-
外観
白色〜わずかにうすい褐色, 結晶性粉末〜粉末
-
溶解性
水に可溶
-
用途
α-グルコシダーゼ阻害剤です。 二糖から単糖に分解するα-グルコシダーゼ を阻害し、糖質の消化・吸収を遅延させる作 用があります。
-
用途
α- グルコシダーゼ阻害剤です。
二糖から単糖に分解するα- グルコシダーゼ
を阻害し、糖質の消化・吸収を遅延させる作
用があります。
-
効能
糖尿病治療薬, α-グルコシダーゼ阻害薬
-
商品名
ベイスン (武田テバ薬品); ベイスン (武田テバ薬品)
-
説明
Voglibose was introduced in Japan for the treatment of postprandial
hyperglycemia in diabetic patients. As an orally active α-D-glucosidase inhibitor, it
is effective in decreasing the release of glucose from carbohydrate ingestion and
slowing the increase of postprandial blood glucose levels, as demonstrated in
animals and humans following sucrose and starch loading. In addlion, voglibose
was reported to have prophylactic effect in genetically obese Wistar rats,
maintaining low plasma levels of glucose, triglyceride and insulin, indicating a
potential usefulness for the management of other carbohydrate-dependent
metabolic disorders such as obesity. Voglibose is much more potent and has fewer
side effects than acarbose, another agent in its class.
-
化学的特性
Colourless Crystalline Solid
-
使用
Voglibose is an α-glucosidase inhibitor, similar to acarbose and miglitol, used for lowering post-prandial hyperglycemia (PPHG) in people with diabetes mellitus. Voglibose is used to study it benefits as a protectant against ischemia-reperfusion injury through glucagon-like peptide 1 receptors and the phosphoinositide 3-kinase-Akt-endothelial nitric oxide synthase pathway.
-
世界保健機関（WHO）
Acarbose and voglibose area-glucosidase inhibitors and delay
digestion/absorption of carbohydrates as well as improving postprandial
hyperglycaemia.
-
一般的な説明
The most potent -glucosidase inhibitor is the valiolamine derivative voglibose. Compared with acarbose its inhibitory potency in vitro, depending on the -glucosidase enzyme, is up to 200 times higher. In Japan, daily dosages are only 0.3 – 0.9 mg, however, therapeutic efficacy on HbA1c reduction could not be clearly demonstrated with those dosages. HbA1c, a glycated hemoglobin species, which occurs in blood, is a diagnostic measure for the non-enzymatic glycation process, and depends on the plasma glucose concentration. The process of protein glycation is discussed to be responsible for the development of diabetic complications (neuropathy, retinopathy, nephropathy). In Europe voglibose is under evaluation with distinctly higher daily dosages of 1.5 to 6 mg. In contrast to acarbose, the smaller inhibitors of the monosaccharide type (miglitol, emiglitate, voglibose) do not inhibit pancreatic -amylase.
-
生物活性
Orally active α -glucosidase inhibitor (IC 50 values are 3.9 and 6.4 nM at sucrase and maltase respectively). Increases glucagon-like peptide 1 (GLP-1) secretion and decreases food consumption in ob/ob mice, and reduces plasma concentrations of glucose, triglycerides and insulin in Wistar fatty rats. Exhibits antidiabetic and antiobesity activity in vivo .
