Glimepiride
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| Clinical data | |
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| Trade names | Amaryl |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a696016 |
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| Routes of administration |
Oral (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 100% |
| Protein binding | >99.5% |
| Metabolism | Complete hepatic (1st stage through CYP2C9) |
| Biological half-life | 5–8 hours |
| Excretion | Urine (~60%), feces (~40%) |
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| ChEMBL | |
| ECHA InfoCard | 100.170.771 |
| Chemical and physical data | |
| Formula | C24H34N4O5S |
| Molar mass | 490.617 g/mol |
| 3D model (Jmol) | |
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Glimepiride (original trade name Amaryl) is an orally available medium-to-long-acting sulfonylurea antidiabetic drug. It is sometimes classified as either the first third-generation sulfonylurea, or as second-generation.
Glimepiride is indicated to treat type 2 diabetes mellitus; its mode of action is to increase insulin production by the pancreas. It is not used for type 1 diabetes because in type 1 diabetes the pancreas is not able to produce insulin.
Its use is contraindicated in patients with hypersensitivity to glimepiride or other sulfonylureas.
Side effects from taking glimepiride include gastrointestinal tract (GI) disturbances, occasional allergic reactions, and rarely blood production disorders including thrombocytopenia, leukopenia, and hemolytic anemia. In the initial weeks of treatment, the risk of hypoglycemia may be increased. Alcohol consumption and exposure to sunlight should be restricted because they can worsen side effects.
Gastrointestinal absorption is complete, with no interference from meals. Significant absorption can occur within one hour, and distribution is throughout the body, 99.5% bound to plasma protein. Metabolism is by oxidative biotransformation, it is hepatic and complete. First, the medication is metabolized to M1 metabolite by CYP2C9. M1 possesses about 1⁄3 of pharmacological activity of glimepiride, yet it is unknown if this results in clinically meaningful effect on blood glucose. M1 is further metabolized to M2 metabolite by cytosolic enzymes. M2 is pharmacologically inactive. Excretion in the urine is about 65%, and the remainder is excreted in the feces.
Like all sulfonylureas, glimepiride acts as an insulin secretagogue. It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.
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Wikipedia