Glibenclamide
Chemical compound
From Wikipedia, the free encyclopedia
Glibenclamide, also known as glyburide (U.S. English), is an antidiabetic medication used to treat type 2 diabetes.[1] It is recommended that it be taken together with diet and exercise.[1] It may be used with other antidiabetic medication.[1] It is not recommended for use by itself in type 1 diabetes.[1] It is taken by mouth.[1]
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| Trade names | Diabeta, Glynase, Micronase, others[1] |
| Other names | Glyburide (USAN US) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a684058 |
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| Routes of administration | By mouth |
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| Protein binding | Extensive |
| Metabolism | Liver hydroxylation (CYP2C9-mediated) |
| Elimination half-life | 10 hours |
| Excretion | Kidney and bile duct |
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| ECHA InfoCard | 100.030.505 |
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| Formula | C23H28ClN3O5S |
| Molar mass | 494.00 g·mol−1 |
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| Melting point | 169 to 170 °C (336 to 338 °F) |
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Common side effects include nausea and heartburn.[1] Serious side effects may include angioedema and low blood sugar.[1] It is generally not recommended during pregnancy but can be used during breastfeeding.[3] It is in the sulfonylureas class of medications and works by increasing the release of insulin from the pancreas.[1]
Glibenclamide was discovered in 1969 and approved for medical use in the United States in 1984.[4][1] It is available as a generic medication.[3] In 2021, it was the 214th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[5][6]
Medical uses
Glibenclamide is used to lower the blood sugar level in patients with type 2 diabetes mellitus, which is not controlled by diet and exercise alone.
It is not as good as either metformin or insulin in those who have gestational diabetes.[7]
Side effects
Frequently reported side effects include: nausea, heartburn, weight gain, and bloating.[8] The medication is also a major cause of medication-induced hypoglycemia. The risk is greater than with other sulfonylureas.[9]
Contraindications
Glibenclamide may be not recommended in those with G6PD deficiency, as it may cause acute hemolysis.[10]
Pregnancy and breastfeeding
It is generally not recommended during pregnancy but can be used during breastfeeding.[3]
Mechanism of action
The medication, a sulfonylurea, works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) inhibitory regulatory subunit sulfonylurea receptor 1 (SUR1)[11] in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening voltage-dependent calcium Channels.[12]
This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.[13]
After a stroke, the blood–brain barrier is broken and glibenclamide can reach the central nervous system. Glibenclamide has been shown to bind more efficiently to the ischemic hemisphere.[14] Moreover, under ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in neurons, astrocytes, oligodendrocytes, endothelial cells[15] and by reactive microglia.[14]
According to the research, this and other sulphonylurea drugs also have extra hepatic effects. It works by inhibiting the enzyme Carnityl Acyl Transferase I (CAT-I) indirectly, which is present in the mitochondria. This prevents the transport of long chain fatty acids into the mitochondria for beta-oxidation. This prevents hyperglycemia for which it is prescribed.[16][17]
History
It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche) and Hoechst (now part of Sanofi-Aventis).[18]
Society and culture
Brand names
Glibenclamide is available as a generic medication, is manufactured by many pharmaceutical companies and is sold under many brand names including Gliben-J, Daonil,[19] Diabeta,[20] Euglucon, Gilemal, Glidanil, Glybovin, Glynase, Maninil, Micronase and Semi-Daonil. It is also available in a fixed-dose combination drug with metformin that is sold under various trade names, e.g. Bagomet Plus, Benimet, Glibomet, Gluconorm, Glucored, Glucovance, Metglib and many others.[21]
