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Pioglitazone

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Pioglitazone is a drug used to treat Type 2 diabetes. It lowers blood sugar by helping the body use insulin more efficiently. As an additional health benefit, pioglitzone may also improve HDL cholesterol and triglycerides. It can be used alone or in combination with other diabetes medicines such as sulfonylureas, metformin, or insulin. Taken alone, pioglitazone does not cause hypoglycemia (low blood sugar levels).

Contents

Other Names

Uses

Diabetes is characterized by abnormally high concentrations of sugar in the blood. Pioglitazone is used to help lower both fasting and after-meal blood sugar levels in patients with type 2 diabetes (non-insulin dependent diabetes). It is used alone (monotherapy) or in combination with a sulfonylurea, metformin, or insulin when dietary and lifestyle modifications fail to control blood sugar adequately.

Pancreas in relation to other organs, and panceatic islet cells. Source: National Institute of Diabetes and Digestive and Kidney Diseases.

How Pioglitazone Is Taken

Pioglitazone is taken, in tablet form, once a day with or without food.

How It Works

Pioglitazone is a type of thiazolidinedione (TZD) that works by making tissues—especially muscle, fat, and liver—more responsive to insulin. The other marketed TZD, rosiglitazone (marketed as Avandia) has a similar mechanism of action. TZDs work in the nucleus of the cell by increasing the transcription of genes involved in glucose metabolism. As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues, increases glucose utilization, decreases production of glucose by the liver, and reduces the amount of glucose and insulin in the bloodstream.

Side Effects

Some common side effects associated with pioglitazone use are listed below:

  • Cough or cold
  • Headache
  • Inflammation of the sinuses or throat
  • Muscle pain
  • Swelling or fluid retention
  • Weight gain
  • Decreased triglycerides and increased HDL (good cholesterol)

Benefits

Uncontrolled diabetes increases the risk of disease in almost every organ system, notably the kidneys and eyes. Normalization of blood sugar with pioglitazone reduces those risks. Apart from benefits of improved blood sugar control, pioglitazone increases good (HDL) cholesterol, lowers bad (LDL) cholesterol and triglycerides, and may have other beneficial effects in limiting the progression of arterial plaques. [1] It also reduces the progression of carotid artery wall thickening, which is a marker of cardiovascular risk. This benefit has been reported in patients with or without cardiovascular disease.

Risks

Interactions

Pioglitazone may reduce the effectiveness of oral contraceptives. In some cases, other forms of birth control are needed.

High blood sugar is more likely to occur if pioglitazone is taken with drugs that elevate blood sugar, such as the following:

Low blood sugar is more likely to occur if pioglitazone is given with drugs that lower blood sugar, such as the following:

The following drugs can interact with pioglitazone:

Complications

Pioglitazone, like other thiazolidinediones, may cause or exacerbate congestive heart failure. Patient monitoring is used to detect symptoms of heart damage such as shortness of breath, swelling, and excessive weight gain. Heart failure is more likely to happen at the initiation of treatment, or after a dosage increase. Pioglitazone is not used in patients with significant symptoms of congestive heart failure before treatment.

Reports of inflammation of the liver (hepatitis) and elevated liver enzymes have surfaced in patients given pioglitazone. However, these effects may not have been due to the drug. Blood tests are used to monitor liver health if liver damage is suspected. Symptoms of liver damage include nausea, vomiting, stomach pain, a feeling of tiredness or having no energy, loss of appetite, dark urine, or jaundice (yellow coloring of eyes and skin).

Pioglitazone may cause harm to the fetus and is only used in pregnancy if necessary. In addition, pioglitazone may interfere with the monthly menstrual cycle.

Recent research also points to an unfavorable effect of pioglitazone on bone—namely, slower bone formation and faster bone loss—resulting in an increased risk of fractures. [2]

History

Pioglitazone is manufactured and marketed by Takeda Pharmaceuticals in the US as Actos and elsewhere as Glustin. It is also available in pre-made combination tablets with metformin (ACTOplus Met) or glimepiride (Duetact).

Pioglitazone chemical structure. Source: Wikimedia Commons

Pioglitazone was approved by the U.S. Food and Drug Administration in July, 1999. [3]

Alternatives

Type 2 diabetes is treated in several ways. Lifestyle modifications, especially in the areas of caloric restriction and increased physical activity, are often sufficient to control the disease, but sometimes medication is needed. Multiple drugs are used if one is not sufficient. Even in patients receiving medication, lifestyle modification is encouraged.

Research

Recent research findings have shed light on some of pioglitazone's long-term effects. In particular, pioglitazone therapy is associated with a decrease in adverse cardiac outcomes, including recurrent heart attack, in high-risk subjects. [4] A separate review of several different clinical trials concluded that pioglitazone is associated with a significantly lower risk of death, heart attack, or stroke among a diverse population of patients with diabetes. [5]

Clinical Trials

For a list of ongoing clinical trials involving pioglitazone, see Pioglitazone Trials

References

  1. ↑ Erdmann E, Dormandy J, Wilcox R, Massi-Benedetti M, Charbonnel B. PROactive 07: pioglitazone in the treatment of type 2 diabetes: results of the PROactive study. Vasc Health Risk Manag. 2007;3(4):355-70. Abstract | PDF
  2. ↑ Meier C, Kraenzlin ME, Bodmer M, Jick SS, Jick H, Meier CR. Use of thiazolidinediones and fracture risk. Arch Intern Med. 2008 Apr 28;168(8):820-5. Abstract
  3. ↑ FDA talk paper. FDA approves pioglitazone to treat type 2 diabetes. T99-33. July 16, 1999.
  4. ↑ Erdmann E. Pioglitazone and recurrent myocardial infarction in patients with diabetes and a previous myocardial infarction Cardiology Review Online Jan 2008. Full Text
  5. ↑ Lincoff AM, Wolski K, Nicholls SJ, Nissen SE. Pioglitazone and Risk of Cardiovascular Events in Patients With Type 2 Diabetes Mellitus: A Meta-analysis of Randomized Trials. JAMA 2007;298(10):1180-8. Abstract | PDF

External Links

U.S. Food and Drug Administration label: Actos (pioglitazone hydrochloride) tablets

European Medicines Agency: European public assessment report (EPAR): Glustin

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The content on or accessible through Medpedia.com is for informational purposes only. Medpedia is not a substitute for professional advice or expert medical services from a qualified health professional. Read more

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