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Pharmacodynamics: Mechanism of Action: Pioglitazone is a thiazolidinediones antidiabetic agent. Pioglitazone decreases insulin resistance in the periphery and in the liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output. Pioglitazone is a potent and highly selective agonist for peroxisome proliferator-activated receptor-gamma (PPARγ). PPARγ receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle and liver.
Pharmacokinetics: Volume of distribution (Vd) of this drug is 0.63 L/kg. Protein binding is 99.8%. This drug metabolizes by hepatic (99%) via CYP2C8, CYP2C9, and CYP3A4 to both active and inactive metabolites. Elimination half-life for parent drug is 3-7 hours and elimination half-life for the total is 16-24 hours. Time to peak is about 2 hours. This drug is excreted by the urine (15% to 30%) and by feces as metabolites.
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