Pioglitazone: Mechanism of Action, Medical Uses, Contraindications, and Common Side Effects

It belongs to a class of drugs called thiazolidinediones.

Pioglitazone is a diabetes medicine used in conjunction with a proper diet and exercise program to control high blood sugar in patients with type 2 diabetes.

Mechanism of action

It works by helping restore your body’s proper response to insulin, thereby lowering blood sugar.

Modulates the transcription of genes involved in the control of glucose and lipid metabolism in muscle, adipose tissue, and liver.

As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues, decreases gluconeogenesis in the liver, and reduces the amount of glucose and glycosylated hemoglobin in the bloodstream.

It helps insulin take glucose from the bloodstream and move it into cells, where it is used for fuel or energy. This lowers blood sugar levels.

Medical uses

Pioglitazone is used to lower blood glucose levels in the treatment of type 2 diabetes mellitus, either alone or in combination with a sulfonylurea, metformin, or insulin.

The main study that looked at the drug, however, found no statistically significant differences in the main cardiovascular outcomes that were analyzed.

The secondary outcome of death from all causes, myocardial infarction, and stroke was lower.

Pioglitazone has also been used to treat nonalcoholic steatohepatitis (fatty liver), but this use is currently considered experimental.

Contraindications

Pioglitazone cannot be used in patients with known hypersensitivity to pioglitazone, other thiazolidinediones or any of the components of their pharmaceutical forms.

It is ineffective and possibly harmful in type 1 diabetes mellitus and diabetic ketoacidosis. Its safety in pregnancy, lactation, and people under 18 years of age has not been established.

Given previous experiences with the drug related to troglitazone, acute liver diseases are considered a contraindication for pioglitazone.

Pioglitazone and all other drugs in its class (thiazolidinediones) are absolutely contraindicated in patients with heart failure.

Most common side effects

The most common side effects that occur with pioglitazone include:

  • Diarrhea.
  • Nausea.
  • Stomachache.
  • Cold-type symptoms (upper respiratory tract infection).
  • Swelling in your legs, ankles, or feet (edema).
  • Headache.
  • Weight gain.

If these effects are mild, they can go away in a few days or a couple of weeks. If they are more severe or do not go away, talk to your doctor or pharmacist.