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| Clinical data | |
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| Trade names | Amaryl, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a696016 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | 100% |
| Protein binding | >99.5% |
| Metabolism | CompleteLiver (1st stage throughCYP2C9) |
| Onset of action | 2–3 hours |
| Eliminationhalf-life | 5–8 hours |
| Duration of action | 24 hours |
| Excretion | Urine (~60%), feces (~40%) |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.170.771 |
| Chemical and physical data | |
| Formula | C24H34N4O5S |
| Molar mass | 490.62 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 207 °C (405 °F) |
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Glimepiride is anantidiabetic medication within thesulfonylurea class, primarily prescribed for the management oftype 2 diabetes.[1][2] It is regarded as a second-line option compared tometformin, due to metformin's well-established safety and efficacy.[1] Use of glimepiride is recommended in conjunction withlifestyle modifications such as diet and exercise.[1] It is taken by mouth,[1] reaching a peak effect within three hours and lasting for about a day.[1]
Common side effects include headache, nausea, and dizziness.[1] Serious side effects may includelow blood sugar.[1] Use duringpregnancy andbreastfeeding is not recommended.[3] It works predominantly by increasing the amount ofinsulin released from thepancreas.[1] It is classified as a second-generationsulfonylurea.[4]
Glimepiride was patented in 1979 and approved for medical use in 1995.[5] It is available as ageneric medication.[2] In 2023, it was the 80th most commonly prescribed medication in the United States, with more than 8 million prescriptions.[6][7]
Glimepiride isindicated to treattype 2 diabetes; its mode of action is to increase insulin secretion by the pancreas. However it requires adequate insulin synthesis as prerequisite to treat appropriately. It is not used fortype 1 diabetes because in type 1 diabetes the pancreas is not able to produce insulin.[8]
Its use is contraindicated in patients with hypersensitivity to glimepiride or other sulfonylureas.
Side effects from taking glimepiride includegastrointestinal tract (GI) disturbances, occasional allergic reactions, and rarely blood production disorders includingthrombocytopenia,leukopenia, andhemolytic 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.[8]
Nonsteroidal anti-inflammatory drugs (such assalicylates),sulfonamides,chloramphenicol,warfarin andprobenecid may potentiate thehypoglycemic action of glimepiride.Thiazides, otherdiuretics, phothiazides, thyroid products, oral contraceptives, andphenytoin tend to producehyperglycemia.
Like allsulfonylureas, glimepiride acts as an insulinsecretagogue.[9] It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.
Not all secondary sulfonylureas have the same risk of hypoglycemia. Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to as low as 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not. Also, glibenclamide diminishes glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not.[10]
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 ishepatic and complete. First, the medication is metabolized to M1 metabolite byCYP2C9. M1 possesses about1⁄3 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.
