Pioglitazone: Difference between revisions

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<applet  load="" size="480" color="" frame="true"  spin="on" Scene ="Pioglitazone/Pioglitazone/1" align="right" caption="Pioglitazone, also known as Actos"/>
<StructureSection load='' size='340' side='right' caption='Pioglitazone, also known as Actos' scene='Pioglitazone/Pioglitazone/1'>
===Better Known as: Actos===
===Better Known as: Actos===
* Marketed By: Takeda Pharmaceuticals<br />
* Marketed By: Takeda Pharmaceuticals<br />
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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===
{| class="wikitable" border="1" width="40%" style="text-align:center"
<table style="background: cellspacing="0px"  align="" cellpadding="0px" width="42%">
|-
<tr>
!  colspan="6" align="center"| Glitazone [[Pharmacokinetics]] Comparison at Equivalent Dosages <ref>doi: 10.1111/j.1365-2125.2007.02986.x</ref><ref>PMID:18997160</ref><ref>PMID: 9454824</ref><ref>PMID: 17594391</ref>
<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
|-
<div style="height:100%; width: 100%">
! Parameter
{{:Glitazone Pharmacokinetics}}
! [[Pioglitazone]] (Actos)
</div>
! [[Rosiglitazone]] (Avandia)
</td>
 
</tr>
|-
</table>
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! 1.8
! 1
 
|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! 617
! 361
|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! 83
! 99
|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! 99
! 99
|-
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 3-8
! 3-4
|-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 6244
! 2024
|-
! [[Pharmacokinetics#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM)
! 360
! 10
|-
! Equivalent Dosage (mg)
! 30
! 4
|-
! Metabolism
! Hepatic <br/>(CYP2C8)
! Hepatic <br/>(CYP2C8)
|}


===References===
===References===
Retrieved from "https://proteopedia.org/Pioglitazone"