2.商品名:Repaglinide [Prandin-Novo Nordisk] [NovoNorm-Novo Nordisk]

0.25mg,0.5mg,1mg,2mg/#

3.化學結構:

4.分類:

•藥理分類:Benzoic acid,Nonsulfonylurea compound,Nonsulfonylurea oral

agents,Insulin secreting agent)

•治療分類:OHA-Oral hypoglycemic agent新型口服降糖藥物

•懷孕危險分類: ? 動物試驗無致畸性,孕婦未列入測試對象

•授乳: ? 未列入測試對象

•小兒使用:不適用於Type 1 Diabetes mellitus

5.適用症與劑量:

(1)對於第2型糖尿病,無法單獨以飲食及運動控制血糖者

0.5-4.0mg TID AC ; < 16mg/D

建議初始劑量:0.5mg TID AC (HbA1c < 8%)

2mg TID AC (HbA1c > 8%)

6.臨床效應:

(1)作用快而短暫,可以控制飯後增高之血糖

(2)可降低HbA1c 1.4-1.9%

(3)臨床試驗

飯後2小時之血糖下降為3-6 mmol/L (54-108mg/dl) [Novo 1998]

7.作用機轉:

(1)促進胰島素之分泌,作用不同於Sulfonylurea (磺基尿素)

抑制ATP-dependent potassium channel (鉀徑路),阻止鉀離子由細胞內外排,

觸發Calcium channel (鈣離子)之開張,鈣離子湧入細胞,促進胰島素之分泌

(2)作用快而短暫

8.代謝與排泄:

口服吸收迅速,口服後1小時達血中最高濃度,然後瞬即消褪,口服4小時後

產物無降血糖作用。

9.討論:

Novo藥廠Dr Peter Damsbo認為吃過飯的時候才真正需要胰島素

[Peter Damsbo,1998]

Repaglinide可以適時掌控進食後之血糖上升,更可避免禁食三餐不繼等造成

10.副作用:

(3)Flushing潮紅

11.參考文獻:

(1)Wolffenbuttel BHR:Effects of a new oral hypoglycaemic agent,repaglinide,on

metabolic control in sulphonylurea-treated patients with NIDDM.

Eur J Clin Pharmacol 1993;445:113-116.

(2)Ampudia-Blasco FJ:Comparative dose-related time-action profiles of

glibenclamide and a new non-sulphonylurea drug,AG-EE 623 ZW,during

euglycaemic clamp in healthy subjects. Diabetologia 1994;37:703-707.

(3)Gromada J:Effects of the hypoglycemic drugs repaglinide and glibenclamide

on ATP-sensitive potassium-channels and cytosolic calcium levels in βTC3

cells and rat pancreatic beta cells. Diabetologia 1995;38:1025-1032.

(4)Kikuchi M:Modulation of insullin secretion in non-insulin-dependent diabetes

mellitus by two novel oral hypoglycaenic agents. NN 623 and A 4166

Diabetic Medicine 1996;13:S151-S155.

(5)Repaglinide Drugs of the Future 1996;21 (7):694-599.

12.致謝:

[87.12.10 (四)]