Gliclazide

Description

What is Gliclazide?

Gliclazide is the second generation of sulfur ureide oral hypoglycemic agents, and it also has dual function of hypoglycemic and improving blood clotting. It not only can improve the metabolism of diabetic patients, but also can improve or delay the occurrence of diabetic vascular complications. Gliclazide was developed by the French SERVIER company, and listed in France as early as 1972. Its trade name is diamicron gliclazide.

Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It has been classified differently according to its drug properties in which based on its chemical structure, gliclazide is considered a first-generation sulfonylurea due to the structural presence of a sulfonamide group able to release a proton and the presence of one aromatic group. On the other hand, based on the pharmacological efficacy, gliclazide is considered a second-generation sulfonylurea which presents a higher potency and a shorter half-life. Gliclazide belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).

Basic Information

Product Name:	Gliclazide
Synonyms:	Gliclazide BP; diamicron gliclazide; Gliclazide HCL; Gliclazidum; Gliclazida
CAS:	21187-98-4
MF:	C15H21N3O3S
MW:	323.41
EINECS:	244-260-5
Product Categories:	Pharmaceutical raw materials;APIs;Intermediates & Fine Chemicals;Hormones and the Endocrine System

Chemical Structure

Gliclazide

Chemical Properties

Melting point	163-169 °C (lit.)
density	1.2205 (rough estimate)
refractive index	1.6740 (estimate)
storage temp.	2-8°C
solubility	methylene chloride: soluble
pka	6.07±0.10(Predicted)
form	powder
color	white
InChIKey	BOVGTQGAOIONJV-UHFFFAOYSA-N

Gliclazide Effects

1. Hypoglycemic effect: Gliclazide is a second-generation oral sulfonylurea hypoglycemic agent, and its effect is more than 10 times stronger than that of tolbutamide. The mechanism of action is to stimulate the pancreatic β-cells to release insulin and reduce hyperglycemia. This may be due to the binding of sulfonylurea drugs to receptors on the surface of β cells, which increases their activation and at the same time increases the sensitivity of peripheral target tissues to insulin.

2. It could reduce platelet aggregation and adhesion, prevent fibrin deposition on capillaries.

3. It could reduce cholesterol accumulation and reduce the plasma concentration of arterial glycerol triphosphate and fatty acid. The three functions, in addition to treating diabetes metabolic disorders, can also prevent and treat diabetic complications-the occurrence and development of vascular, retina, and renal dysfunction.

4. Gliclazide has a strong effect. Its mechanism is to selectively act on pancreatic β cells to promote insulin secretion and increase the release of insulin after eating glucose, which inhibits the production and output of glycogen. It has the effect of lowering blood sugar Chemicalbook for adult diabetic patients, lowering cholesterol accumulation, reducing the plasma concentration of aortic triphosphate glycerides and fatty acids, so Gliclazide can not only treat diabetic metabolic disorders, but also prevent diabetic microangiopathy. Improve retinopathy and kidney function.

Technical Support & Resources

Information provided in the Gliclazide description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

MSDS: MSDS available.

COA: COA can be available if you send us inquiry.

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