Sulfonylureas or sulphonylureas are a class of organic compounds used in medicine and agriculture. The functional group consists of a sulfonyl group (-S(=O)2) with its sulphur atom bonded to nitrogen atom of a ureylene group (N,N-dehydrourea, a urea derivative). The side chains R1 and R2 distinguish various sulfonylureas.
Sulfonylureas are divided into 3 classes on basis of therapeutic efficiency of their antidiabetic action:
First-generation drugs:
They include acetohexamide, carbutamide, chlorpropamide, glycyclamide (tolcyclamide), metahexamide, tolazamide and tolbutamide.
Second-generation drugs:
They include glibenclamide (glyburide), glibornuride, gliclazide, glipizide, gliquidone, glisoxepide and glyclopyramide.
Third-generation drugs:
They include glimepiride, although it is sometimes considered a second-generation drug.
They are widely used as antidiabetic drugs in the management of diabetes mellitus type 2. They act by increasing secretion of insulin from the beta cells in the pancreas.
Sulfonylureas are ineffective where there is absolute deficiency of insulin production such as in type 1 diabetes or post-pancreatectomy.
Sulfonylureas can be used to treat some types of neonatal diabetes. Historically, people with hyperglycemia and low blood insulin levels were diagnosed with type 1 diabetes by default, but it has been found that patients who receive this diagnosis before 6 months of age are often candidates for receiving sulfonylureas rather than insulin throughout life.
A 2011 Cochrane systematic review evaluated the effects on treatment of Latent Autoimmune Diabetes in Adults (LADA) and found that Sulfonylureas did improve metabolic control of glucose at 3 and 12 months, even worsening HbA1c levels in some cases, when compared to insulin. The same review did not find improvement of fasting C-peptide following treatment with sulfonylurea. Still, it is important to highlight that the studies available to be included in this review presented considerable flaws in quality and design.
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Diabetes mellitus, often known simply as diabetes, is a group of common endocrine diseases characterized by sustained high blood sugar levels. Diabetes is due to either the pancreas not producing enough insulin, or the cells of the body becoming unresponsive to the hormone's effects. Classic symptoms include thirst, polyuria, weight loss, and blurred vision. If left untreated, the disease can lead to various health complications, including disorders of the cardiovascular system, eye, kidney, and nerves.
Sulfonamide is a functional group (a part of a molecule) that is the basis of several groups of drugs, which are called sulphonamides, sulfa drugs or sulpha drugs. The original antibacterial sulfonamides are synthetic (nonantibiotic) antimicrobial agents that contain the sulfonamide group. Some sulfonamides are also devoid of antibacterial activity, e.g., the anticonvulsant sultiame. The sulfonylureas and thiazide diuretics are newer drug groups based upon the antibacterial sulfonamides. Allergies to sulfonamides are common.
Beta cells (β-cells) are a type of cell found in pancreatic islets that synthesize and secrete insulin and amylin. Beta cells make up 50–70% of the cells in human islets. In patients with Type 1 diabetes, beta-cell mass and function are diminished, leading to insufficient insulin secretion and hyperglycemia. The primary function of a beta cell is to produce and release insulin and amylin. Both are hormones which reduce blood glucose levels by different mechanisms.
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