Pioglitazone
An oral thiazolidinedione (glitazone) that lowers insulin resistance in type 2 diabetes; it carries a boxed warning for heart failure.
Drug card
- Class
- Thiazolidinedione
- How it works
- Activating PPAR-gamma, so fat, muscle and liver respond better to insulin
- Used for
- Type 2 diabetes
- Known for
- Fluid retention and edema
- Causing or worsening heart failure
- Weight gain
- Its name
- -glitazone means a thiazolidinedione (PPAR-gamma agonist)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does pioglitazone work?
Pioglitazone is a PPAR-gamma agonist that reduces insulin resistance in muscle, fat and liver, raising insulin-dependent glucose uptake and cutting liver glucose output. It is not an insulin secretagogue and works only when insulin is present. CYP2C8 does most of its metabolism, to active metabolites, so the strong CYP2C8 inhibitor gemfibrozil roughly triples its levels.
Uses
What is pioglitazone used for?
- Type 2 diabetes
Side effects
Side effects of pioglitazone
- Fluid retention and edemaKnown for
- Causing or worsening heart failureKnown forSerious
- Weight gainKnown for
- Bone fractures, mainly in womenSerious
- Bladder cancerSerious
- Liver failure (rare)Serious
- Swelling of the retina (macular edema) with blurred visionSerious
- Small fall in hemoglobin
- Hypoglycemia with insulin or a sulfonylurea
- Upper respiratory infections and sinusitis
- Headache
- Muscle pain
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Never start it in NYHA class III–IV heart failure; avoid it in any heart failure with symptoms.
- Gemfibrozil and other strong CYP2C8 inhibitors raise its levels, so a lower maximum dose applies.
- Do not use in active bladder cancer; use with care after past bladder cancer.
- Check liver tests if symptoms suggest liver injury, and do not restart if it is confirmed.
Good to know: Not an insulin secretagogue, so hypoglycemia mainly occurs when it is combined with insulin or a sulfonylurea.
Remember it
A way to remember it
Glitazones are water-and-weight drugs.
They make the body hold fluid and add weight, so edema and heart failure (the boxed warning) are the key risks. With pioglitazone also remember two Bs: bladder cancer and broken bones.
Written for biofideX
Its name
-glitazone means thiazolidinedione (PPAR-gamma agonist)
Pioglitazone and rosiglitazone activate PPAR-gamma. Dual PPAR-alpha and gamma agonists end in -glitazar instead.
- Every drug name stem
Its class
Thiazolidinediones
Thiazolidinediones activate PPAR-gamma, a nuclear receptor and transcription factor found in fat tissue, muscle and liver. It switches on insulin-responsive genes that handle glucose and fat, so insulin resistance falls: tissues take up more glucose and the liver releases less. They need the body's own insulin to work and do not stimulate its release.
Easily mixed up with fibrates and biguanides.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Diabetes
Pioglitazone is one of 14 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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