JOURNAL OF KAOHSIUNG MEDICAL ASSOCIATION 2014. vol. 22, No.

-1
(GLP-1 Receptor Agonist)

Incretin

IncretinIntestinal

DeFronzo2

Secretion of Insulin

Incretin

enteroendocrine cells

Glucagon

Incretin

1906 Morre Bfactor

1932 incretin

1960

1964-1967

1971 GIP gastric inhibitory

polypeptide , glucose-dependent
insulinotropic polypeptide ,

1985 GLP-1glucagon like peptide-1

-1

353

-1(GLP-1 Receptor Agonist)

Incretin effect
GLP-1-1

2GIP

GLP-12

GIP

GLP-1

70%

GLP-1GLP-1
DPP-4

Intestinal
GLP-1
GLP-1
Release

Mixed Meal

GLP-1(7-36)
Active

DPP-4

DPP 4

Rapid Inactivation

(>80% of Pool)

t1/2 = 1-2 Minutes

()

GLP-1(9-36)
Inactive

DPP=dipeptidyl peptidase()
GLP=glucagon-like peptide()

:GLP-1DPP-4(3)

354

 JOURNAL OF KAOHSIUNG MEDICAL ASSOCIATION 2014. vol. 22, No.4

-4

GLP-1DPP-4

GLP-1

GLP-1

2
GLP-1DPP-4

DPP-4GLP-1

GLP-1 ,

2.GLP-1

()

()

()
GLP-1

()
()

()

()

GLP-1(GLP-1
)(4)

DPP-4GLP-1
DPP-4

GLP-1

A1C

0.5-1%
()

()
1.0-1.7%

+16-35mg/dl

(exenatide BID)(exenatide QW
,Liraglutide QD)

1-7mmHg
-12 To -40mg/dl

355

-1(GLP-1 Receptor Agonist)

GLP-1 MimeticsGLP-1 Analogs

GLP-1

Agonists1020325

Bloomgarden

GLP-1DPP-4

GLP-1RA

GLP-1

DPP-4

GLP-1

GLP-1 RA

AnaloguesGLP-1

GLP-1 RA

GLP-1 RAGLP-1 Receptor Agonist

-1

FDA

2005Exenatide BID

Glucagon like

2010

Peptide-1-Receptor Agonist
GLP-1

(A1C,%)
(mg/dl)
(mg/dl)

(nausea)

Exenatide BID
*(Byetta)

Exenatide QW
*(Bydureon)

Linaglutide QD
*(Victaza)

0.8-1.5
11-25
124

,60
60

1.3-1.9
32-41
95

1.1-1.5
19-28

2

29,30,31
23
510 Mg,

356

,
3032
0.6,1.21.8
Mg,

 JOURNAL OF KAOHSIUNG MEDICAL ASSOCIATION 2014. vol. 22, No.4

Liraglutide QD

2012Exenatide QW

GLP-1RA

GLP-1 RA

GLP-1 RA

GLP-12005

FDA,

GLP-1 RA(

)1.BMI352.<50

1.Daniel J.Drucker: The biology of inretin

3.10

hormones, Cell Metabolism;2006:3:153-

4.2

165.
2.Daniel J Drucker, Michael A Nauck: The

A1C8.5%5.,
6.

incretin system: glucagon-like peptide-1

DeFronzo

receptor agonists and dipeptidyl

Metformin + pioglitazon + GLP-

peptidase-4 inhibitors in type 2

1RA

diabetes: Lancet 2006;368:1696-705.

1.

3.Timothy S. Reid: Practical use of

2.

glucagons-like peptide-1 receptor

,eGFR<30mL/

agonist therapy in primary care.

min/1.73m 3.

Clinical Diabetes 2013;31:148-157.

4.Mansur Shomaili: Optimizing the

care of patients with type 2 diabetes

using incretin-based therapy: focus

GLP-1

357

on GLP-1 receptor agonists.Clinical

Diabetes:2014;32(1):32-43.