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Endocrine Diseases
Published in Miriam Orcutt, Clare Shortall, Sarah Walpole, Aula Abbara, Sylvia Garry, Rita Issa, Alimuddin Zumla, Ibrahim Abubakar, Handbook of Refugee Health, 2021
If glycaemic control is not achieved, a sulfonylurea is added. Gliclazide and glibenclamide are widely available sulfonylureas; gliclazide is associated with fewer hypoglycaemic episodes. Sulfonylureas should not be used in ketosis, lactation or porphyria.Start gliclazide at 40 mg daily; increase weekly up to 160 mg/day with breakfast or, if needed and tolerated, increase to a maximum of 160 mg twice daily with meals.Glibenclamide is initiated at 2.5 mg daily with breakfast and increased by 2.5 mg each week, as needed and tolerated, to a maximum of 15 mg daily.
The Endocrine System and Its Disorders
Published in Walter F. Stanaszek, Mary J. Stanaszek, Robert J. Holt, Steven Strauss, Understanding Medical Terms, 2020
Walter F. Stanaszek, Mary J. Stanaszek, Robert J. Holt, Steven Strauss
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
Published in Lelio G. Colombetti, Principles of Radiopharmacology, 2019
Raymond E. Counsell, Nancy Korn
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
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 are a heterogeneous group of drugs that vary in their tissue selectivity and their risk for hypoglycemia and cardiovascular events. They have high glycemic efficacy comparable to or better than most other glucose lowering drugs and the glycemic durability for the new generation sulfonylureas is similar to other agents. The risk of hypoglycemia can be reduced by selection of suitable patients and using the most appropriate drugs. Modest weight gain may occur, and patients should be advised to try to minimize this by attention to lifestyle factors. Sulfonylureas are the first-line treatment for patients with certain types of MODY and neonatal diabetes and they remain the most commonly used second-line treatment after metformin for most patients with T2D. Some of the new generation sulfonylureas have been shown not to be associated with increased cardiovascular risk and a precision medicine approach should help to identify which patients can benefit the most from treatment with sulfonylureas.