Endocrinology

Thiazolidinediones song

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Thiazolidinediones

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Thiazolidinediones (TZDs) — pioglitazone and rosiglitazone — activate PPARγ (peroxisome proliferator-activated receptor gamma), increasing insulin sensitivity in adipose tissue, skeletal muscle, and liver.
TZDs decrease insulin resistance by promoting adipocyte differentiation and enhancing glucose uptake via increased GLUT4 expression.
Major adverse effects include fluid retention and edema, which can precipitate or worsen congestive heart failure — TZDs are contraindicated in NYHA Class III–IV heart failure.
Rosiglitazone is associated with increased risk of myocardial infarction and has severely restricted use in the US; pioglitazone is the preferred TZD in clinical practice.
TZDs cause weight gain due to fluid retention and increased fat deposition, particularly subcutaneous fat redistribution.
Long-term TZD use — especially pioglitazone — is associated with increased risk of bladder cancer; avoid in patients with active bladder cancer.
TZDs cause decreased bone mineral density and increased fracture risk, particularly in distal limbs of women.
Pioglitazone favorably affects lipid profiles by raising HDL and lowering triglycerides, distinguishing it from rosiglitazone.
TZDs have a slow onset of action — therapeutic glucose-lowering effects may take 6–12 weeks to become fully apparent.
TZDs can restore ovulation in women with polycystic ovary syndrome (PCOS) by reducing insulin resistance, increasing pregnancy risk in patients not seeking conception.