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Information @ a Glance


  • Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug sold under the brand name Orinase.

  • Orinase was developed by Upjohn Co. at a time when the primary medical treatment for diabetes was insulin injections.

  • 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.

  • Tolbutamide, tolazamide, or chlorpropamide may be used in combination with insulin when sulfonylurea monotherapy fails to reduce symptoms and/or blood glucose levels.

  • Orinase diagnostic Sterile Powder contains tolbutamide sodium which is a white to off-white, practically odorless, crystalline powder, having a slightly bitter taste. It is freely soluble in water, soluble in alcohol and in chloroform, very slightly soluble in ether.

  • The chemical name for tolbutamide sodium is 1-Butyl-3-(p-tolylsulfonyl) urea monosodium salt C12H17N2NaO3S.

Mechanisms and Applications

  • Sulfonylureas lower blood glucose in patients with type 2 diabetes by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell.

  • Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.

  • Tolbutamide is an antidiabetic medication which is used in those patients with adult maturity onset or non-insulin dependent diabetes (NIDDM). It works by lowering blood sugar levels by stimulating the production and release of insulin from the pancreas. It also promotes the movement of sugar from the blood into the cells in the body which need it.


  • The heritage of Orinase (tolbutamide) has had a lasting effect on medicine and the pharmaceutical industry. Patients today are still diagnosed with prediabetes, many of them managing to stave off the onset of diabetes through dietary and lifestyle changes.

  • Orinase was one of a number of drugs developed during the 1950's and 1960's for a variety of conditions first to treat symptomatic diseases and later to treat asymptomatic conditions that put the patient at risk of developing symptomatic disease.

  • Its use and marketing played a definitive, though not solely sufficient, role in establishing the condition of prediabetes as a legitimate diagnosable condition.

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