Tolbutamide

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Tolbutamide
Systematic (IUPAC) name
3-butyl-1-(4-methylphenyl)sulfonyl-urea
Identifiers
CAS number 64-77-7
ATC code A10BB03 V04CA01
PubChem 5505
DrugBank APRD00267
Chemical data
Formula C12H18N2O3S 
Mol. mass 270.349 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 96%
Metabolism Hepatic (CYP2C19-mediated)
Half life 4.5 to 6.5 hours
Excretion Renal
Therapeutic considerations
Licence data

US
Pregnancy cat.

C(AU) C(US)
Legal status

POM(UK) ℞-only(US)
Routes Oral (tablet)

Tolbutamide is a first generation sulfonylurea oral hypoglycemic drug sold under the brand name Orinase. This drug may be used in the management of type II diabetes if diet alone is not effective. Tolbutamide stimulates the secretion of insulin by the pancreas. Since the pancreas must synthesize insulin in order for this drug to work, it is not effective in the management of type I diabetes. It is not routinely used due to a higher incidence of adverse effects compared to newer second generation sulfonylureas, such as glyburide.

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v • d • e
Oral antidiabetic drugs (A10B)
Biguanides Metformin
Sulfonylureas Chlorpropamide, glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitors Acarbose, Miglitol
Thiazolidinediones (TZD) Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides Nateglinide, Repaglinide, Mitiglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors Saxagliptin, Sitagliptin, Vildagliptin
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