INSULIN SECRETAGOGUES

SULFONYLUREAS, MEGTINIDES, D-PHENYLALANINE DERIVATIVES

Increase basal and/or postprandial insulin

levels
Depend on functional cells
Decrease A1C 1% - 2%
Dosing
>Sulfonylureas 1-2 times daily
> Meglitinides, D-phenylalanine
deviratives 3-4 times daily
Adserve events : Weight gain, rare allergy,
hypoglicemy-half max dose is effective

Insulin Secretagogues :
Sulfony lureas and Glinides

chanism of Action
timulate basal and postprandial insulin secretion
quire funtioning beta cells

ety and Efficacy

ecrease A1C approximatly1-2%
verse events : Weight gain, allergy (rare)
ain risk hypoglicemya

sing
tial dose : 1/8 to maximum dose
osing: 1-2 timesday (SFU), 3 timesday (glinides)
aximum effective dose : maximum (full dose with nateglin
ration frequency : day (s) to weeks

Sulfonylureas

Contraindications

Recommended dosing
ranges

Adjust dosage
Half max dose is
effective

Known
hypersensitivity to
the drug ; DKA; Type
1 DM
Glimepiride: 1-8 mg
QD ; Glipizide XR 520 mg Glyburide
1.25-20 mg QD or as
divided doses
Weekly, if needed
(varies depending on
agent)

Insulin Secretagoguges
Sulfonylureas; Meglitinides;
Phenyalanine Derivates
Increase basal and/or postprandial insulin
levels
Actions depend on fungtional -cells
Decrease HbA1C 1%-2%
Dosing :
Sulfonyureas : 1-2 times daily
Meglitinides, phenylalanine derivates: 3-4
times daily
Adverse events; weight gain, hypoglicemia,
allergy is rare

hiazolidinediones : Effect on Body Fa

o Data suggest that TZDs;
Increase subcutaneous
peripheral fat mass
Reduce intra-hepatic and
visceral fat
May increase overall fat
oxidation

hiazolidinediones in Diabetes Therap

ossible secondary benefit include:

May preserve pancreatic - cell function
oMay help reduce progression of disease
Protective cardiovascular effect
oImprove dyslipidemia ( HDL, TG, LDL
density)
oRenal microalbumin excretion
o Vascular smooth muscle cell proliferation and
migration in arterial wall
oEnhance thrombolytic mechanisms
oDecrease PAI- 1
The impact of TZDs on clinical cardiovascular end

hiazolidinediones in Diabetes Therap

Mechanism of action reverse underlying aetiology
oTZDs improve insulin sensititivity
Glucose control achieved without hypoglicemia
oTZD monotherapy or metformin combination (no
increase in insulin)
Possible secondary benefits include:
oPreservation of pancreatic beta cell function
- May help reduce progression of disease
Protective cardiovascular effect
oImprove dyslipidemia ( HDL, TG, LDL density)
oRenal microalbumin excretion
o Vascular smooth muscle cell proliferation and migration
in arterial wall
oEnhance thrombolytic mechanisms
oDecrease PAI- 1

Oral Antihyperglycemic
Agents
for Type 2 Diabetes

Class
Secretagogue

Biguanide

Agent
Sulfonyureas,
Repaglinide,
nateglinide
Metformin

Glucosidase
Inhibitor

Acarbose, miglitol

Pioglitazone,
rosiglitazone

Glitazone (TZO)