メトホルミン·塩酸塩

外観

白色～ほとんど白色、結晶～結晶性粉末

溶解性

水溶状：試験適合

用途

ビグアニド系化合物です。糖 新生抑制作用を示します。また、膵β細胞 刺激作用は少ないとされています。

用途

ビグアニド系化合物です。糖 新生抑制作用を示します。また、膵β 細胞 刺激作用は少ないとされています。

効能

糖尿病治療薬, 血糖降下薬, AMPキナーゼ活性化薬

商品名

グリコラン (日本新薬); メトグルコ (大日本住友製薬); メトホルミン塩酸塩 (トーアエイヨー); メトホルミン塩酸塩 (ニプロ); メトホルミン塩酸塩 (ファイザー); メトホルミン塩酸塩 (三和化学研究所); メトホルミン塩酸塩 (日医工); メトホルミン塩酸塩 (日本ジェネリック); メトホルミン塩酸塩 (東和薬品); メトホルミン塩酸塩 (第一三共エスファ); メトホルミン塩酸塩 (辰巳化学)

説明

Metformin is a biguanide with diverse biological activities. Metformin (250 mg/kg, i.p.) increases hepatic AMPK activity and reduces blood glucose by more than 50% in a liver kinase B1-dependent manner in mice fed normal and high-fat diets, respectively, and reduces blood glucose by 40% in ob/ob mice. It reduces weight gain, hepatic lipid droplet content, and total cholesterol, LDL cholesterol, and triglyceride levels in the plasma of diet-induced obese mice when administered at doses of 10 or 50 mg/kg per day. It also reverses increased hepatic triglyceride and apolipoprotein A5 levels, as well as hepatic steatosis, in a dose-dependent manner in an ob/ob mouse model of non-alcoholic fatty liver disease (NAFLD). Metformin (250 mg/kg) reduces tumor growth in an HCT116 p53^-\- human colon cancer mouse xenograft model, but has no effect on HCT116 p53^-\- tumors overexpressing recombinant S. cerevisiae Ndi1 NADH dehydrogenase, a single-subunit ortholog of the multi-subunit mammalian mitochondrial complex I. Formulations containing metformin have been used in the treatment of type 2 diabetes.

化学的特性

Crystalline Solid

使用

Metformin hydrochloride may be used as a pharmaceutical primary standard for the determination of the analyte in pharmaceutical formulations and human plasma samples by analytical techniques.

定義

ChEBI: A hydrochloride resulting from the reaction of metformin with one molar equivalent of hydrogen chloride.

一般的な説明

1,1-Dimethylbiguanide hydrochloride (metformin) is a strong base. It forms well defined salts and possessing excellent coordination capacity with transition metals, forming highly colored bidentate chelate complexes. Metformin (MET) exists in various forms: diprotonated (H₂MET)²⁺ in strong acidic solution, monoprotonated (HMET)⁺ in weak acid, MET in neutral and deprotonated (MET)^- in strong alkali solution. It is an oral antidiabetic drug. Pharmacokinetics of metformin has been studied. Determination of metformin in human plasma has been described by simple HPLC-UV method. Metformin is reported to increase plasma active glucagon-like peptide-1 (GLP-1) in humans.

生物活性

Antidiabetic agent; lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis via activation of the LKB1/AMPK pathway. Displays antiproliferative effects in cancer cell lines.