Pharmacology · Thiazolidinediones (glitazones)
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A PPAR-gamma agonist like pioglitazone, now withdrawn from the US market and little used, because of heart failure and debated heart attack risk.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
The figure shows rosiglitazone in the ligand-binding domain of human PPAR-gamma.
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 →
Adverse effects
Common
- Edema and weight gain
- Rise in LDL cholesterol
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.
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.
Related drugs
Related conditions
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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 (MedlinePlus (U.S. National Library of Medicine), 2026); Crystal structure of Peroxisome proliferator-activated receptor gamma (PPARG)in complex with rosiglitazone (RCSB Protein Data Bank, 2020); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 51 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.