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Thia Zoli Dined I Ones

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THIAZOLIDINEDIONES

By-
SOUMYADEEP MONDAL
ROLL NO- 12401915047
INTRODUCTION
 Thiazolidinediones are one of the most important class of
drugs, mainly used as Oral Hypoglycaemics.
 The Thiazolidinediones are also known as “glitazones” are
sometimes referred as Insulin Enhancers.
 They are exemplified from Ciglitazone, the first of these
glitazones. The first drug to be marketed under this class is
Troglitazone.
 Other examples of this class of drugs are Rosiglitazone and
Pioglitazone.
 These drugs are used in combination therapy with Metformin,
Sulfonylureas or Insulin.
 Glitazones lower blood glucose level by improving sensitivity
to insulin in target tissues mainly adipose tissues, skeletal
muscle, liver. These agents are dependent upon insulin for their
activity.
EXAMPLES OF THIAZOLIDINEDIONES
O
O

NH
NH H3C
CH3 S
S O
O CH3 O
O HO O

CIGLITAZONE H3C CH3


TROGLITAZONE

O
O O
CH3
NH
N N S
O S NH
O N
O
H3C
PIOGLITAZONE
ROSIGLITAZONE
MECHANISM OF ACTION
Thiazolidinediones are selective agonists for nuclear peroxisome
proliferator-activated receptor-γ (PPAR γ).
1. These drugs bind to PPARγ, which activates insulin-
responsive genes that regulate carbohydrate and lipid
metabolism (thiazolidinediones require insulin to be present
for their action (preferably Type II).
2. Thiazolidinediones increase glucose transport into muscle
and adipose tissue by enhancing the synthesis and
translocation of specific forms of the glucose transporters.
3. The thiazolidinediones also can activate genes that regulate
fatty acid metabolism in peripheral tissue.
4. Drugs act as agonist for PPARγ which then bind to DNA
activating transcription of a wide variety of metabolic
regulators and they enhance gene expressions.
THANK YOU

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