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Glipizide, sold under the brand name Glucotrol among others, is an anti-diabetic medication of the sulfonylurea class used to treat type 2 diabetes. [1] [2] It is used together with a diabetic diet and exercise. [1] [2] It is not indicated for use by itself in type 1 diabetes. [1] [2] It is taken by mouth.
Drug class [55] Mechanism of action [7] Advantages [55] Disadvantages [55] Sulfonylureas (glyburide, glimepiride, glipizide) Stimulating insulin release by pancreatic beta cells by inhibiting the K ATP channel: Inexpensive; Fast onset of action; No effect on blood pressure; No detrimental effect on low-density lipoprotein
Thiazolidinedione ligand dependent transactivation is responsible for the majority of anti-diabetic effects. The activated PPAR/RXR heterodimer binds to peroxisome proliferator hormone response elements upstream of target genes in complex with a number of coactivators such as nuclear receptor coactivator 1 and CREB binding protein, this causes upregulation of genes (for a full list see PPARγ):
Drugs that worsen glucose tolerance, contravening the effects of antidiabetics, include corticosteroids, isoniazid, oral contraceptives and other estrogens, sympathomimetics, and thyroid hormones. Sulfonylureas tend to interact with a wide variety of other drugs, but these interactions, as well as their clinical significance, vary from ...
The mechanism of action on a cellular level is not well understood. Work is underway to define this mechanism as a prodiuretic with great promise. However, it has been shown that binding of different sugars to the glucose site affects the orientation of the aglycone in the access vestibule. So when the aglycone binds it affects the entire ...
According to the Biopharmaceutical Classification System (BCS), gliclazide falls under the BCS Class II drug, which is poorly soluble and highly permeable. Water solubility = 0.027mg/L [citation needed] Hypoglycemic sulfonylurea, restoring first peak of insulin secretion, increasing insulin Sensitivity. [22] No active circulating Metabolites. [13]
A drug class is a group of medications and other compounds that share similar chemical structures, act through the same mechanism of action (i.e., binding to the same biological target), have similar modes of action, and/or are used to treat similar diseases. [1] [2] The FDA has long worked to classify and license new medications.
It is in the sulfonylureas class of medications and works by increasing the release of insulin from the pancreas. [1] Glibenclamide was discovered in 1969 and approved for medical use in the United States in 1984. [4] [1] It is available as a generic medication. [3]