GLINIDES non-SU INSULIN SECRETAGOGUES NOVONORM STARLIX

促胰島素分泌劑: 磺醯尿素類SU及GLINIDES

GLINIDES類藥物,  又稱 Meglitinides 類似物, 短效促胰島素分泌的非磺醯類藥物, 包含幾種
Glinides 短效
Repaglinide = novonorm 諾和隆錠 = 安息香酸類衍生物
Nateglinide = Starlix (始糖立釋膜衣錠) = 苯丙胺酸衍生物

可降低餐前餐後血糖波動 , 餐前 15 分鐘服用, 或開始用餐時服用, 或開始用餐 30 分鐘內服用

作用時間短 , 相較於 SU, 低血糖風險降低, 適合慢性腎病使用, 因慢性腎病發生低血糖的風險上升
Repaglinide 半衰期 1 小時
Glinides, Repaglinide and Nateglinide , are short acting secretagogues. The short duration of their action means reduced risk of hypoglycemia compared to sulfonylureas. This is an advantage for diabetic subjects with CKD because they belong in the high risk for hypoglycemia group as already mentioned.

Repaglinide 腸胃道吸收, 肝臟代謝(氧化及結合 glucuronic acid), 主要代謝物是 M1, M2, M4 會經由膽汁排出至糞便, 代謝物沒有降血糖的生理活性

Repaglinide 在第四第五期腎衰竭患者不用降低劑量
Repaglinide is absorbed from the gastrointestinal tract and metabolized in the liver by oxidation and conjugation with glucuronic acid. The major metabolites of repaglinide are M1, M2 and M4. These metabolites are excreted via the bile into the feces and have no hypoglycemic activity[20].
Repaglinide can be used even in CKD stages 4 and 5 without dose reduction.

Nateglinide 快速經腸胃道吸收, 由肝臟代謝為九種主要代謝物 ( M1-M9). 代謝物相較於原型藥有非常微弱的降血糖效果, M7 是唯一具有高生理活性的代謝物, 但僅佔 7% 以下, 降血糖作用主要還是靠 nateglinide, 排出至尿液的藥物, 16% 是原型藥, 84% 是代謝物.
Nateglinide 第五期慢性腎病不要使用
Nateglinide 第四期慢性腎病可減量使用 60mg tid.

Nateglinide is also rapidly absorbed from the gastrointestinal tract and metabolized in liver to 9 main metabolites (M1-M9). These metabolites have much weaker hypoglycemic activity than the parent compound. The only metabolite that retains high activity is the metabolite M7. The concentration of this metabolite however is low (< 7%), resulting in a hypoglycemic effect, which is attributed mainly to intact nateglinide. The excretion of the drug in urine is unchanged form at 16% and by 84% in the form of metabolites.

In CKD stage 5 we avoid Nateglinide , and in stage 4 we adjust the dose (60 mg × 3)

Meglitinides 類： 本類藥品與 sulfonylureas 一樣會促進胰島素分泌，但開始作用時間較快，作 用時間較短。
雖然 repaglinide 濃度、半衰期及曲線下面積（area under curve，AUC）會 因 eGFR 降低而增加，但不需調整劑量。
Nateglinide 的活性代謝物會因 eGFR 降 低造成累積，CKD 病人使用需非常小心。