renal and fecal
Therapeutic considerations
Pregnancy cat.	C (Au, U.S.)
Legal status	POM (UK), ℞-only (U.S.)
Routes	Oral

Glipizide is an oral medium-to-long acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. The structure on the R2 group is a much larger cyclo or aromatic group compared to the 1st generation sulfonylureas. This leads to a once a day dosing that is much less than the first generation, about 100 fold.

Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of langerhans. By partially blocking the potassium channels, it will increase the time the cell spends in the calcium release stage of cell signaling leading to an increase in calcium. The increase in calcium will initiate more insulin release from each beta cell.

Originally available in 1984, it is marketed by Pfizer under the brand name Glucotrol in the USA, where Pfizer sells Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL (an extended release form of glipizide) in doses of 2.5, 5, and 10 milligrams. Other companies sell generic forms of glipizide, most commonly extended release tablets of 5 and 10 milligrams.

Tolazamide

Tolazamide is an oral blood glucose lowering drug used for people with Type 2 diabetes. It is part of the sulfonamide family (ATC A10BB).

Mechanism of Action

Mechanism of Action

Acetohexamide lowers blood sugar by stimulating the pancreas to secrete insulin and helping the body use insulin efficiently. The pancreas must produce insulin for this medication to work. For this reason, acetohexamide is not used to treat diabetes mellitus type 1.

Acetohexamide

Acetohexamide (Dymelor) is a first-generation sulfonylurea medication used to treat diabetes mellitus type 2, particularly in people whose diabetes cannot be controlled by diet alone.

Tolbutamide

Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug sold under the brand name Orinase. This drug may be used in the management of type II diabetes if diet alone is not effective. Tolbutamide stimulates the secretion of insulin by the pancreas. Since the pancreas must synthesize insulin in order for this drug to work, it is not effective in the management of type I diabetes. It is not routinely used due to a higher incidence of adverse effects compared to newer second generation sulfonylureas, such as glyburide.