Pioglitazone: Difference between revisions

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<StructureSection load='' size='340' side='right' caption='Pioglitazone, also known as Actos' scene='Pioglitazone/Pioglitazone/1'>
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/>
<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/>
===Better Known as: Actos===
===Better Known as: Actos===
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===Mechanism of Action===
===Mechanism of Action===
Pioglitazone is a selective agonist for Peroxisome Proliferator-Activated Receptor Gamma ([[PPAR]]). When PPAR is not bound by ligand, it forms a complex with various co-repressors which possess histone deacetylation activity, maintaining tight chromatin structure and preventing gene transcription. This complex is released upon ligand binding (typical ligands are lipids), allowing various co-activators and co-activator-associated proteins to be recruited. Pioglitazone functions by by binding to the active site of PPARγ, causing the release of co-repressors and activation of the receptor. Activation of PPAR results in transcription of [[Molecular Playground/Insulin|insulin]] responsive genes involved in the control of glucose production, transport and utilization. This explains why the glitazones are referred to as "insulin sensitizers." <ref>PMID:9744270</ref>
Pioglitazone is a selective agonist for Peroxisome Proliferator-Activated Receptor Gamma ([[PPAR]]). When PPAR is not bound by ligand, it forms a complex with various co-repressors which possess histone deacetylation activity, maintaining tight chromatin structure and preventing gene transcription. This complex is released upon ligand binding (typical ligands are lipids), allowing various co-activators and co-activator-associated proteins to be recruited. Pioglitazone functions by by binding to the active site of PPARγ, causing the release of co-repressors and activation of the receptor. Activation of PPAR results in transcription of [[Molecular Playground/Insulin|insulin]] responsive genes involved in the control of glucose production, transport and utilization. This explains why the glitazones are referred to as "insulin sensitizers." <ref>PMID:9744270</ref>
 
</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
<table style="background: cellspacing="0px"  align="" cellpadding="0px" width="42%">  
<table style="background: cellspacing="0px"  align="" cellpadding="0px" width="42%">  

Revision as of 14:10, 9 January 2024

Pioglitazone, also known as Actos

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Pharmacokinetics

Glitazone Diabetes Comparison at Equivalent Dosages
Parameter Pioglitazone (Actos) PPAR-γ (Avandia)
Pharmaceutical Drugs (hr) 1.8 1
PPAR (ng/ml) 617 361
insulin (%) 83 99
Protein Binding (%) 99 99
T1/2 (hr) 3-8 3-4
AUC (ng/ml/hr) 6244 2024
IC50 (nM) 360 10
Equivalent Dosage (mg) 30 4
Metabolism Hepatic
(CYP2C8)
Hepatic
(CYP2C8)

For Pharmacokinetic Data References, See: References

References


Proteopedia Page Contributors and Editors (what is this?)

David Canner, Alexander Berchansky