レパグリニド

外観

白色～ほとんど白色、結晶性粉末～粉末

溶解性

メタノール、ジクロロメタン及びN,N-ジメチルホルムアミドに溶けやすく、アセトニトリルにやや溶けやすく、水にほとんど溶けない。

用途

レパグリニド（Repaglinide）は、ミチグリニドやナテグリニド等と同じフェニルアラニン誘導体であり、グリニド系と呼ばれる群に属する経口糖尿病薬の一つである。1983年に発見された。膵β細胞からのインスリン分泌を促進する。

用途

速効型インスリン分泌促進剤 です。膵β 細胞膜の スルホニル（SU）受容 体と結合してカリウムチャネルを閉じること によりインスリン分泌を促進します。SU 系 尿素剤と比較し、作用時間が短く、効果の消 失が早いです。

効能

糖尿病治療薬, 血糖降下薬, スルホニル尿素受容体作動薬

商品名

シュアポスト (大日本住友製薬)

使用上の注意

アルゴン封入

説明

Repaglinide was marketed in the US as an orally active hypoglycemic agent in patients with a type Ⅱ diabetes mellitus, to lower blood glucose in synergistic combination with metformin, when hyperglycemia cannot be controlled by diet, exercise or metformin alone. Chiral (S)-repaglinide can be synthesized in several ways, each involving a stereoselective reduction of an imine or enamine group. Repaglinide is a nonsulfonylurea belonging to the meglitinide family, with an insulin-releasing effect mediated by pancreatic betacells, by closing the ATP-sensitive K+ channels that, in turn, increases the cytosolic concentration of Ca++. In several animal models, repaglinide was more efficient than glibenclamide as a dose-dependant promoter of insulin release, but its mechanism of action is probably slightly different. Repaglinide has a rapid onset of action, a short duration of action and a reduced risk of hypoglycemia compared to glyburide.

化学的特性

White to Off-White Solid

使用

The R-enantiomer showed only weak hypoglycemic activity. Repaglinide impurity

一般的な説明

Repaglinide is 2-ethoxy-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid(Prandin); approvals for generics are pending. Combinationsare available with metformin in the United States(Prandimet), and the drug may also be coprescribed with oneof the thiazolidinediones (typically pioglitazone or rosiglitazone;see previous discussion). To establish the most clinicallyvaluable dose, the patient is titrated while monitoringblood glucose levels and hemoglobin glycosylation (HbA1c)as an index of longer-term overall control.

生物活性

K ATP channel blocker that binds with high affinity for SUR1 when co-expressed with Kir6.2 (K d = 0.42 nM). Antidiabetic glucose regulator with hypoglycaemic effect in vivo .

臨床応用

Repaglinide is a nonsulfonylurea insulin secretagogue that was introduced in the United States in 1998 for type 2 diabetes.