格列吡嗪

格列吡嗪用途

【用途一】
为非胰岛素依赖型(II型)糖尿病的降糖药
【用途二】
为非胰岛素依赖型（Ⅱ）型糖尿病之降糖良药。

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格列吡嗪作用

格列吡嗪为第二代磺脲类口服降血糖药。主要是促进胰岛β细胞分泌胰岛素，尤其是促进葡萄糖刺激的胰岛素β细胞分泌；还有增强胰岛素作用，从而有效地降低血糖浓度和糖基化血红蛋白；并可改善高脂血症，降低甘油三酯和胆固醇水平，提高高密度脂蛋白胆固醇在总胆固醇中比率；还可抑制血小板聚集和促进纤维蛋白溶解，因而对血管病变可能有一定的防治作用。①促进胰腺胰岛β细胞分泌胰岛素，先决条件是胰岛β细胞还有一定的合成和分泌胰岛素的功能；②通过增加门静脉胰岛素水平或对肝脏直接作用，抑制肝糖原分解和糖原异生作用，肝生成和输出葡萄糖减少；③也可能增加胰外组织对胰岛素的敏感性和糖的利用（可能主要通过受体后作用），因此，总的作用是药动学吸收快，口服后1～2.5小时血药浓度达峰值，作用持续时间可达24小时，T1/2为2.5～4小时。主要经肝代谢失去活性，第l天97%排出体外，第2天100%排出体外。

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格列吡嗪名称

[ CAS 号 ]:
29094-61-9

[ 中文名 ]:
格列吡嗪

[ 英文名 ]:
Glipizide

[中文别名 ]:

格列甲嗪

[英文别名 ]:

EINECS 249-427-6
Glican
Ozidia
Glipid
k4024
exylurea
Glucotrol
Glipizide
MFCD00072159
Mindiab

格列吡嗪生物活性

[ 描述 ]:

Glipizide可作用于钾离子通道,可用于2型糖尿病。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 代谢疾病

[参考文献]

[1]. Chowdary, K.P. and Y.S. Rao, Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech, 2003. 4(3): p. E39.

[2]. Rao, N.G., et al., Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law, 2006. 46(3): p. 263-9.

[相关活性小分子]

格列吡嗪物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
676.0±65.0 °C at 760 mmHg

[ 熔点 ]:
208-209°C

[ 分子式 ]:
C₂₁H₂₇N₅O₄S

[ 分子量 ]:
445.535

[ 闪点 ]:
362.6±34.3 °C

[ 精确质量 ]:
445.178375

[ PSA ]:
138.53000

[ LogP ]:
3.37

[ 外观性状 ]:
白色或灰白色结晶粉末

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.654

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
methanol: 1.9 mg/mL

格列吡嗪MSDS

详细MSDS(安全技术说明书)

格列吡嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YS7640000

CHEMICAL NAME :: Urea, 1-cyclohexyl-3-((p-(2-(5-methylpyrazinecarboxamido)et hyl)phenyl)sulfonyl)-

CAS REGISTRY NUMBER :: 29094-61-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C21-H27-N5-O4-S

MOLECULAR WEIGHT :: 445.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 2400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

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格列吡嗪安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;Xn: Harmful;

[ 风险声明 (欧洲) ]:
R21

[ 安全声明 (欧洲) ]:
S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
YS7640000

[ 海关编码 ]:
2935009090

格列吡嗪海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

格列吡嗪文献

Identification of CYP3A7 for glyburide metabolism in human fetal livers.

Biochem. Pharmacol. 92(4) , 690-700, (2014)

Glyburide is commonly prescribed for the treatment of gestational diabetes mellitus; however, fetal exposure to glyburide is not well understood and may have short- and long-term consequences for the ...

Maternal-fetal disposition of glyburide in pregnant mice is dependent on gestational age.

J. Pharmacol. Exp. Ther. 350(2) , 425-34, (2014)

Gestational diabetes mellitus is a major complication of human pregnancy. The oral clearance (CL) of glyburide, an oral antidiabetic drug, increases 2-fold in pregnant women during late gestation vers...

Quantitative determination of metformin, glyburide and its metabolites in plasma and urine of pregnant patients by LC-MS/MS.

Biomed. Chromatogr. 29(4) , 560-9, (2015)

This report describes the development and validation of an LC-MS/MS method for the quantitative determination of glyburide (GLB), its five metabolites (M1, M2a, M2b, M3 and M4) and metformin (MET) in ...

更多文献

格列吡嗪

格列吡嗪用途

格列吡嗪作用

格列吡嗪名称

格列吡嗪生物活性

格列吡嗪物理化学性质

格列吡嗪MSDS

详细MSDS(安全技术说明书)

格列吡嗪毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

格列吡嗪安全信息

格列吡嗪海关

格列吡嗪文献

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