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Peroxisome proliferator-activated receptor-γ (PPAR-γ) agonists on glycemic control, lipid profile and cardiovascular

Giuseppe Derosa1, Pamela Maffioli

  • 1Department of Internal Medicine and Therapeutics, University of Pavia, Pavia, Italy. giuseppe.derosa@unipv.it

Current Molecular Pharmacology
|November 30, 2011
PubMed

Insights

Pioglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist, effectively manages type 2 diabetes by improving insulin sensitivity. This review examines its clinical safety and efficacy in treating this common endocrine-metabolic disease.

Area of Science:

  • Endocrinology and Metabolism
  • Pharmacology

Background:

  • Peroxisome proliferator-activated receptor (PPAR) plays a key role in metabolic diseases like obesity and diabetes by influencing insulin resistance and inflammation.
  • Type 2 diabetes mellitus (T2DM) and obesity are prevalent endocrine-metabolic disorders characterized by insulin resistance and impaired insulin secretion.
  • Alterations in carbohydrate, lipid, and protein metabolism are central to the pathogenesis of T2DM.

Purpose of the Study:

  • To review the safety and effectiveness of pioglitazone in the clinical management of type 2 diabetes mellitus.
  • To highlight pioglitazone's role as a PPAR-γ agonist in T2DM treatment.
  • To provide an overview of pioglitazone's therapeutic application following rosiglitazone's market withdrawal.

Main Methods:

  • Literature review focusing on clinical studies and practice data.
  • Analysis of pioglitazone's mechanism of action as a PPAR-γ agonist.
  • Evaluation of safety and efficacy data from clinical trials and real-world evidence.

Main Results:

  • Pioglitazone enhances insulin action by increasing glucose uptake in peripheral tissues and reducing hepatic glucose production.
  • As a PPAR-γ agonist, it regulates genes involved in glucose, lipid, and protein metabolism.
  • Pioglitazone is currently the sole available PPAR-γ agonist for T2DM treatment in many regions.

Conclusions:

  • Pioglitazone demonstrates significant effectiveness in managing type 2 diabetes mellitus.
  • Its safety profile supports its continued use in clinical practice for T2DM.
  • Pioglitazone represents a vital therapeutic option for patients with type 2 diabetes, addressing key metabolic dysregulations.

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