Glimepiride/ja: Difference between revisions
Created page with "グリメピリド" |
Created page with "<!-- Chemical data --> | IUPAC_name = 3-Ethyl-4-methyl-''N''-[2-(4-<nowiki/>{[(''trans''-4-methylcyclohexyl)carbamoyl]sulfamoyl}phenyl)ethyl]-2-oxo-2,5-dihydro-1''H''-pyrrole-1-carboxamide | C = 24 | H = 34 | N = 4 | O = 5 | S = 1 | smiles = O=C3C(/CC)=C(/C)CN3C(=O)NCCc1ccc(cc1)S(=O)(=O)NC(=O)N[C@H]2CC[C@H](C)CC2 | StdInChI_Ref = {{stdinchicite|correct|chemspide..." Tags: Mobile edit Mobile web edit |
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| IUPAC_name = 3-Ethyl-4-methyl-''N''-[2-(4-<nowiki/>{[(''trans''-4-methylcyclohexyl)carbamoyl]sulfamoyl}phenyl)ethyl]-2-oxo-2,5-dihydro-1''H''-pyrrole-1-carboxamide | | IUPAC_name = 3-Ethyl-4-methyl-''N''-[2-(4-<nowiki/>{[(''trans''-4-methylcyclohexyl)carbamoyl]sulfamoyl}phenyl)ethyl]-2-oxo-2,5-dihydro-1''H''-pyrrole-1-carboxamide | ||
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'''Glimepiride''' | '''グリメピリド'''（'''Glimepiride'''）は、[[sulfonylurea/ja|スルホニルウレア薬]]クラスの[[antidiabetic medication/ja|抗糖尿病薬]]であり、主に[[type 2 diabetes/ja|2型糖尿病]]の管理に処方される。メトホルミンの安全性と有効性が確立されているため、[[metformin/ja|メトホルミン]]と比較して第二選択薬とみなされている。グリメピリドは、食事療法や運動療法などの[[lifestyle modification/ja|生活習慣の改善]]と併用することが推奨されている。経口で服用し、3時間以内に効果がピークに達し、約1日間持続する。 | ||
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Revision as of 22:58, 13 March 2024
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| Clinical data | |
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| Trade names | アマリール, その他 |
| 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 | 完全な肝臓（第1段階からCYP2C9まで） |
| Onset of action | 2–3時間 |
| Elimination half-life | 5–8時間 |
| Duration of action | 24時間 |
| Excretion | 尿中 (~60%), 糞中 (~40%) |
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| ChEMBL | |
| 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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グリメピリド（Glimepiride）は、スルホニルウレア薬クラスの抗糖尿病薬であり、主に2型糖尿病の管理に処方される。メトホルミンの安全性と有効性が確立されているため、メトホルミンと比較して第二選択薬とみなされている。グリメピリドは、食事療法や運動療法などの生活習慣の改善と併用することが推奨されている。経口で服用し、3時間以内に効果がピークに達し、約1日間持続する。
Common side effects include headache, nausea, and dizziness. Serious side effects may include low blood sugar. Use during pregnancy and breastfeeding is not recommended. It is classified as a second-generation sulfonylurea.
Glimepiride was patented in 1979 and approved for medical use in 1995. It is available as a generic medication. In 2021, it was the 74th most commonly prescribed medication in the United States, with more than 8 million prescriptions.
Medical uses
Glimepiride is indicated to treat type 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 for type 1 diabetes because in type 1 diabetes the pancreas is not able to produce insulin.
Contraindications
Its use is contraindicated in patients with hypersensitivity to glimepiride or other sulfonylureas.
Adverse effects
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.
Interactions
Nonsteroidal anti-inflammatory drugs (such as salicylates), sulfonamides, chloramphenicol, coumadin and probenecid may potentiate the hypoglycemic action of glimepiride. Thiazides, other diuretics, phothiazides, thyroid products, oral contraceptives, and phenytoin tend to produce hyperglycemia.
Mechanism of action
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.
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.
Pharmacokinetics
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.
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