Sulfonylurea: Difference between revisions
Created page with "{{Short description|Class of organic compounds used in medicine and agriculture}} thumb|right|General structural formula of a sulfonylurea. The functional group consists of a sulfonyl group and a N-substituted ureylene group '''Sulfonylureas''' or '''sulphonylureas''' are a class of organic compounds used in medicine and agriculture. The functional group consists of a sulfonyl group (-S(=O)<sub>2</sub>) with i..." |
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They are widely used as [[antidiabetic drug]]s in the management of [[diabetes mellitus type 2]]. They act by increasing [[secretion]] of [[insulin]] from the [[beta cell]]s in the [[pancreas]]. | They are widely used as [[antidiabetic drug]]s in the management of [[diabetes mellitus type 2]]. They act by increasing [[secretion]] of [[insulin]] from the [[beta cell]]s in the [[pancreas]]. | ||
Sulfonylureas are ineffective where there is absolute deficiency of insulin production such as in type 1 diabetes or post-pancreatectomy. | 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. | 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. | ||
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Sulfonylureas bind to and close [[ATP-sensitive potassium channel|ATP-sensitive K<sup>+</sup>]] (K<sub>ATP</sub>) channels on the cell membrane of pancreatic [[beta cell]]s, which depolarizes the cell by preventing potassium from exiting. This [[depolarization]] opens voltage-gated [[calcium|Ca]]<sup>2+</sup> channels. The rise in intracellular calcium leads to increased fusion of [[insulin]] granules with the cell membrane, and therefore increased [[Insulin#Synthesis|secretion]] of mature insulin. | Sulfonylureas bind to and close [[ATP-sensitive potassium channel|ATP-sensitive K<sup>+</sup>]] (K<sub>ATP</sub>) channels on the cell membrane of pancreatic [[beta cell]]s, which depolarizes the cell by preventing potassium from exiting. This [[depolarization]] opens voltage-gated [[calcium|Ca]]<sup>2+</sup> channels. The rise in intracellular calcium leads to increased fusion of [[insulin]] granules with the cell membrane, and therefore increased [[Insulin#Synthesis|secretion]] of mature insulin. | ||
There is some evidence that sulfonylureas also sensitize β-cells to glucose, that they limit glucose production in the [[liver]], that they decrease lipolysis (breakdown and release of [[fatty acid]]s by [[adipose tissue]]) and decrease clearance of insulin by the liver. | There is some evidence that sulfonylureas also sensitize β-cells to glucose, that they limit glucose production in the [[liver]], that they decrease lipolysis (breakdown and release of [[fatty acid]]s by [[adipose tissue]]) and decrease clearance of insulin by the liver. | ||
The K<sub>ATP</sub> channel is an octameric complex of the [[inward-rectifier potassium ion channel]] K<sub>ir</sub>6.x and [[sulfonylurea receptor]] SUR which associate with a [[stoichiometry]] of 4:4. | The K<sub>ATP</sub> channel is an octameric complex of the [[inward-rectifier potassium ion channel]] K<sub>ir</sub>6.x and [[sulfonylurea receptor]] SUR which associate with a [[stoichiometry]] of 4:4. | ||
