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Sulfonylurea derivatives are a class of antidiabetic drugs that are used in the management of diabetes mellitus type 2 ("adult-onset"). They act by increasing insulin release from the beta cells in the pancreas. An anti-diabetic drug is used to treat diabetes mellitus. ...
Diabetes mellitus is a medical disorder characterized by varying or persistent hyperglycemia (elevated blood sugar levels), especially after eating. ...
The structure of insulin Red: carbon; green: oxygen; blue: nitrogen; pink: sulfur. ...
Beta cells are a type of cell in the pancreas in areas called the islets of Langerhans. ...
The pancreas is a retroperitoneal organ that serves two functions: exocrine - it produces pancreatic juice containing digestive enzymes endocrine - it produces several important hormones // Anatomy The pancreas is a retroperitoneal organ located posterior to the stomach on the posterior abdominal wall. ...
Drugs in this class
First generation: Second generation: Chlorpropamide is a sulphonylurea drug used to treat type 2 diabetes mellitus. ...
Tolbutamide is an sulfonylurea oral hypoglycemic drug sold under the brand name Orinase. ...
Glipizide is an oral medium-to-long acting anti-diabetic drug from the sulfonylurea class. ...
Glibenclamide is a class of drug known as sulphonylureas. ...
Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. ...
Chemistry Please see individual members of the class for their chemical structure
All sulfonylureas have a central phenyl ring with two branching chains. In chemistry, the phenyl group or phenyl ring (often abbreviated as -Ph) is the functional group with the formula -C6H5 Picture where the six carbon atoms are arranged in a cyclic manner. ...
Pharmacology
Method of action Sulfonylureas bind to an ATP-dependent K+ channel on the cell membrane of pancreatic beta cells. This inhibits a tonic, hyperpolarizing outflux of potassium, which causes the electric potential over the membrane to become more positive. This depolarization opens voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of (pro)insulin. Adenosine triphosphate (ATP) Adenosine triphosphate (ATP) is the nucleotide known in biochemistry as the molecular currency of intracellular energy transfer; that is, ATP is able to store and transport chemical energy within cells. ...
General Name, Symbol, Number potassium, K, 19 Chemical series alkali metals Group, Period, Block 1, 4, s Appearance silvery white Atomic mass 39. ...
Beta cells are a type of cell in the pancreas in areas called the islets of Langerhans. ...
In biology, depolarization is the event a cell undergoes when its membrane potential grows more positive with respect to the extracellular solution. ...
General Name, Symbol, Number calcium, Ca, 20 Chemical series alkaline earth metals Group, Period, Block 2, 4, s Appearance silvery white Atomic mass 40. ...
The structure of insulin Red: carbon; green: oxygen; blue: nitrogen; pink: sulfur. ...
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 acids by adipose tissue) and decrease clearance of insulin by the liver. The liver is an organ in vertebrates, including humans. ...
In chemistry, especially biochemistry, a fatty acid is a carboxylic acid (or organic acid), often with a long aliphatic tail (long chains), either saturated or unsaturated. ...
Adipose tissue is an anatomical term for loose connective tissue composed of adipocytes. ...
Pharmacokinetics Various sulfonylureas have different pharmacokinetics. The choice depends on the propensity of the patient to develop hypoglycemia - long-acting sulfonylureas with active metabolites can induce hypoglycemia. They can, however, help achieve glycemic control when tolerated by the patient. The shorter-acting agents may not control blood sugar levels adequately. Hypoglycemia is a medical term referring to a pathologic state produced by a lower than normal amount of sugar (glucose) in the blood. ...
Due to varying half-life, some drugs have to be taken twice (tolbutamide) or three times a day rather than once (glimepiride). The short-acting agents may have to be taken about 30 minutes before the meal, to ascertain maximum efficacy when the food leads to increased blood glucose levels.
Some sulfonylureas are metabolised by liver metabolic enzymes (cytochrome P450) and inducers of this enzyme system (such as the antibiotic rifampicin) can therefore increase the clearance of sulfonylureas. In addition, because some sulfonylureas are bound to plasma proteins, use of drugs that also bind to plasma proteins can release the sulfonylureas from their binding places, leading to increased clearance. Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ...
