Pioglitazone Tablets

Mechanism

Pioglitazone acts as a selective agonist of peroxisome proliferator-activated receptor gamma (PPAR-γ). Activation of this receptor enhances transcription of insulin-responsive genes involved in glucose and lipid metabolism, thereby improving insulin sensitivity and reducing hepatic glucose output. :contentReference[oaicite:0]{index=0}

Pharmacokinetics

• Absorption: Rapidly absorbed; peak plasma concentration within ~2 hours
• Distribution: Highly protein bound (>99%)
• Metabolism: Extensively metabolized in liver via CYP2C8 and CYP3A4
• Elimination: Excreted mainly via bile and feces
• Half-life: 3–7 hours (parent drug); metabolites 16–24 hours

Side Effects

• Weight gain
• Edema
• Headache
• Upper respiratory infection
• Risk of heart failure (rare)

Contraindication

• Heart failure (NYHA Class III/IV)
• Severe hepatic impairment
• Hypersensitivity to pioglitazone

Interaction

• Insulin – increased risk of edema
• Gemfibrozil – increases drug levels
• Rifampicin – reduces effectiveness

Warning and Precautions

• Monitor liver function regularly
• Use cautiously in cardiac patients
• Risk of fluid retention
• Regular blood glucose monitoring required