Brand Name of Pioglitazone
The brand name for pioglitazone (TZD) is Actos. 1
Drug Information
Pioglitazone is marketed under the brand name Actos by Takeda Pharmaceuticals. It belongs to the thiazolidinedione (TZD) class of oral antidiabetic medications used in the management of type 2 diabetes mellitus. 2
Key characteristics of pioglitazone include:
- Pioglitazone is a peroxisome proliferator-activated receptor γ (PPAR-γ) activator that improves insulin sensitivity in skeletal muscle and reduces hepatic glucose production 2
- It is available in tablet form for oral administration in strengths of 15 mg, 30 mg, and 45 mg 1
- Pioglitazone has a half-life of about 9 hours but its glucose-lowering effects are extended due to two active metabolites 3
- It can be administered once daily without regard to meals 3
Mechanism of Action
Pioglitazone works through several mechanisms:
- Acts primarily by decreasing insulin resistance in peripheral tissues and the liver 1, 4
- Improves sensitivity to insulin in muscle and adipose tissue while inhibiting hepatic gluconeogenesis 1
- Enhances glycemic control while reducing circulating insulin levels 1, 5
- Unlike sulfonylureas, it does not increase endogenous insulin secretion 4
Clinical Efficacy
Pioglitazone has demonstrated effectiveness in glycemic control:
- When used as monotherapy, pioglitazone 15-45 mg/day decreases HbA1c levels in patients with type 2 diabetes 4
- It can be used in combination with metformin, sulfonylureas, insulin, or other antidiabetic agents for enhanced glycemic control 4, 6
- Pioglitazone has shown comparable efficacy to metformin in improving glycemic control but with more pronounced improvements in insulin sensitivity 5
- It may have a more durable effect on glycemic control compared to sulfonylureas 2
Cardiovascular Effects and Safety Profile
Important considerations regarding cardiovascular effects include:
- Pioglitazone has been associated with fluid retention and edema, which may exacerbate or lead to heart failure in predisposed individuals 2
- Unlike rosiglitazone (another TZD that is no longer widely available due to concerns about increased myocardial infarction risk), pioglitazone has shown a modest benefit on cardiovascular events in patients with overt macrovascular disease 2
- Pioglitazone should be avoided in patients with NYHA class III or IV heart failure 2
- The drug has been associated with weight gain, which is a common side effect 2, 7
- Recent studies have suggested a possible increased risk of bladder cancer with pioglitazone use 2
Other Considerations
Additional important information about pioglitazone includes:
- It has beneficial effects on lipid profiles, including reduced triglycerides and increased HDL cholesterol 3, 6
- Unlike troglitazone (the first TZD that was withdrawn due to liver toxicity), pioglitazone has not shown significant hepatotoxicity 4
- Lower doses (15-30 mg) may mitigate weight gain and edema concerns 2
- Pharmacokinetics are not significantly altered in elderly patients or those with renal insufficiency 3
When prescribing pioglitazone, clinicians should be aware of its potential side effects and contraindications, particularly in patients with heart failure or at risk for bladder cancer, and should monitor patients accordingly.