Details
Glibenclamide
Synonyms: N- [2- [4 - [[[([Cyclohexylamino] carbonyl] amino] sulfonyl] phenyl] ethyl] -2-methoxy-5-chlorobenzamide; ; 5-chloro-N- [2- [4 - [[[([cyclohexylamino] carbonyl] amino] sulfonyl] phenyl] ethyl] -2-methoxybenzamide; Phenylurea; glibenclamide; glibenclamide; glibenclamide, 99%
English name: 5-Chloro-N- [2- [4 - [[(cyclohexylamino) carbonyl] -amino] sulfonyl] phenyl] -ethyl] -2-methoxybenzamide
2-CHOORY-N- [2- [4- [4- [4- [4- [4- [4- [4- [4- (4- [4- [4- (4- [4- (4- [4- (4- [4- [[(CYCLOHEXYLAMINO) CARBONYL] AMINO] -SULFONYL] PHENYL] ETHYL] -2-METHOXYBENZAMIDE
CAS: 10238-21-8
Nature: white crystalline powder, insoluble in water, slightly soluble in ethanol, acetone, chloroform.
Uses: Hypoglycemic agents for the treatment of mild, non-insulin-dependent diabetes mellitus
Glibenclamide is also called hypoglycemic, daan therapy, is the second generation of oral sulfonylurea hypoglycemic agents, the mechanism of action with tolbutamide, the hypoglycemic effect of the strongest sulfonylurea, the role of intensity Tocopidone 200 to 250 times. Can selectively act on pancreatic β cells, promote insulin secretion, can enhance the role of exogenous insulin hypoglycemic effect, strengthen the role of insulin receptor. Oral absorption fast, high protein binding rate, in 30 minutes began to play a role in the 1.5 hours of the strongest role, the duration of 16 to 24 hours. Distribution volume of 0.1L / kg, plasma protein binding rate of 90% to 95%, half-life of 4 to 8 hours. Mainly by the liver metabolism, there are six kinds of metabolites, known as two kinds of hydroxyl compounds, no hypoglycemic effect, mainly from the urine, a small amount of stool discharged. Clinically, mainly for the treatment of mild to moderate non-insulin-dependent diabetes mellitus.
Recently, an international study found that the commonly used diabetes drugs glibenclamide can help the body's immune system to deal with certain bacterial infections, such as treatment of gangrene, the mortality rate can be reduced by about half.
The class of glanders is a disease prevalent in tropical areas such as Southeast Asia and northern Australia. It is caused by pathogens, and its symptoms include sepsis and pneumonia. The mortality rate is higher. Diabetics are often more susceptible to infection with glanders, but compared with other patients, the mortality rate is low.
Glibenclamide is currently the most commonly used in the treatment of type 2 diabetes one of the drugs, because the role of this product is fast and strong, so the effect is more obvious, can be a good control of blood sugar, suitable for high blood sugar, with other sulfonyl Urea hypoglycemic agents ineffective.
Sulfonylurea oral hypoglycemic agents commonly used in the two drugs are glibenclamide and glimepiride, two hypoglycemic effect comparison is as follows:
(1) Effects on Glucose Transport and Metabolism: Glibenclamide and glimepiride can promote the expression of glucose in the surrounding tissues by stimulating the key enzymes of glucose metabolism and improving the translocation / dephosphorylation of the glucose transporter (GLUT4) Intake, the specific performance in the synthesis of glycogen and fat formation increased. Glycogen synthase and 3-phosphoglycerol fatty acyltransferase are key enzymes in glycogen and fat synthesis, while glimepiride is stronger than glibenclamide in activating these key enzymes, such as activating glycogen synthase The activity of glimepiride is 2.5 times that of glibenclamide, the ability to activate fat synthase, and glimepiride is 1.9 times that of glibenclamide. Glimepiride enhances the expression of GLUT4 on the cell membrane by inducing dephosphorylation of GLUT4.
(2) The role of glycosylation-phosphatidylinositol-specific phospholipase (GPI-PLC): GPI is located in the outer layer of the cell membrane, involved in insulin signaling, can interfere with muscle and fat cells glucose metabolism. GPI-PLC can make GPI shedding, thereby improving the cell phosphorylation status. Insulin and sulfonylurea can activate GPI-PLC, contribute to muscle, adipose tissue uptake of glucose. But when insulin resistance is present, insulin itself is difficult to activate GPI-PLC, but glimepiride still activates the enzyme. In vivo and in vitro studies, glimepiride in the sulfonylurea drugs in the strongest pancreatic effect, can improve the synthesis of sugar source 2.5 times, fat synthesis 4 times. The ratio of the strength of glimepiride and glibenclamide was 2: 1. Thus, the incidence of secondary failure of glimepiride is lower than that of other sulfonylureas.
Precautions:
Glibenclamide should be used from small doses. During the medication should be regularly checked urine sugar, urine ketone body, urine protein and blood sugar, blood, liver and kidney function, vision, retinal blood vessels.
(1) liver, renal insufficiency, leukopenia, allergic to sulfonamides, pregnant women and diabetes complicated with acidosis and acute infection disabled.
(2) can cause bloating, abdominal pain, anorexia, nausea and other gastrointestinal reactions. Also visible allergies (skin erythema or urticaria), leukopenia, granulocyte deficiency, thrombocytopenia, hypoglycemia, etc., should be immediately discontinued and treated. Which is more common in hypoglycemic reactions.
(3) glibenclamide and other sulfonylurea hypoglycemic agents are not with thiazide diuretics or glucocorticoids combined.
(4) should be avoided with anticoagulants such as dicoumaux equivalent service.
(5) and the combination of Baotai Song, the goods can make the hypoglycemic effect increased, causing acute hypoglycemia.
(6) and sulfonamides can make the role of glibenclamide and toxicity are enhanced, should not be combined.
(7) combined with chloramphenicol can also make the role of this product and toxic side effects, such as the two drugs combined, according to the patient's blood glucose levels to adjust the dose, or can cause hypoglycemic shock.
(8) sulfonylurea drugs can enhance the toxicity of ethanol, during treatment should be alcohol.
KG Pharmaceutical Grade 98% Powder White 25KG / Cardboard Barrel
China (Mainland)