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| Clinical data | |
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| Trade names | Glucotrol, Glucotrol XL, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a684060 |
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| Routes of administration | By mouth |
| Drug class | Sulfonylurea |
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| Pharmacokinetic data | |
| Bioavailability | 100% (regular formulation) 90% (extended release) |
| Protein binding | 98 to 99% |
| Metabolism | Liver hydroxylation |
| Elimination half-life | 2 to 5 hours |
| Excretion | Kidney and fecal |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.044.919 |
| Chemical and physical data | |
| Formula | C21H27N5O4S |
| Molar mass | 445.54 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 208 to 209 °C (406 to 408 °F) |
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Glipizide, sold under the brand name Glucotrol among others, is an anti-diabetic medication of the sulfonylurea class used to treat type 2 diabetes. [1] [2] It is used together with a diabetic diet and exercise. [1] [2] It is not indicated for use by itself in type 1 diabetes. [1] [2] It is taken by mouth. [1] [2] Effects generally begin within half an hour and can last for up to a day. [1]
Common side effects include nausea, diarrhea, low blood sugar, and headache. [1] Other side effects include sleepiness, skin rash, and shakiness. [3] The dose may need to be adjusted in those with liver or kidney disease. [1] Use during pregnancy or breastfeeding is not recommended. [3] It works by stimulating the pancreas to release insulin and increases tissue sensitivity to insulin. [1]
Glipizide was approved for medical use in the United States in 1984. [1] It is available as a generic medication. [1] In 2023, it was the 42nd most commonly prescribed medication in the United States, with more than 15 million prescriptions. [4] [5]
Glipizide sensitizes the beta cells of pancreatic islets of Langerhans insulin response, meaning that more insulin is released in response to glucose than would be without glipizide ingestion. [2] Glipizide acts by partially blocking potassium channels among beta cells of pancreatic islets of Langerhans. By blocking potassium channels, the cell depolarizes, which results in the opening of voltage-gated calcium channels. The resulting calcium influx encourages insulin release from beta cells. [6]
It was patented in 1969, and approved for medical use in 1971. [7] Glipizide was approved for medical use in the United States in 1984. [1]