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Author: Admin | 2025-04-28
Boxed WarningCongestive heart failure:Thiazolidinediones, including pioglitazone, can cause or exacerbate congestive heart failure (CHF) in some patients. After initiation of pioglitazone, and after dose increases, observe patients carefully for signs and symptoms of heart failure (including excessive, rapid weight gain, dyspnea, and/or edema). If these signs and symptoms develop, manage the heart failure according to the current standards of care. Furthermore, discontinuation or dose reduction of pioglitazone must be considered.Pioglitazone is not recommended in patients with symptomatic heart failure. Initiation of pioglitazone in patients with established New York Heart Association (NYHA) class III or IV heart failure is contraindicated. Dosage FormsExcipient information presented when available (limited, particularly for generics); consult specific product labeling.Tablet, Oral:Actos: 15 mg, 30 mg, 45 mgGeneric: 15 mg, 30 mg, 45 mg PharmacologyMechanism of ActionThiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Pioglitazone is a potent and selective agonist for peroxisome proliferator-activated receptor-gamma (PPARgamma). Activation of nuclear PPARgamma receptors influences the production of a number of gene products involved in glucose and lipid metabolism. PPARgamma is abundant in the cells within the renal collecting tubules; fluid retention results from stimulation by thiazolidinediones which increases sodium reabsorption. Pharmacokinetics/PharmacodynamicsDistributionVd (apparent): 0.63 ± 0.41 L/kgMetabolismHepatic (99%) via CYP2C8 and 3A4 to active and inactive metabolites; M-III and M-IV are major circulating active metabolitesExcretionUrine (15% to 30%) and feces as metabolitesOnset of ActionDelayed;
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