What is Pioglitazone (Actos)?

Pioglitazone is an oral anti-diabetic agent that is useful in regulating blood sugar levels in patients suffering from type 2 diabetes mellitus. It acts primarily by increasing the sensitivity of fat, muscle, and liver cells to the hormone insulin. This results in significantly lower levels of blood sugar, insulin, and sugar-coated red blood cells (i.e. HBA1C which indicates control of diabetes within the last three months). Moreover, it can also reduce the sugar output by the liver, improve the levels of good cholesterol, and may even preserve the pancreas cells that secrete insulin where normally they would degrade as the disease progresses.

Pioglitazone Mechanism of Action

When pioglitazone is in the body, it works by binding to receptors on the cell surface called peroxisome proliferator activated receptor (PPAR-gamma). This receptor is found throughout the fat, muscle, and liver cells and activates the expression of a protein called glucose transporter GLUT4 which increases the sugar uptake. Insulin is further sensitized by chemical components called tumor necrosis factor alfa, resistin, and adiponectin. The free fatty acid storage shifting from non-fat cells to fat cells also enhances insulin action. A redistribution of fat stores also occurs, where fat cells deep in the organs are transferred to dermal layers that are more insulin sensitive. In a 24-week study, patients given pioglitazone were found to have a 14.9% increase in the levels of high-density lipoprotein (good cholesterol). The overall metabolic effects are contributed by these known mechanisms. Pioglitazone usually takes two hours from the time it enters the digestive tract to be present in the body system, and it takes about seven days for it to achieve a steady level of concentration.

If you are taking this medication and still have questions about how it works, contact your doctor for more information.


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