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盐酸吡格列酮

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 盐酸吡格列酮
中文同义词: 5-{4-[2-(5-乙基-2-吡啶)-乙氧基]-苯基}-2,4-噻唑烷二酮盐酸盐;盐酸吡格列酮;吡格列酮;皮格列酮;匹格列酮盐酸盐;盐酸皮格列酮;盐酸匹格列酮;吡格列酮
特性:吡格列酮与罗格列酮是目前我国临床上治疗糖尿病常用的噻唑烷二酮类抗糖尿病药物,属胰岛素增敏剂。可减少外周组织和肝脏的胰岛素抵抗,增加依赖胰岛素的葡萄糖的处理,并减少肝糖的输出。
药理作用:1. 吡格列酮通过直接降低胰岛素抵抗和改善β细胞功能达到持久的控制血糖。吡格列酮是一种具有高度选择性且作用很强的过氧化物酶体增殖活化受体 γ (PPARγ) 激动剂。该受体是一种蛋白质,存在于胰岛素敏感组织的脂肪、骨骼肌和肝脏组织中。
2. 吡格列酮可降低高胰岛素血症和血浆游离脂肪酸水平。血浆胰岛素水平降低表明吡格列酮可减轻胰腺β细胞的负担。由于游离脂肪酸水平高对胰腺有毒性作用,因此降低游离脂肪酸水平亦对胰腺β细胞功能有保护作用。因此,对2型糖尿病的基本生理环节是减少胰岛素抵抗,改善β细胞功能达到控制血糖。
用途:1.吡格列酮主要适用于单靠饮食和运动不能控制血糖的非胰岛素依赖型糖尿病(Ⅱ型)患者的治疗。可单独治疗或与磺酰脲类降糖药、二甲双胍和胰岛素合用治疗。
2. 临床研究表明,吡格列酮可改善胰岛素抵抗患者的胰岛素敏感性,提高胰岛素对细胞的反应性,并改善体内葡萄糖平衡障碍。在临床对照实验中,吡格列酮与磺酰脲类、二甲双胍或胰岛素合用,能提高疗效。


Pioglitazone hydrochloride
Synonyms: Pioglitazone HCl; 5-[[4-[2-(5-Ethyl-2-pyridinyl]ethoxy]phenyl]methyl]-2,4-thiazolidinedione N-Oxide; Pioglitazone N-Oxide; 5-{4-[2-(5-ethyl-1-oxidopyridin-2-yl)ethoxy]benzyl}-1,3-thiazolidine-2,4-dione; 5-[[4-2-(5-ethyl-2-pyridinyl)ethoxy]benzylidene]-2,4-thiazolidinedione Hydrochloride
CAS: 112529-15-4
MF: C19H21ClN2O3S
MW: 392.9
Assay: 98.5%
Appearance: White crystalline powder
Property: Pioglitazone and rosiglitazone is at present the clinical treatment of diabetes common thiazolidine two ketones anti diabetes drugs, belonging to the insulin sensitizing agent. Can reduce the peripheral tissue and hepatic insulin resistance, increase insulin dependent glucose, and decrease hepatic glucose output.
Pharmacological effects:
1. pioglitazone through direct reduce insulin resistance and improve the beta cell function to control blood glucose and lasting. Pioglitazone is a highly selective and very powerful effect of peroxisome proliferator activated receptor gamma (PPAR γ) agonist. The receptor is a protein found in insulin sensitive tissue, fat, skeletal muscle and liver tissue.
2. pioglitazone can reduce hyperinsulinemia and plasma free fatty acid level. Lower plasma insulin levels suggest that pioglitazone can reduce the burden of pancreatic beta cells. Since the level of free fatty acids of high toxic effect on the pancreas, thus reducing the level of free fatty acids also have protective effect on pancreatic beta cell function. Therefore, the basic physiological aspects of type 2 diabetes to reduce insulin resistance, improved beta cell function to control blood glucose.
Usage:
1. mainly applicable to 1 of pioglitazone on diet and exercise can not control the blood glucose in non insulin dependent diabetes mellitus (NIDDM) patients. Can treatment alone or with a sulfonylurea, metformin and insulin treatment.
2. clinical study showed that pioglitazone can improve the insulin resistance, insulin sensitivity, improve the insulin response to cell, and improve glucose homeostasis disorder. In the clinical trials, pioglitazone, metformin and sulfonylurea or insulin, can enhance the curative effect.
Packing: 1kg/bag
Price: USD 198/kg

 

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