Sulfonylureas
Sulfonylureas (UK: sulphonylurea) are a class of organic compounds used in medicine and agriculture, for example as antidiabetic drugs widely used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta cells in the pancreas. A number of sulfonylureas are also used as herbicides, because they can interfere with plant biosynthesis of certain amino acids. Sulfonylureas are also used experimentally to inhibit interleukin 1 beta release from the NALP3 (or NLRP3) inflammasome. Drugs * First-generation drugs include acetohexamide, carbutamide, chlorpropamide, glycyclamide (tolcyclamide), metahexamide, tolazamide and tolbutamide. * Second-generation drugs include glibenclamide (glyburide), glibornuride, gliclazide, glipizide, gliquidone, glisoxepide and glyclopyramide. * Third-generation drugs include glimepiride, although it is sometimes considered a second-generation agent. Medical uses Sulfonylureas are used primarily for the treatm ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Antidiabetic Drugs
Drugs used in diabetes treat diabetes mellitus by altering the glucose level in the blood. With the exceptions of insulin, most GLP receptor agonists (liraglutide, exenatide, and others), and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of anti-diabetic drugs, and their selection depends on the nature of the diabetes, age and situation of the person, as well as other factors. Diabetes mellitus type 1 is a disease caused by the lack of insulin. Insulin must be used in type 1, which must be injected. Diabetes mellitus type 2 is a disease of insulin resistance by cells. Type 2 diabetes mellitus is the most common type of diabetes. Treatments include agents that (1) increase the amount of insulin secreted by the pancreas, (2) increase the sensitivity of target organs to insulin, (3) decrease the rate at which glucose is absorbed from the gastrointestinal tract, and (4) incre ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Tolbutamide
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 # 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. ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Chlorpropamide
Chlorpropamide is a drug in the sulfonylurea class used to treat diabetes mellitus type 2. It is a long-acting first-generation sulfonylurea. Mechanism of action Like other sulfonylureas, chlorpropamide acts to increase the secretion of insulin, so it is only effective in patients who have some pancreatic beta cell function. It can cause relatively long episodes of hypoglycemia; this is one reason why shorter-acting sulfonylureas such as gliclazide or tolbutamide are used instead. The risk of hypoglycemia makes this drug a poor choice for the elderly and patients with mild to moderate hepatic and renal impairment. Chlorpropamide is also used in partial central diabetes insipidus. Pharmacokinetics Maximal plasma concentrations are reached 3 to 5 hours after quick and nearly complete (>90%) resorption from the gut. Plasma half life is 36 hours; the drug is effective for about 24 hours, longer than other sulfonylureas. A stable plasma level is only reached after three days of conti ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Glimepiride
Glimepiride, is an anti-diabetic medication used to treat type 2 diabetes. It is less preferred than metformin. Use is recommended together with diet and exercise. It is taken by mouth. Glimepiride takes up to three hours for maximum effect and lasts for about a day. Common side effects include headache, nausea, and dizziness. Serious side effects may include low blood sugar. Use during pregnancy and breastfeeding is not recommended. It works mainly by increasing the amount of insulin released from the pancreas. It is classified as a second-generation sulfonylurea. Glimepiride was patented in 1979 and approved for medical use in 1995. It is available as a generic medication. In 2020, it was the 87th most commonly prescribed medication in the United States, with more than 8million prescriptions. Medical uses Glimepiride is indicated to treat Diabetes mellitus type 2, type 2 diabetes mellitus; its mode of action is to increase insulin secretion by the pancreas. However it req ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Gliclazide
Gliclazide, sold under the brand name Diamicron among others, is a sulfonylurea type of anti-diabetic medication, used to treat type 2 diabetes. It is used when dietary changes, exercise, and weight loss are not enough. It is taken by mouth. Side effect may include low blood sugar, vomiting, abdominal pain, rash, and liver problems. Use by those with significant kidney problems or liver problems or who are pregnant is not recommended. Gliclazide is in the sulfonylurea family of medications. It works mostly by increasing the release of insulin. Gliclazide was patented in 1966 and approved for medical use in 1972. It is on the World Health Organization's List of Essential Medicines. It is not available for sale in the United States. Medical uses Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, type 2 diabetes. It is used when diabetes cannot be controlled by proper dietary management and exerci ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Glisoxepide
