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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* Date of FDA Approval (Patent Expiration): 1999 (2011)<br />
* Date of FDA Approval (Patent Expiration): 1999 (2011)<br />
* 2009 Sales: $2.4 Billion <ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS</ref>
* 2009 Sales: $2.4 Billion <ref>http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS</ref>
* Why You Should Care: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States.  
* Importance: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States.  
* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information
* See [[Pharmaceutical Drugs]] for more information about other drugs and disorders
 
===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>
</StructureSection>
===Pharmacokinetics===
===Pharmacokinetics===
 
<table style="background: cellspacing="0px" align="" cellpadding="0px" width="42%">  
{| class="wikitable" border="1" width="40%" style="text-align:center"
<tr>
|-
<td style="width:100%; vertical-align:top;border-width:0px; border-style:inset">
!  colspan="6" align="center"| Glitazone [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|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>
<div style="height:100%; width: 100%">
|-
{{:Glitazone Pharmacokinetics}}
! Parameter
</div>
! [[Pioglitazone]] (Actos)
</td>
! [[Rosiglitazone]] (Avandia)
</tr>
 
</table>
|-
! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr)
! 1.8
! 1
 
|-
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml)
! 617
! 361
|-
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%)
! 83
! 99
|-
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%)
! 99
! 99
|-
! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! 3-8
! 3-4
|-
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! 6244
! 2024
|-
! [[Pharmaceutical_Drugs#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"