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Pioglitazone

Pioglitazone is a thiazolidinedione medicine used as an adjunct to diet and exercise to improve glycaemic control in adults with type 2 diabetes. It works only in the presence of the body’s own insulin and is not itself an insulin secretagogue; MedlinePlus’s drug information on pioglitazone and the US prescribing information for ACTOS both cover the medicine in more detail.

Actos

Type 2 Diabetes Mellitus

15mg · 30mg · 45mg

Utilised to manage glucose concentrations to alleviate chronic hyperglycaemia and support peripheral tissue metabolism.

From$0.81/ tabletView

Actoplus Met

Type 2 Diabetes Mellitus

15mg + 500mg

Designed to support glycaemic control to manage blood glucose levels and address insulin resistance.

From$2.02/ tabletView

Key points

  • Pioglitazone carries a boxed warning because thiazolidinediones, including this medicine, cause or exacerbate congestive heart failure in some patients.
  • It is metabolised mainly by the enzyme CYP2C8, with a smaller role for CYP3A4 and other isoforms.
  • Tablets are formulated with excipients that include lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium and magnesium stearate.
  • Pioglitazone should not be used to treat type 1 diabetes or diabetic ketoacidosis, as it would not be effective in these settings.

How it works

Pioglitazone acts as an agonist for peroxisome proliferator-activated receptor-gamma (PPARγ), a receptor found in tissues important for insulin action such as adipose tissue, skeletal muscle and liver. Through this action it decreases insulin resistance in the periphery and in the liver, increasing insulin-dependent glucose disposal and decreasing hepatic glucose output.

Safety specific to Pioglitazone

Pioglitazone carries a boxed warning, the FDA’s strongest alert, about heart failure. Thiazolidinediones, including pioglitazone, cause or exacerbate congestive heart failure in some patients. Anyone starting pioglitazone, or having their dose increased, needs to be watched closely for signs and symptoms of heart failure such as sudden or rapid weight gain, breathlessness, or swelling (oedema); if heart failure develops, it should be managed according to current standards of care, and stopping or reducing the dose of pioglitazone must be considered. Pioglitazone is not recommended for anyone with symptomatic heart failure, and starting it in a person with established New York Heart Association (NYHA) Class III or IV heart failure is contraindicated.

Bladder tumours have been observed in male rats in a two-year carcinogenicity study. In two three-year clinical trials in people, bladder cancer was reported in 16 of 3,656 patients taking pioglitazone (0.44%) against 5 of 3,679 patients not taking it (0.14%).

Bone fractures have also been studied: over a mean follow-up of 34.5 months, bone fractures occurred in 5.1% of women taking pioglitazone (44 of 870) against 2.5% of women taking placebo (23 of 905); no such increase was seen in men, at 1.7% on pioglitazone against 2.1% on placebo.

There have also been postmarketing reports of fatal and non-fatal liver (hepatic) failure in people taking pioglitazone, though those reports do not contain enough information to establish the probable cause with confidence. Liver function is monitored during treatment because of rare postmarketing reports of hepatocellular dysfunction.

When to seek urgent care

Seek prompt medical attention if you notice blood in your urine, or pain or urgency when passing urine, during treatment with pioglitazone, as advised in the UK product information for Pioglitazone 15 mg Tablets.

Further reading

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