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Tolbutamide


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 potassium channel blocker, 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.

Additional recommended knowledge

v • d • e Oral antidiabetic drugs and Insulin analogs (A10)
Biguanides	Metformin
Sulfonylureas	Chlorpropamide, Glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide
Alpha-glucosidase inhibitors	Acarbose, Miglitol, Voglibose
Thiazolidinediones (TZD)	Pioglitazone, Rosiglitazone, Troglitazone
Meglitinides	Nateglinide, Repaglinide, Mitiglinide
Dipeptidyl peptidase-4 (DPP-4) inhibitors	Saxagliptin, Sitagliptin, Vildagliptin
Glucagon-like peptide-1 analog	Exenatide
Insulin analogs	fast acting (Insulin lispro, Insulin aspart, Insulin glulisine), intermediate-acting (NPH insulin), long acting (Insulin glargine, Insulin detemir)