Tolbutamide
Chemical compound / From Wikipedia, the free encyclopedia
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Not to be confused with topilutamide.
Tolbutamide is a first-generation potassium channel blocker, sulfonylurea oral hypoglycemic medication. This drug may be used in the management of type 2 diabetes if diet alone is not effective. Tolbutamide stimulates the secretion of insulin by the pancreas.
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Quick Facts Clinical data, Trade names ...
Clinical data | |
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Trade names | Orinase |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682481 |
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Routes of administration | Oral (tablet) |
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Protein binding | 96% |
Metabolism | Hepatic (CYP2C19-mediated) |
Elimination half-life | 4.5 to 6.5 hours |
Excretion | Renal |
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ECHA InfoCard | 100.000.541 |
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Formula | C12H18N2O3S |
Molar mass | 270.35 g·mol−1 |
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Melting point | 128.5 to 129.5 °C (263.3 to 265.1 °F) |
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It is not routinely used due to a higher incidence of adverse effects compared to newer, second-generation sulfonylureas, such as Glibenclamide. It generally has a short duration of action due to its rapid metabolism, so is safe for use in older people.
It was discovered in 1956.[1]