Glisoxepide (INN) is an orally available anti-diabetic drug from the group of sulfonylurea Sulfonylureas (UK: sulphonylurea) are a class of organic compounds used in medicine and agriculture, for example as antidiabetic drugs widely used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta ...s. It belongs to second-generation sulfonylureas. References Potassium channel blockers Azepanes Carboxamides Isoxazoles Benzenesulfonylureas {{gastrointestinal-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Metahexamide
Metahexamide (INN) is an anti-diabetic drug from the group of sulfonylurea Sulfonylureas (UK: sulphonylurea) are a class of organic compounds used in medicine and agriculture, for example as antidiabetic drugs widely used in the management of diabetes mellitus type 2. They act by increasing insulin release from the beta ...s. It is long-acting and belongs to the first-generation cyclohexyl-containing sulfonylureas. It was first described in 1959. References Potassium channel blockers 1-(Benzenesulfonyl)-3-cyclohexylureas {{gastrointestinal-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Tolazamide
Tolazamide is an oral blood glucose lowering drug used for people with Type 2 diabetes. It is part of the sulfonylurea family (ATC A10BB). Synthesis ''para''-Toluenesulfonamide is converted to its carbamate with ethyl chloroformate in the presence of a base. Heating that intermediate with 1-amino-azepane Azepane is the organic compound with the formula (CH2)6NH. It is a colorless liquid. A cyclic secondary amine, it is a precursor to several drugs and pesticides. It is produced by partial hydrogenolysis of hexamethylene diamine. Like many amine ... leads to the displacement of the ethoxy group and the formation of tolazemide: Azepane proper would lead to 3078-23-4 References External links * Potassium channel blockers Benzenesulfonylureas Azepanes p-Tosyl compounds {{gastrointestinal-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Glyclopyramide
Glyclopyramide (INN, marketed under the tradename Deamelin-S) is a sulfonylurea drug used in the treatment of diabetes. It has been marketed in Japan Japan ( ja, 日本, or , and formally , ''Nihonkoku'') is an island country in East Asia. It is situated in the northwest Pacific Ocean, and is bordered on the west by the Sea of Japan, while extending from the Sea of Okhotsk in the north ... since 1965. It is classified as second generation. References External links DEAMELIN·S Tablets 250 mg Potassium channel blockers Benzenesulfonylureas Pyrrolidines Chloroarenes {{gastrointestinal-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Gliquidone
Gliquidone (INN, sold under the trade name Glurenorm) is an anti-diabetic medication in the sulfonylurea class. It is classified as a second-generation sulfonylurea. It is used in the treatment of diabetes mellitus type 2. It is marketed by the pharmaceutical company Boehringer Ingelheim (Germany). Contraindications * Allergy to sulfonylureas or sulfonamides * Diabetes mellitus type 1 * Diabetic ketoacidosis * Patients that underwent removal of the pancreas * Acute porphyria * Severe liver disease accompanying with liver insufficiency * Several conditions (e.g., infectious diseases or major surgical intervention), when insulin administration is required * Pregnancy or breastfeeding Pharmacokinetics Gliquidone is fully metabolized by the liver. Its metabolites are excreted virtually completely with bile (even with long-term administration), thus allowing the use of medication in diabetic patients with kidney disease and diabetic nephropathy Diabetic nephropathy, also known as ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Carbutamide
Carbutamide (brand name Glucidoral) is an anti-diabetic drug of the sulfonylurea class, developed by Servier. It is classified as first-generation. It was patented A patent is a type of intellectual property that gives its owner the legal right to exclude others from making, using, or selling an invention for a limited period of time in exchange for publishing an enabling disclosure of the invention."A p ... in 1953 and approved for medical use in 1956. See also * Hellmuth Kleinsorge (1920-2001) German medical doctor References Potassium channel blockers Benzenesulfonylureas Anilines {{gastrointestinal-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |