[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Thiazolidinediones (glitazones)](https://durgical.com/en/pharmacology/classes/thiazolidinediones/) › Rosiglitazone

[Pharmacology](https://durgical.com/en/pharmacology/) · [Thiazolidinediones (glitazones)](https://durgical.com/en/pharmacology/classes/thiazolidinediones/)

# Rosiglitazone

A PPAR-gamma agonist like pioglitazone, now withdrawn from the US market and little used, because of heart failure and debated heart attack risk.

Updated 2026-11-01

- Class: [Thiazolidinediones (glitazones)](https://durgical.com/en/pharmacology/classes/thiazolidinediones/)
- Receptor: PPAR-gamma (nuclear receptor)
- ATC code: A10BG02

◎**PPAR-gamma (nuclear receptor)**Rosiglitazone

ⓘ The figure shows rosiglitazone in the ligand-binding domain of human PPAR-gamma.

**Target in 3D:** PPAR-gamma (nuclear receptor). PDB structure 7AWC (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/7AWC) · Drag to rotate · pinch to zoom

## Mechanism of action

Rosiglitazone is a potent, selective PPAR-gamma agonist. With RXR it switches on genes that increase fat storage in adipocytes and insulin sensitivity in muscle and liver. Unlike pioglitazone it barely changes triglycerides, and its consistent lipid effect is a rise in LDL cholesterol. Sodium retention in the kidney causes edema.

- Binds PPAR-gamma in the nucleus
- PPAR-gamma and RXR switch on insulin-action genes
- Insulin sensitivity in muscle and liver improves
- Glucose falls over weeks; salt and water are retained

## Pharmacokinetics

**Absorption**
Oral, well absorbed.

**Metabolism**
In the liver by cytochrome P450 enzymes.

**Onset and duration**
Full effect takes weeks.

## Indications

- Type 2 diabetes, with diet and exercise [Type 2 diabetes mellitus →](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

## Adverse effects

### Common

- Edema and weight gain
- Rise in LDL cholesterol

### Serious (rare, important)

- Heart failure, new or worse
- Possible increase in heart attacks (debated)
- Fractures (upper arm, hand, foot)
- Macular edema

## Contraindications

- Starting in established NYHA class III or IV heart failure
- Hypersensitivity to rosiglitazone

## Key interactions

**Gemfibrozil**
Slows its metabolism and raises its levels.

**Rifampicin**
Induces liver enzymes and lowers its levels.

**Insulin**
More fluid retention, heart failure and hypoglycemia.

## What is monitored

- Weight, edema and signs of heart failure
- Liver tests
- Lipids and HbA1c

## Administration and safety

- Oral tablet, with or without food.
- Several weeks are needed before judging the effect.

## Nursing care

- Before: heart failure and coronary history, liver tests.
- During: daily weight, edema, chest pain, breathlessness.
- Teach to report vision changes and fractures.

## Pregnancy and breastfeeding

Data in pregnancy are limited; insulin is the usual choice.

## Memory aid

Rosiglitazone: the glitazone with the 'red heart' warning. Same fluid problem as pioglitazone, plus doubts about heart attacks and higher LDL.

## Test yourself

Think of the answer, then tap the question to see it.

## How do rosiglitazone and pioglitazone differ in their effect on lipids?

Pioglitazone lowers triglycerides and raises HDL; rosiglitazone barely changes triglycerides and raises LDL cholesterol.

## Which boxed warning do both glitazones share?

They can cause or worsen congestive heart failure.

## Which eye problem is a warning with glitazones?

Macular edema.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/rosiglitazone/)

## Related drugs

- [Pioglitazone](https://durgical.com/en/pharmacology/pioglitazone/)

## Related conditions

- [Type 2 diabetes mellitus](https://durgical.com/en/conditions/type-2-diabetes-mellitus/)

[← Back to the class: Thiazolidinediones (glitazones)](https://durgical.com/en/pharmacology/classes/thiazolidinediones/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Rosiglitazone: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a699023.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Crystal structure of Peroxisome proliferator-activated receptor gamma (PPARG)in complex with rosiglitazone](https://www.rcsb.org/structure/7AWC) (RCSB Protein Data Bank, 2020); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 51 (McGraw Hill, 2023); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A10BG02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/rosiglitazone/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/rosiglitazone/