Pharmacological activity of glipizide

Summary

The author traces the history of the sulphonylurea hypoglycaemic agents leading up to the development of glipizide. A review is made of the pharmacodynamic and pharinacokinetic studies carried out in animals to assess the mode of action and activity of glipizide compared with earlier low-dose agents such as tolbutamide and glibenclamide. Results of these experiments show that glipizide acts faster and more efficiently than glibenclanzide on insulin and glucose levels, which quickly return to normal. It is suggested that glipizide exerts its hypoglycaemic effect through stimulation of insulin secretion by the pancreatic beta cells and that it is more specific in action than tolbutamide. Following oral administration, glipizide is rapidly and completely absorbed and is largely bound to plasma proteins. It undergoes prompt and almost complete metabolic transformation and does not accumulate to any extent in the tissues because it is rapidly eliminated by urinary excretion of the nzetabolites. Acute and chronic toxicity studies indicate that glipizide is well tolerated and has an exceptionally favourable therapeutic ratio.

Key Words::

• Glipizide
• sulphonylurea compounds
• antidiabetics
• pharmacology