Pioglitazone: Difference between revisions
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< | <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 /> | ||
* Major Indication: Hypoglycemia & Type 2 [[Diabetes]]<br /> | * Major Indication: Hypoglycemia & Type 2 [[Diabetes]]<br /> | ||
* Drug Class: [[PPAR|PPAR-γ]] | * Drug Class: [[PPAR|PPAR-γ]] Agonist - Thiazolidinedione (Glitazones) | ||
* 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> | ||
* | * Importance: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States. | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and disorders | ||
===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> | |||
</StructureSection> | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:Glitazone Pharmacokinetics}} | |||
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===References=== | ===References=== | ||