Rifampicin (INN) or rifampin (USAN) is a bacteriocidal (kills bacteria) rather than bacteriostatic (keeps bacteria from replicating) antibiotic drug of the rifamycin group. ...
Uses Sulfonylureas are used almost exclusively in diabetes mellitus type 2. Other types of diabetes generally do not respond to sulfonylurea therapy, or (in diabetes of pregnancy) there are other contraindications. Diabetes mellitus is a medical disorder characterized by varying or persistent hyperglycemia (elevated blood sugar levels), especially after eating. ...
Gestational diabetes is a form of diabetes found in pregnant women. ...
Although for many years sulfonylureas were the first drugs to be used in new cases of diabetes, in the 1990s it was discovered that obese patients might benefit more from metformin. // Events and trends The 1990s are generally classified as having moved slightly away from the more conservative 1980s, but keeping the same mind-set. ...
Obesity is a significant public health concern throughout the developed and developing world. ...
Metformin (Glucophage®) is an anti-diabetic drug from the biguanide class (its other members are the withdrawn agents phenformin and buformin). ...
In about 10% of patients, sulfonylureas alone are ineffective in controlling blood glucose levels. Addition of metformin or a thiazolidinedione may be necessary, or (ultimately) insulin. Triple therapy of sulfonylureas, a biguanide (metformin) and a thiazolidinedione is generally discouraged, but some doctors prefer this combination over resorting to insulin. The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ...
Side-effects and cautions Sulfonylureas, as opposed to metformin and the thiazolidinediones, can induce hypoglycemia when insulin production overshoots. It is treated with sugary food, or (in the case of hypoglycemic coma) with intravenous dextrose. The best way to prevent this side-effect is to choose the lowest possible dose that adequately controls glucose levels. Metformin (Glucophage®) is an anti-diabetic drug from the biguanide class (its other members are the withdrawn agents phenformin and buformin). ...
The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ...
Hypoglycemia is a medical term referring to a pathologic state produced by a lower than normal amount of sugar (glucose) in the blood. ...
An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ...
A space-filling model of glucose Glucose, a simple monosaccharide sugar, is one of the most important carbohydrates and is used as a source of energy in animals and plants. ...
Like insulin, sulfonylureas can induce weight gain, mainly as a result of fluid retention and improvement of osmotic diuresis. Other side-effects are: abdominal upset, headache and hypersensitivy reactions. The structure of insulin Red: carbon; green: oxygen; blue: nitrogen; pink: sulfur. ...
A headache is a condition of mild to severe pain in the head; sometimes upper back or neck pain may also be interpreted as a headache. ...
Sulfonylureas are potentially teratogenic and cannot be used in pregnancy or in patients who intend to get pregnant. Impairment of liver or kidney function increase the risk of hypoglycemia, and are contraindications. As other anti-diabetic drugs cannot be used either under these circumstances, insulin therapy is the only option in pregnancy and hepatic and renal failure. Teratogenesis is a medical term from the Greek, literally meaning monster making. ...
History Sulfonylureas were discovered by the chemist Marcel Janbon and co-workers, who were studying sulfonamide antibiotics and discovered that the compound sulfonylurea induced hypoglycemia in animals (see also Patlak 2002). It was reported in: Janbon M, Chaptal J, Vedel A, Schaap J. Accidents hypoglycémiques graves par un sulfamidothiodiazol (le VK 57 ou 2254 RP). Montpellier Med. 1942;441:21-22. Sulfonamides, also known as sulfa drugs, are synthetic antimicrobial agents derived from sulfonic acid. ...
An antibiotic is a drug that kills or slows the growth of bacteria. ...
Hypoglycemia is a medical term referring to a pathologic state produced by a lower than normal amount of sugar (glucose) in the blood. ...
See also Diabetes mellitus is a medical disorder characterized by varying or persistent hyperglycemia (elevated blood sugar levels), especially after eating. ...
Metformin (Glucophage®) is an anti-diabetic drug from the biguanide class (its other members are the withdrawn agents phenformin and buformin). ...
The medication class of thiazolidinedione was introduced in the late 1990s as an adjunctive therapy for diabetes mellitus (type II) and related diseases. ...
References - Patlak M. New Weapons to Combat an Ancient Disease: Treating Diabetes. FASEB J 2002;16:1853E full text.
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