The Endocrine System and Its Disorders
Walter F. Stanaszek, Mary J. Stanaszek, Robert J. Holt, Steven Strauss in Understanding Medical Terms, 2020
Major components of treatment for diabetes mellitus are diet, exercise, insulin, and oral hypoglycemic agents. Diet and exercise are indicated for all patients with diabetes mellitus, regardless of type. Insulin is indicated for Type I diabetes and in Type II during times of stress or illness or when symptoms cannot be controlled by diet or oral agents. Use of oral sulfonylureas and other hypoglycemic agents is reserved for patients with Type II diabetes whose symptoms cannot be controlled with diet and exercise.
Biochemical and Pharmacological Rationales in Radiotracer Design
Lelio G. Colombetti in Principles of Radiopharmacology, 2019
The sulfonylurea hypoglycemic agents exert their effect primarily by stimulating the release of insulin from the beta cells of the pancreas.77 Therefore, a radioiodinated analog of the hypoglycemic agent chlorpropamide (Figure 7) was synthesized as a potential agent for imaging the pancreas.78 While initial studies in the dog did not show selective uptake in the pancreas as compared to other tissues, autoradiographic studies of the dog pancreas showed that the radioactivity was associated with the islet cells.79 These cells comprise only 1 to 4°7o of total pancreas weight,80 so that even high concentrations in these cells might not lead to selective concentration of the radiodiagnostic in the whole organ. Subsequently this agent was tested in hamsters with functional islet cell tumors, but no selective tumor uptake was demonstrated.81
Management of Obesity-Associated Type 2 Diabetes
Emmanuel C. Opara, Sam Dagogo-Jack in Nutrition and Diabetes, 2019
Sulfonylureas function by binding to and closing an ATP-dependent potassium (K-ATP) channel. In the pancreatic beta-cell, this action results in sustained membrane depolarization, activation of voltage-dependent calcium channels, calcium influx, and migration of insulin-containing vesicles to the cell surface, leading to insulin release. Sulfonylureas also increase insulin sensitivity. In the United States, the most commonly used sulfonylureas are glyburide, glipizide, and glimepiride. Unlike the biguanides, sulfonylureas can be associated with hypoglycemic episodes, particularly if food intake is poor or variable. Thus, the lowest effective dose should be used, and these agents should be used with caution in patients with erratic food intake, such as some elderly individuals. Furthermore, the kinetics of sulfonylureas may be changed with renal or hepatic dysfunction. Thus, these agents should be avoided in patients with significant impairment of these organs [147].
Potential molecular mechanism of action of sodium-glucose co-transporter 2 inhibitors in the prevention and management of diabetic retinopathy
Published in Expert Review of Ophthalmology, 2022
Lia Meuthia Zaini, Arief S Kartasasmita, Tjahjono D Gondhowiardjo, Maimun Syukri, Ronny Lesmana
There are several types of glucose-lowering agents with different mechanisms of action. Among all glucose-lowering agents, the most commonly used antidiabetic oral is metformin, which increases insulin sensitivity and suppresses hepatic gluconeogenesis. With its low price, metformin remains the first choice for type-2 diabetes mellitus (T2DM) treatment unless contraindicated or not tolerated based on its efficacy, safety, and tolerability. In addition, metformin also demonstrates other beneficial characteristics, such as low incidence of hypoglycemia and associated weight loss [4–6]. Sulfonylureas reduce blood glucose levels by stimulating endogenous insulin secretion from pancreatic β-cell. Long-term use of sulfonylureas is beneficial for increasing β-cell sensitivity and decreasing gluconeogenesis. However, they are also associated with increased body weight due to hyperinsulinemia [6].
The effect of co-administration of berberine, resveratrol, and glibenclamide on xenobiotic metabolizing enzyme activities in diabetic rat liver
Published in Drug and Chemical Toxicology, 2022
Azra Bozcaarmutlu, Canan Sapmaz, Ömer Bozdoğan, Aysel Kükner, Leyla Kılınç, Salih Tunç Kaya, Oğulcan Talat Özarslan, Didem Ekşioğlu
Diabetes is one of the most common metabolic diseases in the world. It often causes the continuous use of drugs. High blood glucose level characterized in diabetes causes organ damages and early aging. The studies have been shown that diabetes alone can disrupt the oxidant/antioxidant balance and lead to an increase in free radicals (Elbe et al. 2015, Al-Bishri 2017). In addition, diabetes is also effective on cytochrome P450 (CYP) system. It leads to an increase in the amount of CYP2E and CYP1A (Raza et al. 2000, 2004, Arınç et al. 2005). It is treated by many drugs. Glibenclamide is one of them. Glibenclamide is one of the sulfonylurea class of drugs. Sulfonylureas stimulate beta cells of the pancreas to release insulin. Glibenclamide is converted into cis- and trans-hydroxylglybenclamide metabolites in the liver (Kirchheiner et al. 2005). Both of these metabolites have anti-hyperglycemic activities and decrease blood glucose level. Fifty percent of the glibenclamide taken is removed from the urine as glibenclamide metabolites while the remaining glibenclamide is excreted from the intestines (Kirchheiner et al. 2005).
The role of sulfonylureas in the treatment of type 2 diabetes
Published in Expert Opinion on Pharmacotherapy, 2022
Brian Tomlinson, Nivritti Gajanan Patil, Manson Fok, Paul Chan, Christopher Wai Kei Lam
Sulfonylureas reduce plasma glucose by increasing insulin release from the pancreas, largely in a non-glucose dependent manner. They bind to receptor sites on a transmembrane protein called the sulfonylurea receptor (SUR) which modulates ATP-sensitive potassium (KATP) channels that are inhibited by ATP and activated by Mg-ADP and which normally transduce the cellular metabolic status into electrical signals [19]. Sulfonylurea binding inhibits potassium ion efflux through the channel resulting in membrane depolarization, which in turn opens a voltage-gated calcium channel and the influx of calcium causes release of preformed insulin from the beta-cell. KATP channels are also present in other cells including cardiac myocytes, vascular smooth muscle, skeletal muscle and neurons [20].
Related Knowledge Centers
- Acetohexamide
- Chlorpropamide
- Glibenclamide
- Organic Compound
- Urea
- Sulfonyl Group
- Carbutamide
- Metahexamide
- Tolazamide
- Tolbutamide