Glibenclamide
Encyclopedia
Glibenclamide also known as glyburide (USAN
), is an antidiabetic drug in a class of medications known as sulfonylurea
s, closely related to sulfa
drugs. It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche
) and Hoechst
(now part of Sanofi-Aventis
).
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 and Delmide in India.
It is also sold in combination with metformin
under the trade names Glucovance and Glibomet.
). As of 2003, in the United States, it was the most popular sulfonylurea.
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.
beta cell
s. This inhibition causes cell membrane depolarization
opening voltage-dependent calcium channel
. This results in an increase in intracellular calcium
in the beta cell
and subsequent stimulation of insulin
release.
. Cholestatic jaundice
is noted.
Recently published data suggest 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.
Gilbenclamide causes cholestasis
as the major side effect.
Glibenclamide has been demonstrated to block the protection offered by myocardial preconditioning in dogs.
United States Adopted Name
United States Adopted Names are unique nonproprietary names assigned to pharmaceuticals marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association , the United States Pharmacopeial Convention , and the American Pharmacists...
), is an antidiabetic drug in a class of medications known as sulfonylurea
Sulfonylurea
Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas.-First generation:* Carbutamide...
s, closely related to sulfa
SULFA
SULFA, short for Surrendered ULFA, i.e. members of the United Liberation Front of Asom that surrendered to the government.Beginning with 1990, the Government of India has attempted to wean away members of ULFA. In 1992 a large section of second rank leaders and members surrendered to government...
drugs. It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche
Roche
Roche is French for "boulder/rock". The word is several names:-Business & companies:* Hoffmann–La Roche AG, Basel, Switzerland, one of the largest pharmaceutical companies in the world....
) and Hoechst
Hoechst
Hoechst or Höchst may refer to:* Hoechst AG, a former German life-sciences company* Hoechst stain, one of a family of fluorescent DNA-binding compounds* Höchst , Germany* Höchst im Odenwald, Germany* Höchst, Austria...
(now part of Sanofi-Aventis
Sanofi-Aventis
Sanofi S.A. is a multinational pharmaceutical company headquartered in Paris, France, the world's fourth-largest by prescription sales. Sanofi engages in the research and development, manufacturing and marketing of pharmaceutical products for sale principally in the prescription market, but the...
).
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 and Delmide in India.
It is also sold in combination with metformin
Metformin
Metformin is an oral antidiabetic drug in the biguanide class. It is the first-line drug of choice for the treatment of type 2 diabetes, in particular, in overweight and obese people and those with normal kidney function. Its use in gestational diabetes has been limited by safety concerns...
under the trade names Glucovance and Glibomet.
Uses
It is used in the treatment of type II diabetes. , it is one of only two oral antidiabetics in the World Health Organization Model List of Essential Medicines (the other being metforminMetformin
Metformin is an oral antidiabetic drug in the biguanide class. It is the first-line drug of choice for the treatment of type 2 diabetes, in particular, in overweight and obese people and those with normal kidney function. Its use in gestational diabetes has been limited by safety concerns...
). As of 2003, in the United States, it was the most popular sulfonylurea.
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 in pancreaticPancreas
The pancreas is a gland organ in the digestive and endocrine system of vertebrates. It is both an endocrine gland producing several important hormones, including insulin, glucagon, and somatostatin, as well as a digestive organ, secreting pancreatic juice containing digestive enzymes that assist...
beta cell
Beta cell
Beta cells are a type of cell in the pancreas located in the so-called islets of Langerhans. They make up 65-80% of the cells in the islets.-Function:...
s. This inhibition causes cell membrane depolarization
Depolarization
In biology, depolarization is a change in a cell's membrane potential, making it more positive, or less negative. In neurons and some other cells, a large enough depolarization may result in an action potential...
opening voltage-dependent calcium channel
Voltage-dependent calcium channel
Voltage-dependent calcium channels are a group of voltage-gated ion channels found in excitable cells with a permeability to the ion Ca2+...
. This results in an increase in intracellular calcium
Calcium
Calcium is the chemical element with the symbol Ca and atomic number 20. It has an atomic mass of 40.078 amu. Calcium is a soft gray alkaline earth metal, and is the fifth-most-abundant element by mass in the Earth's crust...
in the beta cell
Beta cell
Beta cells are a type of cell in the pancreas located in the so-called islets of Langerhans. They make up 65-80% of the cells in the islets.-Function:...
and subsequent stimulation of insulin
Insulin
Insulin is a hormone central to regulating carbohydrate and fat metabolism in the body. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle....
release.
Side effects and contraindications
This drug is a major cause of drug induced hypoglycemiaHypoglycemia
Hypoglycemia or hypoglycæmia is the medical term for a state produced by a lower than normal level of blood glucose. The term literally means "under-sweet blood"...
. Cholestatic jaundice
Jaundice
Jaundice is a yellowish pigmentation of the skin, the conjunctival membranes over the sclerae , and other mucous membranes caused by hyperbilirubinemia . This hyperbilirubinemia subsequently causes increased levels of bilirubin in the extracellular fluid...
is noted.
Recently published data suggest 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.
Gilbenclamide causes cholestasis
Cholestasis
In medicine, cholestasis is a condition where bile cannot flow from the liver to the duodenum. The two basic distinctions are an obstructive type of cholestasis where there is a mechanical blockage in the duct system such as can occur from a gallstone or malignancy and metabolic types of...
as the major side effect.
Glibenclamide has been demonstrated to block the protection offered by myocardial preconditioning in dogs.