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.
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.
Side effects
Side effects include:
- Hypoglycemia
- Weight gain
- Hypersensitivity: cross-allergicity with sulfonamides
- Drug interactions (especially first-generation drugs): Increased hypoglycemia with cimetidine, insulin, salicylates, and sulfonamides
Salicylates displace tolbutamide from its binding site on plasma binding proteins which lead to increase in free tolbutamide concentration, thus hypoglycemic shock.
History
Orinase was developed by Upjohn Co. at a time when the primary medical treatment for diabetes was insulin injections. Eli Lilly had a lock on the market for insulin production at the time. The practical applicability of Orinase, like that of other treatments for disease states detected by paraclinical signs (such as lab test results) rather than clinically observable signs or patient-reported symptoms, benefited from increased sensitivity and availability of testing (in this instance, urinary glucose testing and later also fingerstick blood glucose testing). Milton Moskowitz (editor in 1961 of Drug and Cosmetic Industry) claimed that the introduction of Orinase, "expanded the total market by bringing under medical care diabetics who were formerly not treated." It did this by changing the mindset about diabetes even more than insulin had. Treatment of this chronic disease was no longer seen as a mere slowing of "inexorable degeneration", but instead viewed through "a model of surveillance and early detection." While impressive, the lifestyle-modification arm of that same trial demonstrated a 58% reduction.
<!-- flowery, not encyclopedic, uncited Orinase was one of a number of drugs developed during the 1950s and 1960s 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. As such, it illustrates that science, medicine, markets, and health can interact in complicated and fascinating ways that are neither clearly desirable nor undesirable. -->
See also
- Chlorpropamide